us-fda-guidance-575428717a78ff1f5a94e9098a018b5a•General Clinical Pharmacology Considerations for Pediatric Studies of Drugs, Including Biological Products
General Clinical Pharmacology Considerations for Pediatric Studies of Drugs, Including Biological Products
us-fda-guidance-575428717a78ff1f5a94e9098a018b5aGeneral Clinical Pharmacology Considerations for Pediatric Studies of Drugs, Including Biological ProductsDraft Guidance
Administrative draft guidance, not enacted legislation. This captured publisher edition preserves the listed document and attachments; later developments are not independently consolidated.
- Docket Number:
- FDA-2013-D-1275
- Issued by:
- Guidance Issuing OfficeCenter for Drug Evaluation and Research
This guidance assists sponsors of investigational new drug applications (INDs) and applicants of new drug applications (NDAs) under section 505 of the Federal Food, Drug, and Cosmetic Act (the FD&C Act), biologics license applications (BLAs) under section 351(a) of the Public Health Service Act (PHS Act), and supplements to such applications who are planning to conduct clinical studies in pediatric populations. In addition, this guidance assists clinical investigators in the design and planning of, and Institutional Review Boards (IRBs) in the assessment of, clinical studies in pediatric populations.
Effectiveness, safety, or dose-finding studies in pediatric populations involve gathering clinical pharmacology information, such as information regarding a product’s pharmacokinetics and pharmacodynamics, to inform dose selection and individualization. This guidance addresses general clinical pharmacology considerations for conducting studies so that the dosing and safety information for drugs in pediatric populations can be sufficiently characterized, leading to well-designed trials to evaluate effectiveness. This guidance focuses on the clinical pharmacology information (e.g., exposure-response, pharmacokinetics, and pharmacodynamics) that supports findings of effectiveness and safety and helps identify appropriate doses in pediatric populations. This guidance also describes how quantitative approaches (i.e., pharmacometrics) can use disease and exposure-response knowledge from relevant prior clinical studies to help design and evaluate future pediatric studies.
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General Clinical Pharmacology Considerations for Pediatric Studies of Drugs, Including Biological Products Guidance for Industry DRAFT GUIDANCE This guidance document is being distributed for comment purposes only. Comments and suggestions regarding this draft document should be submitted within 90 days of publication in the Federal Register of the notice announcing the availability of the draft guidance. Submit electronic comments to https://www.regulations.gov. Submit written comments to the Dockets Management Staff (HFA-305), Food and Drug Administration, 5630 Fishers Lane, Rm. 1061, Rockville, MD 20852. All comments should be identified with the docket number listed in the notice of availability that publishes in the Federal Register. For questions regarding this draft document, contact CDER_OCP_GPT@fda.hhs.gov U.S. Department of Health and Human Services Food and Drug Administration Center for Drug Evaluation and Research (CDER) September 2022 Clinical Pharmacology Revision 1
General Clinical Pharmacology Considerations for Pediatric Studies of Drugs, Including Biological Products Guidance for Industry Additional copies are available from: Office of Communications, Division of Drug Information Center for Drug Evaluation and Research Food and Drug Administration 10001 New Hampshire Ave., Hillandale Bldg., 4th Floor Silver Spring, MD 20993-0002 Phone: 855-543-3784 or 301-796-3400; Fax: 301-431-6353 Email: druginfo@fda.hhs.gov https://www.fda.gov/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/default.htm U.S. Department of Health and Human Services Food and Drug Administration Center for Drug Evaluation and Research (CDER) September 2022 Clinical Pharmacology Revision 1
Contains Nonbinding Recommendations Draft — Not for Implementation TABLE OF CONTENTS I. INTRODUCTION............................................................................................................. 1 II. BACKGROUND ............................................................................................................... 2 III. CLINICAL PHARMACOLOGY CONSIDERATIONS .............................................. 3 A. Pharmacokinetics .................................................................................................................5 B. Pharmacodynamics...............................................................................................................7 C. Pharmacogenomics ...............................................................................................................7 IV. ETHICAL CONSIDERATIONS ..................................................................................... 7 A. Case 1: IRB Review of a Clinical Pharmacology Study Involving Pediatric Participants Under 21 CFR 50.53 .....................................................................................................................9 B. Case 2: IRB Review of a Clinical Pharmacology Study Involving Pediatric Participants Under 21 CFR 50.52 ................................................................................................................... 10 C. Ethical Justification for Pediatric Pharmacology Studies ................................................... 10 V. THE PEDIATRIC STUDY PLAN DESIGN AND POINTS TO CONSIDER ......... 11 A. Approaches to Pediatric Studies ......................................................................................... 12 B. Alternative Approaches to Conventional PK Studies .......................................................... 15 C. Pediatric Dose Selection ...................................................................................................... 17 D. Pediatric Dosage Formulation............................................................................................. 18 E. Sample Size ......................................................................................................................... 19 F. Sample Collection ............................................................................................................... 20 G. Covariates and Phenotype Data .......................................................................................... 21 H. Drug-Drug Interactions ...................................................................................................... 23 I. Sample Analysis .................................................................................................................. 24 J. Data Analysis ...................................................................................................................... 24 K. Clinical Study Report ......................................................................................................... 25 L. Data Submission ................................................................................................................. 25
Contains Nonbinding Recommendations Draft — Not for Implementation 1 General Clinical Pharmacology Considerations for Pediatric Studies 1 of Drugs, Including Biological Products 2 Guidance for Industry1 3 4 5 This draft guidance, when finalized, will represent the current thinking of the Food and Drug 6 Administration (FDA or Agency) on this topic. It does not establish any rights for any person and is not 7 binding on FDA or the public. You can use an alternative approach if it satisfies the requirements of the 8 applicable statutes and regulations. To discuss an alternative approach, contact the FDA staff responsible 9 for this guidance as listed on the title page. 10 11 12 13 14 I. INTRODUCTION 15 16 This guidance assists sponsors of investigational new drug applications (INDs) and applicants of 17 new drug applications (NDAs) under section 505 of the Federal Food, Drug, and Cosmetic Act 18 (the FD&C Act), biologics license applications (BLAs) under section 351(a) of the Public Health 19 Service Act (PHS Act), and supplements to such applications who are planning to conduct 20 clinical studies in pediatric populations.2,3,4 In addition, this guidance assists clinical 21 investigators in the design and planning of, and Institutional Review Boards (IRBs) in the 22 assessment of, clinical studies in pediatric populations. 23 24 Effectiveness, safety, or dose-finding studies in pediatric populations involve gathering clinical 25 pharmacology information, such as information regarding a product’s pharmacokinetics and 26 pharmacodynamics, to inform dose selection and individualization. This guidance addresses 27 general clinical pharmacology considerations for conducting studies so that the dosing and safety 28 1 This guidance has been prepared by the Pediatric Working Group of the Office of Clinical Pharmacology in conjunction with the Pediatric Subcommittee of the Medical Policy Coordinating Committee in the Center for Drug Evaluation and Research at the Food and Drug Administration. 2 For the purposes of this guidance, the term sponsor refers to both sponsors and applicants. 3 For purposes of this guidance, references to drugs includes drugs approved under section 505 of the FD&C Act (21 U.S.C. 355) and biological products licensed under 351(a) of the PHS Act (42 U.S.C. 262(a)) that are regulated as drugs. Hereafter, the term drug will be used to refer to all such products. 4 This guidance is applicable to BLAs submitted under section 351(a) of the PHS Act. For the Agency’s thinking regarding clinical pharmacology considerations for BLAs submitted under section 351(k), see the FDA guidance entitled Clinical Pharmacology Data to Support a Demonstration of Biosimilarity to a Reference Product (December 2016). We update guidances periodically. For the most recent version of a guidance, check the FDA guidance web page at https://www.fda.gov/RegulatoryInformation/Guidances/default.htm. Additionally, for information about the Pediatric Research Equity Act (PREA) (section 505B of the FD&C Act) in the context of biosimilar applications, see the FDA guidance entitled Questions and Answers on Biosimilar Development and the BPCI Act (Revision 2) (September 2021).
Contains Nonbinding Recommendations Draft — Not for Implementation 2 information for drugs in pediatric populations can be sufficiently characterized, leading to well- 29 designed trials to evaluate effectiveness. 30 31 In general, this guidance focuses on the clinical pharmacology information (e.g., exposure- 32 response, pharmacokinetics, and pharmacodynamics) that supports findings of effectiveness and 33 safety and helps identify appropriate doses in pediatric populations. This guidance also describes 34 how quantitative approaches (i.e., pharmacometrics) can use disease and exposure-response 35 knowledge from relevant prior clinical studies to help design and evaluate future pediatric 36 studies. 37 38 This guidance does not describe: (1) the standards for the approval of drugs in the pediatric 39 population; (2) the determination that the course of a disease is the same in adults and pediatric 40 populations; or (3) the clinical pharmacology studies for the development of vaccine therapies, 41 blood products, or other products not regulated by the Center for Drug Evaluation and Research. 42 43 In general, FDA’s guidance documents do not establish legally enforceable 44 responsibilities. Instead, guidances describe the Agency’s current thinking on a topic and 45 should be viewed only as recommendations, unless specific regulatory or statutory 46 requirements are cited. The use of the word should in Agency guidance means that 47 something is suggested or recommended, but not required. 48 49 50 II. BACKGROUND 51 52 Over the past several decades, the FDA has tackled the problem of inadequate testing of drugs in 53 pediatric patients and inadequate pediatric use information in drug labeling. The Food and Drug 54 Administration Modernization Act of 1997 (FDAMA) addressed the need for improved 55 information about the use of drugs in the pediatric population by establishing incentives for 56 conducting pediatric studies on drugs for which exclusivity or patent protection exists.5 57 Congress subsequently passed the Best Pharmaceuticals for Children Act (BPCA)6 in 2002 and 58 the Pediatric Research Equity Act (PREA) in 2003.7 Both BPCA and PREA were reauthorized 59 in 2007.8 In 2010, the Biologics Price Competition and Innovation Act extended certain 60 provisions of the BPCA to biological products.9 In 2012, BPCA and PREA were made 61 permanent under Title V of the FDA Safety and Innovation Act (FDASIA).10 62 63 5 Public Law No. 105-115, 111 Stat. 2296 (November 21, 1997). 6 Public Law No. 107-109, 115 Stat. 1408 (January 4, 2002). 7 Public Law No. 108-155, 117 Stat. 1936 (December 3, 2003). 8 Food and Drug Administration Amendments Act of 2007 (FDAAA), Public Law No. 110-85, 121 Stat. 823 (September 27, 2007). 9 See section 351(m) of the PHS Act (42 U.S.C. 262(m)). 10 Public Law No. 11 2-144, 126 Stat. 993 (July 9, 2012).
Contains Nonbinding Recommendations Draft — Not for Implementation 3 Under BPCA, sponsors of certain applications and supplements filed under section 505 of the 64 FD&C Act and under section 351(a) of the PHS Act can obtain an additional six months of 65 exclusivity if, in accordance with the requirements of the statute, the sponsor submits 66 information responding to a Written Request from the Secretary relating to the use of a drug in 67 the pediatric population.11 68 69 Under PREA, sponsors of certain applications and supplements filed under section 505 of the 70 FD&C Act or section 351(a) of the Public Health Service Act are required to submit pediatric 71 assessments, unless they receive an applicable waiver or deferral of this requirement.12,13 If 72 applicable, sponsors must submit a request for a deferral or waiver as part of an initial pediatric 73 study plan (iPSP)14 (see section V of this guidance). 74 75 The FD&C Act requires a description of pediatric study data in labeling arising from study data 76 submitted in response to a Written Request under BPCA and/or data from studies required under 77 PREA, whether the findings are positive, negative, or inconclusive.15 The PREA requirements 78 are triggered by the submission of an application or supplement for a drug under section 505 of 79 the FD&C Act or section 351 of the PHS Act for a new active ingredient, new indication, new 80 dosage form, new dosing regimen, or new route of administration.16 If a full or partial waiver is 81 granted under PREA because there is evidence that the drug would be ineffective or unsafe in 82 some or all pediatric populations, the information must be included in the product’s labeling.17 83 84 This guidance addresses the clinical pharmacology considerations of any planned pediatric study, 85 whether or not it is conducted pursuant to BPCA or PREA.18 86 87 88 III. CLINICAL PHARMACOLOGY CONSIDERATIONS 89 90 Clinical pharmacology studies in the pediatric population should be conducted in individuals 91 with the disease which the drug is intended to treat, or in rare instances, in those who are at risk 92 of this disease. Identifying the appropriate pediatric population to study should take into 93 11 Section 505A of the FD&C Act, 21 U.S.C. 355a. 12 Section 505B of the FD&C Act, 21 U.S.C. 355c. 13 For more information, see the FDA draft guidance entitled How to Comply with the Pediatric Research Equity Act (September 2005). When final, this guidance will represent the Agency’s current thinking on this topic. 14 Section 505B(e)(2)(B) of the FD&C Act, 21 U.S.C. 355c(e)(2)(B). 15 Section 505A(j) of the FD&C Act, 21 U.S.C. 355a(j); Section 505B(g)(2) of the FD&C Act, 21 U.S.C. 355c(g)(2). 16 Section 505B(a)(1) of the FD&C Act, 21 U.S.C. 355c(a)(1). 17 Section 505B(a)(5)(D) of the FD&C Act, 21 U.S.C. 355c(a)(5)(D). 18 For more information, please see the FDA guidance entitled General Clinical Pharmacology Considerations for Neonatal Studies for Drugs and Biological Products (July 2022).
Contains Nonbinding Recommendations Draft — Not for Implementation 4 consideration: 1) the disease; 2) the profile of the drug under study; 3) scientific and ethical 94 justifications; and 4) developmental changes in the pediatric population. 95 96 Sponsors should address the entire pediatric age range (birth to <17 years of age19) in their iPSP 97 (waivers and deferrals of the requirements under PREA may be appropriate for specific age 98 ranges). The pharmacokinetics of a drug is typically evaluated over the entire pediatric age 99 range in which the agent will be used. See the FDA guidance entitled E11 Clinical Investigation 100 of Medicinal Products in the Pediatric Population (December 2000) for more information. The 101 Center for Drug Evaluation and Research generally divides the pediatric population into the 102 following groups:20 103 104 • Neonates: Birth up to 1 month21,22 105 • Infants: 1 month up to 2 years 106 • Children: 2 years up to 12 years 107 • Adolescents: 12 years up to younger than 17 years 108 109 If other categorizations such as physiologic categories based upon systems ontogeny or disease 110 pathophysiology are used, they should be supported with scientific and developmental data. 111 These categories should not be arbitrarily applied for trial enrollment but can help ensure 112 adequate inclusion of participants across the pediatric age range. 113 114 The measurement or prediction of a drug’s pharmacokinetics (exposure) and pharmacodynamics 115 (response) is essential to the clinical pharmacology assessment. It is important to describe the 116 exposure-response relationship of a drug in the pediatric population when possible to enhance 117 the understanding of effective dose ranges or support the ability to extrapolate information from 118 older pediatric participants. A pediatric drug development program should consider the time 119 course of development of the drug metabolizing enzymes, drug excretory systems, transporters 120 and drug target/receptors relevant (if known) to the drug being studied. This can be addressed by 121 characterizing the pharmacokinetics and/or pharmacodynamics of the drug across the appropriate 122 pediatric age range. 123 124 19 See 21 CFR 201.57(c)(9)(iv). 20 In 1994, the FDA revised its regulations to include more complete information about the use of a drug in pediatric populations. See the final rule on Specific Requirements on Content and Format of Labeling for Human Prescription Drugs; Revision of “Pediatric Use” Subsection in the Labeling, 59 FR 64240, 64241-42, (December 13, 1994). Pediatric age groups are described in the preamble to that final rule. Although the Agency has since further revised those labeling requirements (see the final rule on Requirements on Content and Format of Labeling for Human Prescription Drug and Biological Products, 71 FR 3922 (January 24, 2006)), the Agency’s general thinking regarding these pediatric subpopulations has remained the same. 21 In this guidance, as in the FDA guidance entitled E11(R1) Addendum: Clinical Investigation of Medicinal Products in the Pediatric Population (April 2018), the neonatal period is defined for the term and post-term newborn as the day of birth plus 27 days, and for the preterm newborn, as the day of birth, through the expected date of delivery plus 27 days. 22 For more information, please see the FDA guidance entitled General Clinical Pharmacology Considerations for Neonatal Studies for Drugs and Biological Products (July 2022).
Contains Nonbinding Recommendations Draft — Not for Implementation 5 A. Pharmacokinetics 125 126 Pharmacokinetic (PK) measures, such as area under the curve (AUC) and maximum 127 concentration (Cmax), and parameters such as clearance (CL), half-life, and volume of 128 distribution, reflect the absorption (A), distribution (D), and excretion (E) of a drug from the 129 body. Drugs can be eliminated in the unchanged (parent) form or undergo metabolism (M) to 130 one or more active and inactive metabolites. This overall set of processes is often referred to as 131 ADME, which ultimately determines the systemic exposure to a drug and its metabolites after 132 drug administration. This systemic exposure, reflected as drug or metabolite concentrations or 133 both, is generally correlated with both beneficial and adverse drug effects. All drugs show inter- 134 and intra-individual variability in PK measures and parameters. 135 136 In the pediatric population, growth and developmental changes in the factors that influence 137 ADME can lead to changes in PK parameters which can lead to changes in drug 138 response/adverse effects. Specifically, the ontogeny of drug metabolizing enzymes, transporters, 139 and receptors should be taken into account when planning and analyzing data from pediatric PK 140 studies. 141 142 The methodological issues in designing pediatric PK studies have been reviewed previously.23 143 Special areas of importance in planning pediatric PK studies are discussed in the following 144 paragraphs. 145 146 1. Absorption 147 148 Developmental changes in the pediatric population that can affect absorption include effects on 149 gastric acidity, rates of gastric and intestinal emptying, surface area of the absorption site, 150 gastrointestinal drug-metabolizing enzyme systems, gastrointestinal permeability, biliary 151 function, and transporter expression. Similarly, developmental changes in skin, muscle, and fat, 152 including changes in water content and degree of vascularization, can affect absorption patterns 153 of drugs delivered by intramuscular, subcutaneous, or percutaneous absorption.24 See section 154 V.D for a discussion on the effect of the formulation on drug absorption. 155 156 2. Distribution 157 158 Distribution of a drug can be affected by changes in body composition, such as changes in total 159 body water and adipose tissue, which are not necessarily proportional to changes in total body 160 weight. Plasma protein binding and tissue-binding changes arising from changes in body 161 composition with growth and development can also influence distribution. Differences between 162 the pediatric and adult populations in blood flow to an organ, such as the brain, can also affect 163 the distribution of a drug in the body. 164 23 Burckart, GJ, KE Estes, R Leong, Y Mulugeta, V Tandon, J Wang, DR Abernethy, and PR Jadhav, 2012, Methodological Issues in the Design of Pediatric Pharmacokinetic Studies, Pharm Med, 26:13-22. 24 Hong, L and S Rosenbaum, 2014, Developmental Pharmacokinetics in Pediatric Populations, J Pediatr Pharmacol Ther, 19(4):262-276.
Contains Nonbinding Recommendations Draft — Not for Implementation 6 165 3. Metabolism 166 167 Drug metabolism commonly occurs in the liver, but can also occur in the blood, gastrointestinal 168 wall, kidney, lung, and skin. Developmental changes in metabolizing capacity can affect both 169 bioavailability and elimination, depending on the degree to which intestinal and hepatic 170 metabolic processes are involved.25 Developmental changes in drug metabolism are well 171 recognized, and information on the ontogeny of drug metabolism in newborns, infants, and 172 children is now included in modeling approaches to predicting drug elimination in these groups. 173 Both the rates of metabolite formation and the principal metabolic pathway can be different in 174 the pediatric population compared to adults and within the pediatric population. In vitro studies 175 performed early in drug development can be useful in identifying the metabolic pathways for a 176 drug. See the FDA guidance entitled In Vitro Drug Interaction Studies - Cytochrome P450 177 Enzyme- and Transporter-Mediated Drug Interactions (January 2020) for more information. 178 179 4. Excretion 180 181 Drug excretion by the kidney is the net result of glomerular filtration, tubular secretion, and 182 tubular reabsorption. Because these processes mature at different rates in the pediatric 183 population, age can affect the systemic exposure of drugs when renal excretion is a dominant 184 pathway of elimination. The maturation of other excretory pathways, including biliary and 185 pulmonary routes of excretion, is also important. 186 187 5. Protein Binding 188 189 Protein binding to a drug or its metabolites can change with age and concomitant illness. In 190 certain circumstances, an understanding of protein binding is important to interpret the data from 191 a blood level measurement and to determine appropriate dose adjustments.26 In vitro plasma 192 protein binding studies can determine the extent of binding of the parent and the major active 193 metabolite(s) and identify specific binding proteins, such as albumin and alpha-1 acid 194 glycoprotein. 195 196 6. Clearance 197 198 Clearance of drugs as a function of age and body weight is generally a valuable parameter for 199 determining the dose in the pediatric population, and drug clearance has provided a valuable tool 200 in the assessment of pediatric clinical pharmacology studies. Scaling of drug clearance from one 201 age group to another is a commonly used approach. 202 203 25 Leeder, JS, 2004, Translating Pharmacogenetics and Pharmacogenomics into Drug Development for Clinical Pediatrics and Beyond, Drug Disc Today, 9(13):567-573. 26 Kearns, GL, SM Abdel-Rahman, SW Alander, DL Blowey, JS Leeder, and RE Kauffman, 2003, Developmental Pharmacology - Drug Disposition, Action, and Therapy in Infants and Children, NEJM, 349;12:1157-1167.
Contains Nonbinding Recommendations Draft — Not for Implementation 7 B. Pharmacodynamics 204 205 Sponsors should collect and analyze PK and, whenever possible, pharmacodynamic (PD) data in 206 pediatric studies to determine how the two are linked (i.e., the PK-PD or exposure-response 207 relationship). PD data can include the effect of the drug on biomarkers or clinical endpoints for 208 both effectiveness and safety. These measurements can allow a better understanding of whether 209 the PK-PD relationships of the drug in pediatrics are similar to those observed in adults and can 210 help derive rational dosing strategies in pediatrics. 211 212 If the clinical endpoint cannot be measured directly because the effect is delayed or infrequent, 213 then the selection of an appropriate biomarker to substitute for the clinical effectiveness or 214 toxicity endpoint is essential. Endpoint selection is a critical part of pediatric study design.27 215 216 C. Pharmacogenomics 217 218 Documentation that genetic differences can impact drug exposure and response is increasing,28 219 but the relationship between genomic profiles and developmentally regulated gene expression 220 has not been extensively studied in pediatric populations. Genotype-phenotype relationships 221 observed in adults are not always representative of those observed in pediatric populations, 222 particularly neonates and infants.29 Nevertheless, if drug exposure and/or response is dependent 223 on a well-known pharmacogenomic biomarker (e.g., cytochrome P4502D6), collecting and 224 analyzing pharmacogenetic samples in a pediatric clinical pharmacology study could provide 225 additional information for the interpretation of the PK and PD results. See the FDA guidance 226 entitled Clinical Drug Interaction Studies - Cytochrome P450 Enzyme- and Transporter- 227 Mediated Drug Interactions (January 2020) for more information. 228 229 230 IV. ETHICAL CONSIDERATIONS 231 232 FDA-regulated clinical investigations are governed, in part, by IRB regulations in 21 CFR Part 233 56 and the human subject protection regulations in 21 CFR Part 50. The requirements in 21 CFR 234 Part 50, subpart D, Additional Safeguards for Children in Clinical Investigations, apply to FDA- 235 regulated clinical pharmacology studies that enroll pediatric participants. If the proposed 236 intervention or procedure does not offer a prospect of direct clinical benefit to the individual 237 child, these safeguards restrict the allowable risk to which a pediatric participant can be exposed 238 in a clinical investigation to minimal risk (21 CFR 50.51) or no more than a minor increase over 239 27 Green, DJ, JM Burnham, P Schuette, XI Liu, BM Maas, L Yao, SK McCune, J Chen, JN van den Anker, and GJ Burckart, 2018, Primary Endpoints in Pediatric Efficacy Trials Submitted to the US FDA, J Clin Pharmacol 58(7):885-890. 28 Food and Drug Administration: Table of Pharmacogenomic Biomarkers in Drug Labeling (June 2021)), available at: https://www.fda.gov/media/124784/download (Accessed December 21, 2021). 29Green, DJ, P Mummaneni, IW Kim, JM Oh, M Pacanowski, and GJ Burckart, 2016, Pharmacogenomic Information in FDA-Approved Drug Labels: Application to Pediatric Patients, Clin Pharmacol Ther, 99(6):622-632.
Contains Nonbinding Recommendations Draft — Not for Implementation 8 minimal risk (21 CFR 50.53) unless the protocol is referred to the FDA by the IRB and allowed 240 to proceed under 21 CFR 50.54 (see further description below). 241 242 Clinical pharmacology studies generally do not provide a direct clinical benefit to individual 243 pediatric participants and must therefore present minimal risk (21 CFR 50.51) or no more than a 244 minor increase over minimal risk (21 CFR 50.53) in order to be approved by an IRB under 21 245 CFR Part 50, subpart D. However, if a clinical pharmacology study offers the prospect of direct 246 benefit to the participant, such as by ensuring that serum levels of a drug remain within the 247 therapeutic range, then the study potentially could be approvable by an IRB under 21 CFR 50.52. 248 249 Before initiation of the clinical trial, an IRB must determine that the proposed trial is in 250 compliance with the requirements of 21 CFR 50, subpart D.30 However, if FDA has concerns 251 that the rights and safety of pediatric participants may not be adequately protected, such concerns 252 could present sufficient grounds for the FDA to impose a clinical hold because the investigation 253 could present an unreasonable and significant risk of illness or injury to the pediatric participants 254 (21 CFR 312.42(b)). 255 256 The assessment of a clinical pharmacology protocol under 21 CFR part 50, subpart D depends on 257 whether the investigational drug is being administered: (1) solely for the purposes of obtaining 258 PK data; or (2) in such a way that it offers the pediatric participant a prospect of direct clinical 259 benefit. The two scenarios are discussed further in the case studies below. 260 261 Regardless of the scenario, administration of an investigational drug would generally be 262 considered to represent more than minimal risk and thus would not meet the requirements for 263 approval by an IRB under 21 CFR 50.51 (clinical investigations not involving greater than 264 minimal risk). For IRB approval under 21 CFR 50.53, the pediatric participants must have a 265 disorder or condition that is the focus of the clinical investigation, the investigational drug must 266 present experiences to those subjects that are reasonably commensurate with those inherent in 267 their actual or expected medical, dental, psychological, social, or educational situations, and the 268 clinical investigation must be likely to yield generalizable knowledge about the disease or 269 condition that is of vital importance for the understanding or amelioration of that disorder or 270 condition. For IRB approval of a clinical investigation under 21 CFR 50.52, the pediatric 271 participants must have a prospect of direct clinical benefit from administration of the 272 investigational product, the risk to the pediatric participants must be justified by the anticipated 273 benefit, and the relation of the anticipated benefit to the risk must be at least as favorable to the 274 pediatric participants as that presented by available alternative approaches. Accordingly, healthy 275 pediatric participants (i.e., without a disorder or condition which is the focus of the research) 276 cannot be enrolled in FDA-regulated clinical pharmacology studies unless the Commissioner 277 determines, after consultation with a panel of experts in pertinent disciplines and opportunity for 278 public review and comment, that the conditions in 21 CFR 50.54 are met.31 That regulation 279 applies to clinical investigations that are not approvable under 21 CFR 50.51, 50.52, or 50.53 but 280 30 See 21 CFR 56.109(h) and 21 CFR 56.111(c). 31 See the FDA guidance entitled Process for Handling Referrals to FDA Under 21 CFR 50.54 - Additional Safeguards for Children in Clinical Investigations (December 2006).
Contains Nonbinding Recommendations Draft — Not for Implementation 9 that present an opportunity to understand, prevent, or alleviate a serious problem affecting the 281 health or welfare of children. 282 283 A. Case 1: IRB Review of a Clinical Pharmacology Study Involving Pediatric 284 Participants Under 21 CFR 50.53 285 286 When the investigational drug is being administered to a pediatric participant with the disease or 287 condition for which the drug is being developed, but the intent of the study is solely for the 288 purpose of obtaining PK data, the risk(s) presented by the investigational drug, the route of 289 administration, and the PK sampling schedule must represent no more than a minor increase over 290 minimal risk (21 CFR 50.53(a)) in order to be approvable by the IRB. Pediatric participants may 291 be exposed to no more than a minor increase over minimal risk if, among other criteria, the 292 intervention or procedure is likely to yield generalizable knowledge about the subjects’ disorder 293 or condition that is of vital importance for the understanding or amelioration of that disorder or 294 condition (21 CFR 50.53(c)). Thus, for a clinical investigation to be approved by an IRB under 295 this category, the enrolled pediatric participant must have a disorder or condition that meets these 296 requirements. The FDA interprets “condition” to include being at risk for the disease (disorder) 297 based on, for example, epidemiologic, genetic, and other factors. 298 299 Furthermore, sufficient empirical data regarding the risks of the proposed interventions or 300 procedures should be available to ascertain that the risks are no more than a minor increase over 301 minimal risk (21 CFR 50.53(a)). If available, adult data (including dose-response information) 302 should be considered for this purpose. When there are not enough human data to adequately 303 characterize the risk, then the intervention or procedure generally would not be considered to 304 present no more than a minor increase over minimal risk because the risks of the intervention or 305 procedure would not be known with sufficient accuracy. 306 307 The risks of any blood and/or fluid sampling procedures also must represent no more than a 308 minor increase over minimal risk (21 CFR 50.53(a)). The limited venipunctures to obtain 309 specimens for PK analyses would generally be considered either minimal risk or a minor 310 increase over minimal risk, and therefore could be approvable by the IRB even without the 311 prospect of direct benefit (see 21 CFR 50.51(a) and 50.53(a)). This approach to the analysis of 312 clinical trials is often called a component analysis of risk, whereby to determine the overall 313 acceptability of the clinical investigation, the risks and anticipated direct clinical benefits of the 314 interventions included in a protocol are analyzed individually as well as collectively.32,33,34 315 316 An example of a clinical pharmacology study that generally would fall under 21 CFR 50.53 is 317 the pharmacokinetics of the oral administration of a single dose of an over-the-counter cough and 318 cold product. To be enrolled in such a study, a child would either be symptomatic from an upper 319 32 See the National Commission for the Protection of Human Subjects of Biomedical and Behavioral Research, Research Involving Children: Report and Recommendations of the Commission for the Protection of Human Subjects of Biomedical and Behavioral Research, (43 FR 2084, 2086), January 13, 1978. 33 See Preamble to the Final Rule, Additional Safeguards for Children in Clinical Investigations of Food and Drug Administration-Regulated Products, (78 FR12937, 12937-12950), February 26, 2013. 34 See the FDA guidance entitled Acute Bacterial Otitis Media: Developing Drugs for Treatment (October 2012).
Contains Nonbinding Recommendations Draft — Not for Implementation 10 respiratory infection (URI) or be at risk for a future URI based on the presence of criteria such as 320 the frequency of past infections, number of people living in the home, or exposure to others in a 321 preschool or school setting. As stated above, the associated blood draws to collect PK samples 322 would generally be considered to be minimal risk (21 CFR 50.51(a)) or no more than a minor 323 increase over minimal risk (21 CFR 50.53(a)) and a single oral dose of the over-the-counter 324 cough and cold product would generally be considered as no more than a minor increase over 325 minimal risk (21 CFR 50.53(a)), thus allowing the study to proceed under 21 CFR 50.53. 326 327 If administration of a single dose of an investigational drug exceeds a minor increase over 328 minimal risk (or there are insufficient data available to make that determination), the clinical 329 pharmacology study either would be required to meet the requirements in 21 CFR 50.52 (as 330 discussed below) or would require referral for review under 21 CFR 50.54 (assuming that the 331 other requirements of that regulation were met). 332 333 B. Case 2: IRB Review of a Clinical Pharmacology Study Involving Pediatric 334 Participants Under 21 CFR 50.52 335 336 The administration of an investigational drug with more than a minor increase over minimal risk 337 could be approved by an IRB if the level of risk exposure is justified by a sufficient prospect of 338 direct clinical benefit to the participants (21 CFR 50.52(a)). For example, dose-monitoring 339 studies that ensure serum levels of an investigational drug remain within a therapeutic range 340 generally would fall under 21 CFR 50.52 when the investigational drug presents the prospect of 341 direct benefit to the enrolled pediatric participants and the investigational drug is administered 342 under the protocol using a dosing regimen (including duration) that offers a sufficient prospect of 343 direct clinical benefit to justify the risks (21 CFR 50.52(a)). 344 345 Multiple-dose PK-PD studies can be designed to offer a prospect of direct benefit, but the dose 346 and duration of exposure to the investigational product should be sufficient to result in potential 347 changes in the clinical manifestations of the condition or in disease-specific biomarkers that 348 reflect a clinical benefit. For example, the duration of the PK-PD study could be extended, or 349 perhaps combined as the lead-in phase to an efficacy trial, to provide a suitable duration of drug 350 exposure that offers a sufficient prospect of direct clinical benefit to justify the risks.35 351 352 C. Ethical Justification for Pediatric Pharmacology Studies 353 354 Adequate information from clinical pharmacology studies to support pediatric dosing is critical 355 to the development of ethically sound confirmatory trials. Inadequate pediatric dosing may lead 356 35 Roth-Cline, M and RM Nelson, 2015, Ethical Considerations in Conducting Pediatric and Neonatal Research in Clinical Pharmacology, Curr Pharm Design, 21:5619-5635.
Contains Nonbinding Recommendations Draft — Not for Implementation 11 to failed pediatric clinical trials.36 The FDA considers the public health need for adequate 357 pediatric dosing in its assessment of the ethical propriety of proposed studies.37,38 358 359 360 V. THE PEDIATRIC STUDY PLAN DESIGN AND POINTS TO CONSIDER 361 362 A sponsor who is planning to submit a marketing application (or supplement to an application) 363 for a new active ingredient, new indication, new dosage form, new dosing regimen, or new route 364 of administration is required to submit an iPSP39 unless the drug is for an indication for which 365 orphan designation has been granted.40 In addition, a sponsor who is planning to submit, on or 366 after August 20, 2020, an original application for a new active ingredient that is subject to the 367 molecularly targeted cancer drug provision of PREA (i.e., the drug that is the subject of the 368 application is intended for the treatment of an adult cancer and is directed at a molecular target 369 that the FDA determines to be substantially relevant to the growth or progression of a pediatric 370 cancer) is also required to submit an iPSP,41 regardless of whether the drug is for an indication 371 for which orphan designation has been granted.42 By statute, a biosimilar product that has not 372 been determined to be interchangeable with the reference product is considered to have a new 373 active ingredient for purposes of PREA.43 374 375 The submission of the iPSP is intended to encourage sponsors to consider pediatric studies early 376 in product development and, when appropriate, begin planning for these studies. The FDA 377 guidance entitled Pediatric Study Plans: Content of and Process for Submitting Initial Pediatric 378 Study Plans and Amended Pediatric Study Plans (July 2020) discusses the content of and process 379 for submitting initial and amended PSPs and states that Section 10.1 (Pediatric Pharmacokinetic 380 or Pharmacokinetic/Pharmacodynamic Studies) should include: 381 382 36 Benjamin, DK, Jr, PB Smith, P Jadhav, JV Gobburu, MD Murphy, V Hasselblad, C Baker-Smith, RM Califf, and JS Li, 2008, Pediatric Antihypertensive Trial Failures: Analysis of End Points and Dose Range, Hypertension, 51(4):834-840. 37 See the FDA guidance entitled E6(R2) Good Clinical Practice: Integrated Addendum to ICH E6(R1) (March 2018). 38 This issue is also discussed in the American Academy of Pediatrics Guidelines for the Ethical Conduct of Studies to Evaluate Drugs in Pediatric Populations. See Shaddy, R and SC Denne, 2010, Clinical Report-Guidelines for the Ethical Conduct of Studies to Evaluate Drugs in Pediatric Populations, Pediatrics,125(4):850-860. 39 See section 505B(e)(1) of the FD&C Act; 21 U.S.C. 355c(e)(1); and section 505B(a)(1)(A) of the FD&C Act; 21 U.S.C. 355c(a)(1)(A). 40 See section 505B(k)(1) of the FD&C Act; 21 U.S.C. 355c(k)(1). 41 See section 505B(e)(1) of the FD&C Act; 21 U.S.C. 355c(e)(1); and section 505B(a)(1)(B) of the FD&C Act; 21 U.S.C. 355c(a)(1)(B). 42 See section 505B(k)(2) of the FD&C Act; 21 U.S.C. 355c(k)(2). 43 See section 505B(l) of the FD&C Act; 21 U.S.C. 355c(l).
Contains Nonbinding Recommendations Draft — Not for Implementation 12 • The type of study/study design 383 384 • The objectives of the study 385 386 • The age group and population in which the study will be conducted 387 388 • The pediatric formulation(s) to be used in the study 389 390 • The dose ranges to be used in the PK studies 391 392 • The endpoints and justification (PK parameters; PD parameters) 393 394 • The existing or planned modeling and simulation to support dose selection and/or study 395 design, data analysis, and interpretation for planned pediatric studies 396 397 • Any planned pharmacogenomic analyses 398 399 • A justification for the sample size 400 401 When designing pediatric clinical studies, sponsors should be mindful that modeling and 402 simulation and pharmacologic considerations are often critical for the successful completion of a 403 study. Modeling and simulation (e.g., PK, PD, and trial simulations) should use all of the 404 information available and be an integral part of all pediatric development programs followed by 405 verification using results from pediatric clinical studies. The following sections are critically 406 important when developing the clinical pharmacology components of a pediatric study plan. 407 408 A. Approaches to Pediatric Studies 409 410 There are several recognized approaches to providing substantial evidence to support the safe 411 and effective use of drugs in pediatric populations.44 In some cases, previous data in adults and 412 other pediatric indications can be leveraged to provide this substantial evidence. This concept is 413 often referred to as pediatric extrapolation. 414 415 Pediatric extrapolation of efficacy is defined as an approach to providing evidence in support of 416 effectiveness of drugs in the pediatric population when it can be assumed that the course of the 417 disease and the expected response to a medicinal product would be sufficiently similar in the 418 pediatric and reference (adult or other pediatric) populations.45 Determination of the extent of 419 pediatric extrapolation is predicated on the understanding of the disease and drug effect in the 420 reference (adult or other pediatric) population and their similarity to the target pediatric 421 44 For more information, see the FDA draft guidance entitled Demonstrating Substantial Evidence of Effectiveness for Human Drug and Biological Products (December 2019). When final, this guidance will represent the Agency’s current thinking on this topic. 45 See the FDA guidance entitled E11(R1) Addendum: Clinical Investigation of Medicinal Products in the Pediatric Population (April 2018). See also 21 CFR 314.55(a).
Contains Nonbinding Recommendations Draft — Not for Implementation 13 population. The data necessary to support efficacy when pediatric extrapolation is considered 422 will depend upon the existing data and the gaps in knowledge that should be addressed.46 423 Examples of potential approaches based on the availability and confidence in existing data are 424 discussed in sections 1 through 3 below. 425 426 While it is helpful and provides additional evidence to support extrapolation, formally 427 establishing and documenting similarity in exposure-response in adults and target pediatric 428 population is not a requirement in order to consider some degree of extrapolation. Exposure- 429 response assessments are, however being conducted more frequently in both adult and pediatric 430 patients. Knowledge of exposure-response, when available, can play a critical role in informing 431 the assessment of drug effect similarity between adults and pediatric patients and the 432 acceptability of an exposure-matching approach. In addition, exposure-response information can 433 serve a crucial role in supporting pediatric dose selection, dose optimization and formulation 434 development. When applicable, similarity in exposure-response relationships on a clinically 435 relevant biomarker or an appropriate clinical endpoint can contribute to an assessment of the 436 appropriateness of efficacy extrapolation from adults to pediatric patients. 437 438 Additionally, the extent of the required pediatric safety data can take into consideration prior 439 experience with similar drugs in pediatric populations and the seriousness of the adverse events 440 in adults or in pediatric populations. Usually, additional safety data in the indicated pediatric 441 indication will be needed. See the FDA guidance entitled E11(R1) Addendum: Clinical 442 Investigation of Medicinal Products in the Pediatric Population (April 2018) for more 443 information. The potential for pediatric patients to have a significantly different incidence, 444 severity, and types of adverse events compared to adults should always be considered.47,48 445 446 1. PK, Safety, and Efficacy Approach 447 448 If the disease or disease progression is unique to pediatric patients or its progression and/or 449 response to intervention is undefined or dissimilar to that in adults, then the pediatric 450 development program should use a PK, safety, and efficacy approach. The objectives of the 451 studies in the pediatric program would be to characterize the PK and exposure-response 452 relationships to help optimize pediatric dosing strategies and to provide evidence of effectiveness 453 and safety. A population PK analysis can be conducted using PK data from the efficacy study to 454 confirm PK estimates in the age subgroups. 455 456 46 See the FDA guidance entitled E11 Clinical Investigation of Medicinal Products in the Pediatric Population (December 2000) for more information. 47 Liu XI, P Schuette, GJ Burckart, DJ Green, J La, JM Burnham, N Rakhmanina, A Robb, SM Huang, and JN van den Anker, 2019, A Comparison of Pediatric and Adult Safety Studies for Antipsychotic and Antidepressant Drugs Submitted to the US FDA, J Pediatrics, doi: 10.1016/j.jpeds.2018.12.033. 48 Momper JD, Y Chang, M Jackson, P Schuette, S Seo, I Younis, DR Abernethy, L Yao, EV Capparelli, and GJ Burckart, 2015, Adverse Event Detection and Labeling in Pediatric Drug Development: Antiretroviral Drugs, Ther Inn Reg Sci, 49(2):302-309.
Contains Nonbinding Recommendations Draft — Not for Implementation 14 2. PK, Safety, and PD/Efficacy Approach 457 458 This approach should be considered when the disease and intervention are believed to behave 459 similarly in pediatrics and adults, but the exposure-response relationship in pediatrics is either 460 inadequately documented or assumed to not be sufficiently similar to adults. A clinically 461 relevant PD biomarker may be appropriate for purposes of evaluating the evidence of 462 effectiveness and to select pediatric doses. In the absence of a clinically relevant PD biomarker, 463 clinical measures (e.g., symptoms, signs, outcomes) may be appropriate. The number, type, and 464 size of pediatric studies to support a pediatric program depends on the residual uncertainty 465 associated with understanding of similarity of the disease and drug effect. 466 467 For the two approaches described above, response data in pediatric studies should be collected 468 and analyzed. Response or PD data can include biomarkers or clinical endpoints for both safety 469 and effectiveness. The specific endpoints, including those for an exposure-response evaluation, 470 for each drug should be discussed with the Agency. Appropriate endpoint selection and 471 enrichment strategies for the pediatric population in a trial are important. Of note, endpoints that 472 are unique to pediatric participants have been previously associated with failed pediatric trials 473 and should be carefully considered.49 474 475 3. PK and Safety Approach 476 477 The PK and safety approach should be considered when there is evidence that adults and 478 pediatrics share a sufficiently similar disease course and response to intervention to allow for 479 exposure matching to establish efficacy. 480 481 A PK study should be performed to identify the pediatric dose that will provide an exposure 482 similar to that found to be effective in adults. The antibacterial therapeutic area is a good 483 example of this approach, where the organism is expected to respond to similar systemic 484 concentrations in adults and pediatrics. In this example, the study should focus on identifying 485 the doses in the pediatric setting that would result in exposures similar to those attained in adults. 486 The criteria for determining exposure matching should be prospectively agreed upon with the 487 Agency before initiating these studies.50 488 489 Before conducting a PK study in any of these approaches, simulations should be performed to 490 identify initial dosing regimens. Clinical trial simulations may be performed to determine a trial 491 design, sample size, and the appropriateness of an endpoint for the pediatric study. Refining 492 models with available data can help verify assumptions made during the design of the study. 493 494 49 Green DJ, J Burnham, P Schuette, XI Liu, BM Maas, L Yao, SK McCune, J Chen, JN van den Anker, and GJ Burckart, 2018, Primary Endpoints in Pediatric Efficacy Trials Submitted to the US FDA, J Clin Pharmacol, 58(7):885-890. 50 Mulugeta, Y, JS Barrett, R Nelson, AT Eshete, A Mushtaq, L Yao, N Glasgow, AE Mulberg, D Gonzalez, D Green, J Florian, K Krudys, S Seo, I Kim, D Chilukuri, and GJ Burckart, 2016, Exposure Matching for Extrapolation of Efficacy in Pediatric Drug Development, J Clin Pharmacol, 56(11):1326-1334.
Contains Nonbinding Recommendations Draft — Not for Implementation 15 B. Alternative Approaches to Conventional PK Studies 495 496 A dedicated PK study with intensive PK sampling may not be necessary in every age group. For 497 example, prior experience with dosing in adolescent participants has demonstrated that 498 knowledge of adult dosing and appropriate dose scaling can be sufficient for some drugs with 499 adequate justification. When a dedicated PK study is not considered essential or cannot be 500 conducted, it may be appropriate to use sparse PK sampling in the safety and/or efficacy studies 501 to confirm dose predictions. Modeling and simulation can also be used, when appropriate, to 502 help to fill these gaps in knowledge. See the FDA guidance entitled Considerations for the 503 Inclusion of Adolescent Patients in Adult Oncology Clinical Trials (March 2019) for more 504 information. 505 506 Other approaches beyond the use of conventional PK studies with intensive blood sampling may 507 be appropriate in pediatric participants to obtain useful drug exposure information, including: 508 509 • Sparse PK sampling with the use of modeling and simulation 510 511 • Opportunistic approaches that use excess blood collected for laboratory studies51 512 513 • Use of alternative specimens: 514 515 o Urine and saliva collection are noninvasive. However, the interpretation of drug 516 analyses of either source is complicated and requires careful consideration before 517 use. 518 519 o Likewise, tissue or cerebrospinal fluid collected for clinical purposes present both 520 an opportunity and a challenge for the appropriate interpretation of these results 521 in understanding the pharmacokinetics of the drug. 522 523 Modeling and simulation can help reduce the uncertainty about drug dosing in pediatric 524 populations. Model-informed drug development has been applied in regulatory applications for 525 pediatric drug development.52 Population PK approaches are commonly used, and 526 physiologically based PK (PBPK) approaches are increasingly applied in pediatric drug 527 development. In addition, quantitative systems pharmacology (QSP) models can help 528 51 For more information, see the FDA guidance entitled General Clinical Pharmacology Considerations for Neonatal Studies for Drugs and Biological Products (July 2022). 52 Bi, Y, J Liu, L Li, J Yu, A Bhattaram, M Bewernitz, R Li, C Liu, J Earp, L Ma, L Zhuang, Y Yang, X Zhang, H Zhu, and Y Wang, 2019, Role of Model-Informed Drug Development in Pediatric Drug Development, Regulatory Evaluation, and Labeling, J Clin Pharmacol, 59(S1):S104-S111.
Contains Nonbinding Recommendations Draft — Not for Implementation 16 incorporate disease processes.53,54 As science and technology continue to advance, in silico and 529 other alternative modeling study methods can provide preliminary data to inform the design and 530 conduct of PK-PD studies for investigational drugs in pediatric populations. For example, the 531 development of a PBPK in silico model that integrates drug-dependent parameters (e.g., 532 physicochemical properties, hepatic intrinsic clearance, affinities to metabolic enzymes, 533 transporters, and proteins) and system- and age-dependent parameters (e.g., blood flow rate, 534 protein contents, tissue and organ size and composition, and enzyme and transporter abundances 535 and activities) is one possible approach. 536 537 Various modeling approaches have been used in pediatric drug development programs for a 538 variety of purposes, including: 539 540 • Planning for a first-in-pediatric PK study 541 542 • Optimizing the study design 543 544 • Verifying the model in specific age groups 545 546 • Recommending starting doses 547 548 • Informing enzyme ontogeny using a benchmark drug 549 550 • Facilitating covariate analysis for the effects of organ dysfunction or drug interactions in 551 pediatric participants55 552 553 The model selected should incorporate in vivo PK-PD data obtained in other groups of pediatric 554 and adult participants as well as human volunteer studies, as appropriate. To account for growth 555 across the pediatric population for modeling purposes, refer to standardized growth charts. The 556 Centers for Disease Control and Prevention (CDC) growth charts provide a preliminary 557 assessment of the weight ranges that can be anticipated within specific age groups.56 For 558 example, weights can vary 2.5- to 3-fold in healthy children between the 10 th percentile at 2 559 years and 90th percentile at age 6 (10.6 kg to 25.3 kg for males) and between the 10th percentile at 560 53 Momper, JD, GJ Burckart, and P Jadhav, 2013, Applications of Population Pharmacokinetics for Pediatric Drug Development, Pediatric Drug Development: Concepts and Applications, AE Mulberg, D Murphy and LL Mathis, Chichester, UK, John Wiley & Sons Ltd. 54 Wang, J, AN Edginton, D Avant, and GJ Burckart, 2015, Predicting Neonatal Pharmacokinetics From Prior Data Using Population Pharmacokinetic Modeling, J Clin Pharmacol, 55(10):1175-1183. 55 Leong, R, MLT Vieira, P Zhao, Y Mulugeta, CS Lee, SM Huang, and GJ Burckart, 2012, Regulatory Experience With Physiologically Based Pharmacokinetic Modeling for Pediatric Drug Trials, Clin Pharmacol Ther, 91(5):926- 931. 56 Centers for Disease Control and Prevention, National Center for Health Statistics, 2000 CDC Growth Charts for the United States: Methods and Development (May 2002), available at: http://www.cdc.gov/nchs/data/series/sr_11/sr11_246.pdf (Accessed September 17th, 2019).
Contains Nonbinding Recommendations Draft — Not for Implementation 17 6 years and the 90th percentile at 12 years (17.7 kg to 54 kg in males). Caution should be taken 561 in the use of standardized growth charts as they do not always represent the target pediatric 562 patient population. 563 564 C. Pediatric Dose Selection 565 566 Selecting a dose(s) and an age range should consider the overall benefit/risk profile of the drug. 567 When possible, a range of doses should be studied in the pediatric population. 568 569 Factors for consideration in dose selection include: 570 571 • The similarity of the disease and exposure-response in pediatric and adult groups 572 573 • The relative bioavailability of the new formulation compared to the previous 574 formulations 575 576 • The age and developmental stage of the pediatric population 577 578 • Any pharmacogenomic characteristics of the drug 579 580 • The toxicity of the drug 581 582 • Any PK data from other pediatric populations 583 584 Because there can be limited information on the safety of the dose to be administered to a 585 neonate or infant, the dose range used in initial studies requires careful consideration.57 When 586 developmental maturation and body size changes impact dosing, modeling and simulation can 587 help define an initial pediatric dosing in order to adequately minimize the risk for specific age 588 groups. Initial doses within a pediatric age group are typically normalized to body size (e.g., 589 mg/kg), but developmental maturation can be an additional critical factor to be considered in 590 establishing initial doses in some age groups. In some pediatric participants such as adolescents, 591 body weight or surface area-based dosing are not always necessary. In some cases, final dosing 592 recommendations can include tiered dosing based on weight bands. 593 594 There are situations in which interpolation or scaling can reduce the uncertainty regarding initial 595 pediatric dosing. PK or PD information in certain pediatric age groups can be gained by 596 interpolating or bridging from existing data in adults, pediatric participants in other age groups, 597 or both. However, bridging of data to younger pediatric age groups, particularly neonates, 598 should be done cautiously and confirmed. Significant developmental differences that can exist 599 between young pediatric age groups and older pediatric age groups or adults are associated with 600 considerable differences in metabolism and drug disposition. This difference can lead to an 601 altered dose-exposure relationship and therefore the dose-response relationships. 602 603 57 For more information, see the FDA guidance entitled General Clinical Pharmacology Considerations for Neonatal Studies for Drugs and Biological Products (July 2022).
Contains Nonbinding Recommendations Draft — Not for Implementation 18 When initial PK studies are not feasible (see section IV), an adaptive design to selecting a dose 604 can be practical for the pediatric clinical studies. Adaptive designs should be prospectively 605 determined. See the FDA guidance entitled E11(R1) Addendum: Clinical Investigation of 606 Medicinal Products in the Pediatric Population (April 2018) for more information. 607 608 When separate efficacy studies in pediatrics are not conducted (i.e., for the PK and safety only 609 approach described in section V.A above), in general, PK studies in the pediatric population 610 should determine how the dosage regimen should be adjusted to achieve the same level of 611 systemic exposure in adults. Differences in intersubject variability in these PK measures and/or 612 parameters between age groups or between pediatric and adult populations should be interpreted 613 with regard to their impact on dosing, safety, and/or efficacy. In these instances, the sponsor 614 should pre-specify the criteria by which exposure matching is acceptable. For example, one 615 approach is to select the appropriate dosing strategy through simulations which result in pediatric 616 exposures within the 5th to 95th percentile shown to be safe and effective in adults. 617 618 Estimating the exposure-response relationship across a range of body-size doses (dose/kg or 619 dose/m 2) can be important. For the PK and PD/efficacy approaches discussed in section V.A2 620 above, investigating a range of doses and exposures allows for an assessment of those 621 relationships and the development of rational dosing instructions. The sponsor should also 622 consider determining the variability in achieved systemic exposures in the pediatric population in 623 the context of the exposure-response relationships for pharmacodynamics or efficacy. 624 625 When PK-PD data are available, the dose range should account for observed differences in 626 response between adults and the pediatric population, both in terms of exposure and response. 627 For example, there is evidence that pediatric populations are on average less sensitive to 628 antihypertensive drugs than the adult population.58 Therefore, pediatric studies could include 629 exposures greater than the highest drug exposure associated with the approved adult dose, 630 provided that prior data about the exposure-response relationship and safety information justify 631 such an exposure. Studies of distinctly different ranges of exposure are desirable to provide 632 sufficient information for the calculation of an optimal dose. 633 634 D. Pediatric Dosage Formulation 635 636 Pediatric formulations that permit accurate dosing and enhance adherence (e.g., palatability) are 637 an important part of pediatric drug development.59 See the FDA guidance entitled E11 Clinical 638 58 Benjamin, DK, Jr, PB Smith, P Jadhav, JV Gobburu, MD Murphy, V Hasselblad, C Baker-Smith, RM Califf, and JS Li, 2008, Pediatric Antihypertensive Trial Failures: Analysis of End Points and Dose Range, Hypertension, 51(4):834-840. 59 Refer to the FDA draft guidance entitled Use of Liquids and/or Soft Foods as Vehicles for Drug Administration: General Considerations for Selection and In Vitro Methods for Product Quality Assessments (July 2018) for information on the use of liquids and/or soft foods for drug administration. When final, this guidance will represent the Agency’s current thinking on this topic. In addition, refer to the following FDA guidances for more information on assessing the bioavailability and effect of food on a new formulation: Assessing the Effects of Food on Drugs in INDs and NDAs - Clinical Pharmacology Considerations (June 2022) and Bioavailability Studies Submitted in NDAs or INDs - General Considerations (April 2022).
Contains Nonbinding Recommendations Draft — Not for Implementation 19 Investigation of Medicinal Products in the Pediatric Population (December 2000) for more 639 information. If there is a pediatric indication, an age-appropriate dosage formulation must be 640 made available for pediatric patients in all relevant age groups.60 One way to fulfill this 641 requirement, when the adult formulation is not acceptable for the planned pediatric age range, is 642 to develop and test a pediatric formulation and seek approval for that formulation. To the extent 643 practicable, sponsors should include information in the iPSP regarding planned excipients that 644 will be contained in a pediatric formulation. 645 646 The bioavailability of any formulation used in pediatric studies should be characterized in 647 relation to the adult formulation. In some circumstances, a relative bioavailability study 648 comparing the age-appropriate formulation to the approved drug may be required.61 These 649 studies are generally performed in adults due to ethical reasons. Potential drug-food or vehicle 650 interactions should be considered, such as those that have been reported with apple juice.62 651 652 E. Sample Size 653 654 1. Number of Pediatric Participants 655 656 Prior knowledge of the disease, exposure, and response from adult and other relevant pediatric 657 data, such as that related to variability, can be used to derive a sample size for ensuring precise 658 parameter estimation. The sponsor should account for all potential sources of variability, 659 including inter-subject and intra-subject variability as well as differences between the adult and 660 pediatric populations when making the final selection of the sample size for each age group. 661 662 The distinct age groups to be studied should be chosen based upon what is known about potential 663 changes in drug response with age, the development of the drug-metabolizing enzymes and 664 excretory mechanisms, as well as safety considerations. Pediatric studies in all age groups 665 should be initiated as early as possible in drug development. The sequential study of age 666 cohorts, starting with the oldest pediatric age group, may be appropriate when there is a clear 667 rationale for doing so. If the drug is intended to be used in newborn infants, the iPSP should 668 specify how premature infants will be considered in the study population. 669 670 Because the selected age groups (strata) will be drug product-specific, the sponsor should discuss 671 the stratification plan, the distribution of the number of pediatric participants within each 672 stratum, and the appropriateness of these strata with the Agency.63 Justification should be 673 provided for the sample size selected. For example, one approach would be to prospectively 674 60 See section 505B(a)(2) of the FD&C Act, 21 U.S.C. 355c(a)(2). 61 21 CFR 320.21. 62 Abdel-Rahman, SM, MD Reed, TG Wells, and GL Kearns, 2007, Considerations in the Rational Design and Conduct of Phase I/II Pediatric Clinical Trials: Avoiding the Problems and Pitfalls, Clin Pharmacol Ther, 81(4):483- 494. 63 McMahon, AW, K Watt, J Wang, D Green, R Tiwari, and GJ Burckart, 2016, Stratification, Hyopthesis Testing, and Clinical Trial Simulation in Pediatric Drug Development, Ther Inn Regu Sci, doi: 10.1177/2168479016651661.
Contains Nonbinding Recommendations Draft — Not for Implementation 20 target a 95 percent confidence interval within 60 percent and 140 percent of the geometric mean 675 estimates of clearance and volume of distribution for the drug in each pediatric stratum with at 676 least 80 percent power. Noncompartmental analysis (NCA) based on rich PK sampling, 677 population PK modeling analysis based on sparse PK sampling, or other scientifically justified 678 methods can be applied as appropriate to achieve this precision standard.64 679 680 Conceivably, certain disease states might not allow for the recruitment of an adequate number of 681 participants to meet the above standard, and as such, practical considerations should be taken 682 into account in determining the sample size. 683 684 2. Number of Samples Per Participant 685 686 In addition to the number of participants, the number of blood samples collected in the clinical 687 pharmacology study to estimate PK measures and parameters for each individual in the study 688 should be carefully considered. The amount of blood or number of samples possible is very 689 limited in some pediatric participants such as neonates (for more on collection of blood or 690 plasma samples, see section F below). Clinical trial simulations and optimal sampling strategies 691 are recommended to justify the proposed sampling scheme. 692 693 F. Sample Collection 694 695 The volume and frequency of blood sampling are often of concern in pediatric studies. Blood 696 samples can be obtained by direct venipuncture, through the use of an indwelling intravascular 697 catheter, or when appropriate, by capillary sampling. Because repeated venipuncture can cause 698 discomfort and bruising at the puncture site, an indwelling intravascular catheter should be used 699 when possible. The volume and frequency of blood sampling may be minimized by using micro- 700 volume drug assays, dried blood spots, and sparse-sampling techniques. See the FDA guidance 701 entitled Bioanalytical Method Validation (May 2018) for more information. These types of 702 assays and analysis are especially relevant when studying neonates.65 Modern assay techniques 703 allow small sample volumes to be used to determine drug concentrations, but data quality can be 704 affected if the sample volume is insufficient to allow for reanalysis when necessary. Blood 705 samples for analysis should be collected from the circulating blood volume and not from 706 reservoir dead space created by catheters or other devices. Sampling technique is critical when 707 using the available pediatric indwelling intravenous catheters. The time of sample collection, 708 proper sample transportation and storage, and sample handling techniques should be 709 documented. The collection of fluids such as cerebral spinal fluid (CSF) or bronchial fluids can 710 be beneficial when samples are being obtained for clinical purposes. Noninvasive sampling 711 procedures, such as urine and saliva collection, may be sufficient if correlated with outcomes or 712 if the correlation with blood, serum or plasma levels has been documented. 713 714 64 Wang, Y, PR Jadhav, M Lala, and JV Gobburu, 2012, Clarification on Precision Criteria to Derive Sample Size When Designing Pediatric Pharmacokinetic Studies, J Clin Pharmacol, 52:1601-1606. 65 Long, D, G Koren, and A James, 1987, Ethics of Drug Studies in Infants: How Many Samples are Required for Accurate Estimation of Pharmacokinetic Parameters in Neonates?, J Pediatrics, 111(6Pt1):918-921.
Contains Nonbinding Recommendations Draft — Not for Implementation 21 Samples for DNA should be collected when appropriate, as discussed in section III of this 715 guidance. See also the FDA guidance entitled Clinical Pharmacogenomics: Premarket 716 Evaluation in Early-Phase Clinical Studies and Recommendations for Labeling (January 2013) 717 for more information. 718 719 G. Covariates and Phenotype Data 720 721 Growth and developmental changes in the pediatric population create substantial changes in the 722 ADME characteristics of a drug. PK measures and parameters for a drug should be described as 723 a function of age and be related to some measure of body size, such as height, weight, or body 724 surface area (BSA). The maturational changes in systems affecting ADME, such as membrane 725 transporters and metabolizing enzymes, should be considered when choosing age groups and 726 doses to study in the pediatric population (see section III). 727 728 The sponsor should, at a minimum, obtain the following covariates for each pediatric participant: 729 730 • Age 731 • Body weight 732 • Height 733 • Calculated BMI 734 • Gestational age 735 • Post-menstrual and postnatal age for neonates66 736 • Race and ethnicity 737 • Sex 738 • Laboratory tests reflecting the function of organs responsible for drug elimination 739 • Concomitant and recent drug therapy 740 741 The impact of the disease state and obesity upon drug disposition and response should be 742 considered.67 Sponsors are encouraged to collect DNA samples in pediatric PK studies under the 743 circumstances described in section III, along with appropriate phenotype information to optimize 744 the interpretation of pharmacogenomics findings. For example, when genotype information is 745 obtained for a cytochrome P450 enzyme, the sponsor should investigate the influence of genetic 746 mutations on pharmacokinetics, pharmacodynamics, and/or dose-response to determine whether 747 genetically defined subsets of patients need special dosing considerations. 748 749 The sponsor should examine the relationship between the covariates and the pharmacokinetics of 750 the drug of interest. The contribution of weight or BSA and age to PK variability should be 751 assessed. Examples of practices for assessing the effect of age on pediatric pharmacokinetics 752 could include: 753 66 See the FDA guidance entitled General Clinical Pharmacology Considerations for Neonatal Studies for Drugs and Biological Products (July 2022) for more information. 67 Vaughns JD, LS Conklin, Y Long, P Zheng, F Faruque, D Green, J van den Anker, and GJ Burckart, 2018, Obesity and Pediatric Drug Development, J Clin Pharmacol, doi:10.1002/jcph.1054.
Contains Nonbinding Recommendations Draft — Not for Implementation 22 754 • Identifying the accurate relationship between a drug’s pharmacokinetics and body weight 755 or BSA using allometric scaling 756 757 • Analyzing the residuals versus age, after accounting for body weight or the BSA effect 758 on CL, followed by a more formal analysis exploiting the physiological understanding 759 underlying CL, if appropriate. Testing for other biologically relevant predictive factors 760 for determining the pharmacokinetics of a drug in pediatrics can be important. The 761 covariate analysis may be performed on pooled data sets to allow for comparisons 762 between adults and/or different pediatric subgroups. 763 764 1. Immunogenicity 765 766 The pharmacokinetics of a drug such as therapeutic proteins can be affected by immunogenicity 767 to the drug. Immunogenicity to the administered product can negatively impact the safety and/or 768 efficacy of the drug. Therefore, assessing the immunogenicity of the relevant drugs and 769 determining its impact on pharmacokinetics, safety, and efficacy are critical components of drug 770 development and post-marketing surveillance. See the following FDA guidances for more 771 information: 772 773 • Immunogenicity Assessment for Therapeutic Protein Products (August 2014) 774 775 • Immunogenicity Testing of Therapeutic Protein Products - Developing and Validating 776 Assays for Anti-Drug Antibody Detection (January 2019) 777 778 In general, it is not appropriate to apply findings of the immunogenicity potential of a drug from 779 adult populations to pediatric populations; therefore, evaluation of the immunogenicity potential 780 of a drug should be conducted in pediatric trials regardless of the knowledge gained from adult 781 trials. 782 783 2. Renal Function 784 785 For drugs that are renally cleared, exposures can be impacted by both the maturation of kidney 786 function and renal impairment due to kidney disease. For this reason, pediatric patients with 787 impaired renal function should be recruited for clinical study when it is possible and ethically 788 justifiable to do so. One commonly used equation for the estimation of renal function is the 789 bedside Schwartz equation;68 however, in general any widely accepted measurement method 790 (where necessary) or equation for the estimation of renal function in pediatric PK studies is 791 acceptable69 and should be described in the protocol and labeling when relevant dose 792 68 Schwartz, GJ, A Munoz, MF Schneider, RH Mak, F Kaskel, BA Warady, and SL Furth, 2009, New Equations to Estimate GFR in Children with CKD, J Amer Soc Nephrol 20(3):629-637. 69 Muhari-Stark E and GJ Burckart, 2018, Glomerular Filtration Rate Estimation Formulas for Pediatric and Neonatal Use, J Pediatr Pharmacol Ther, 23(6):424–431.
Contains Nonbinding Recommendations Draft — Not for Implementation 23 adjustments are derived. Sponsors should be aware of the laboratory methods used for the 793 measurement of creatinine, as this can influence which equation is useful. 794 795 Data from adults are generally used to complement the information obtained in pediatrics to 796 characterize the relationship between renal function and pharmacokinetics. Modeling and 797 simulation approaches should be applied to derive dosing recommendations for the entire 798 pediatric age range in which the product will be used.70 Generally, for children over the age of 2 799 years, where kidney function maturation is considered complete, the need for dose adjustment 800 should be evaluated and derived based on information evaluated in adults. For children less than 801 2 years of age, the additional impact of renal function ontogeny should be considered.71 802 Quantitative approaches such as PBPK analysis can also be explored to address dosing needs in 803 these situations. Of note, the application of modeling is limited by current understanding of 804 ontogeny and is particularly challenging in neonates. However, modeling approaches should use 805 all of the clinical information available. 806 807 H. Drug-Drug Interactions 808 809 In general, evaluations of drug-drug interactions (DDIs) are performed in adults. In some cases, 810 however, the potential or magnitude of a DDI in pediatrics can differ from that observed in 811 adults. Such differences in DDIs in pediatrics compared to adults can potentially be attributed to 812 the ontogeny of metabolizing enzymes and transporters as well as differences in intragastric pH, 813 gastric emptying, intestinal motility, or protein binding. Differences in diet, concomitant 814 medications, drug formulation, and dosing regimen could also contribute to differences in DDIs 815 between adults and pediatrics.72 816 817 Considering potential ethical concerns for standalone DDI studies in pediatrics, quantitative 818 approaches such as PBPK analyses should be explored to address pediatric DDIs during drug 819 development when differences in DDI are expected. Refer to the following FDA guidances for 820 more information: 821 822 • Clinical Drug Interaction Studies - Cytochrome P450 Enzyme- and Transporter- 823 Mediated Drug Interactions (January 2020) 824 825 • Physiologically Based Pharmacokinetic Analyses — Format and Content (September 826 2018) 827 828 70 For information on studying trial participants with impaired renal function, see the FDA draft guidance entitled Pharmacokinetics in Patients with Impaired Renal Function — Study Design, Data Analysis, and Impact on Dosing (September 2020) for general concepts of study design. When final, this guidance will represent FDA’s current thinking on the topic. 71 Zhang Y, N Mehta, E Muhari-Stark, GJ Burckart, J van den Anker, L Yao, and J Wang, 2019, Pediatric Renal Ontogeny and Applications in Drug Development, J Clin Pharmacol, 59(S1):S9-S20. 72 Salerno, SN, GJ Burckart, SM Huang, and D Gonzalez, 2019, Pediatric Drug-Drug Interaction Studies: Barriers and Opportunities, Clin Pharmacol Ther 105(5):1067-1070.
Contains Nonbinding Recommendations Draft — Not for Implementation 24 Planning for DDI evaluations should be included as a section of the iPSP under Pediatric 829 Pharmacokinetic Studies and should address the impact of DDIs on drug dosing in specific age 830 groups. See the FDA guidance entitled Pediatric Study Plans: Content of and Process for 831 Submitting Initial Pediatric Study Plans and Amended Pediatric Study Plans (July 2020) for 832 more information. 833 834 I. Sample Analysis 835 836 An accurate, precise, sensitive, specific, and reproducible analytical method to quantify the drug 837 and metabolites in the biological fluids of interest is essential. See the FDA guidance entitled 838 Bioanalytical Method Validation (May 2018) for more information. The sponsor should choose 839 a method that is readily adaptable and uses only minimum sample volumes. 840 841 J. Data Analysis 842 843 The development of PK models should occur throughout the pediatric development program. 844 All prior knowledge, including adult data, should be used to develop initial models which can be 845 adapted as new data become available in pediatric subgroups. There are several basic 846 approaches for performing PK analysis in pediatrics. Population PK and noncompartmental PK 847 approaches are two of the most commonly used; however, novel approaches may be acceptable as 848 justified by the sponsor. 849 850 1. Population Analysis 851 852 A common approach for analyzing data from pediatric clinical pharmacology studies is the 853 population approach to PK analysis. Population PK accommodates rich (intensive) and 854 infrequent (sparse) sampling of blood, serum, or plasma from a larger population than in a 855 compartmental or noncompartmental analysis PK approach to determine the PK parameters. 856 Sparse sampling is generally considered more acceptable for pediatric studies because the total 857 volume of blood sampled in an individual can be minimized. Sampling can even be performed 858 concurrently with clinically necessary blood or urine sampling (e.g., opportunistic PK studies). 859 Because relatively large numbers of pediatric participants are studied, and samples can be 860 collected at various times of the day and repeated over time in a given participant, estimates of 861 both population and individual means, as well as estimates of intra- and inter-subject variability, 862 can be obtained if the population PK study is properly designed. See the FDA guidance entitled 863 Population Pharmacokinetics (February 2022) for more information. 864 865 Exposure-response analyses predominantly employ a population analysis approach. Individual 866 analysis is generally not recommended unless responses from a wide range of doses from each 867 participant are available. Modeling of data across all study participants typically provides the 868 best opportunity to describe the exposure-response relationship. See the FDA guidance entitled 869 Exposure-Response Relationships – Study Design, Data Analysis, and Regulatory Applications 870 for more information (May 2003). 871 872 2. Noncompartmental Analysis 873 874
Contains Nonbinding Recommendations Draft — Not for Implementation 25 If consistent with relevant ethical considerations (see Section IV: Ethical Considerations), it may 875 be possible to utilize intensive PK sampling with relatively frequent blood and urine sample 876 collection, when administering either single or multiple doses of a drug to a relatively small 877 group of study participants. Samples are collected over specified time intervals chosen on the 878 basis of absorption and disposition half-lives, and subsequently assayed for either total or 879 unbound concentrations of drug and relevant metabolites. Noncompartmental analysis is a 880 general approach to establish PK statistics and parameters such as AUC, C max, CL, volume of 881 distribution, and half-life, which are descriptive of the concentration of drug or metabolite over 882 time. Data are usually expressed as the means of the relevant measure or parameter and inter- 883 individual variances. In this approach, including a sufficient number of study participants to give 884 a precise estimate of the mean is essential, as discussed in section V.E. If drug administration 885 and sampling are repeated in a participant in the PK study, some understanding of intra- 886 individual variability in PK parameters can be obtained. 887 888 K. Clinical Study Report 889 890 The clinical study report should follow the FDA guidance entitled E3 Structure and Content of 891 Clinical Study Reports (January 2013) for the general content and the format of the pediatric 892 clinical study report. The evaluation of exposure-response relationships and the population PK 893 analyses should be included as stipulated in the following FDA guidances: 894 895 • Exposure-Response Relationships – Study Design, Data Analysis, and Regulatory 896 Applications (May 2003) 897 898 • Population Pharmacokinetics (February 2022) 899 900 When submitting PK information, the sponsor should submit data that illustrate the relationship 901 between the relevant PK parameters (e.g., CL unadjusted and adjusted for body size in the 902 manner described in section VI.G) and important covariates (e.g., age, renal function) in addition 903 to the results of noncompartmental analysis. 904 905 L. Data Submission 906 907 The preferred submission standard for clinical data is the Clinical Data Interchanges Standards 908 Consortium (CDISC) Study Data Tabulation Model (SDTM) standard. Please see the FDA Data 909 Standards Advisory Board73 and the CDER Study Data Standards web sites for more 910 information.74 The sponsor should also submit PK and exposure-response data used for 911 modeling and simulation in an SAS.XPT-compatible format. 912 73 See the FDA Data Standards Advisory Board, available at: https://www.fda.gov/industry/fda-resources-data- standards. 74 See the FDA Study Data Standards for Submission to CDER, available at: https://www.fda.gov/industry/study- data-standards-resources/study-data-submission-cder-and-cber.
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