us-fda-guidance-3dc24c31504c2f84ff37672a02234cca•Chronic Hepatitis B Virus Infection: Developing Drugs for Treatment
Chronic Hepatitis B Virus Infection: Developing Drugs for Treatment
us-fda-guidance-3dc24c31504c2f84ff37672a02234ccaChronic Hepatitis B Virus Infection: Developing Drugs for TreatmentGuidance
Administrative guidance, not enacted legislation. This captured publisher edition preserves the listed document and attachments; later developments are not independently consolidated.
- Docket Number:
- FDA-2018-D-3903
- Issued by:
- Guidance Issuing OfficeCenter for Drug Evaluation and Research
The Food and Drug Administration (FDA or Agency) is announcing the availability of a guidance for industry entitled “Chronic Hepatitis B Virus Infection: Developing Drugs for Treatment.” The purpose of this guidance is to assist sponsors in the clinical development of drugs and biologics for the treatment of chronic hepatitis B virus (HBV) infection from the initial investigational new drug application (IND) through the new drug application (NDA)/biologics license application (BLA) and postmarketing phases.
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Chronic HepaƟƟs B Virus InfecƟon: Developing Drugs for Treatment Guidance for Industry
U.S. Department of Health and Human Services Food and Drug AdministraƟon Center for Drug EvaluaƟon and Research (CDER) April 2022 Clinical/AnƟmicrobial
Chronic HepaƟƟs B Virus InfecƟon: Developing Drugs for Treatment Guidance for Industry AddiƟonal copies are available from: Office of CommunicaƟons, Division of Drug InformaƟon Center for Drug EvaluaƟon and Research Food and Drug AdministraƟon 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 hƩps://www.fda.gov/drugs/guidance-compliance-regulatory-informaƟon/guidances-drugs
U.S. Department of Health and Human Services Food and Drug AdministraƟon Center for Drug EvaluaƟon and Research (CDER) April 2022 Clinical/AnƟmicrobial
TABLE OF CONTENTS I. INTRODUCTION ......................................................................................................................1 II. BACKGROUND ........................................................................................................................2 III. DEVELOPMENT PROGRAM ......................................................................................................3 A. General Drug Development ConsideraƟons.............................................................................3 1. Early Phase Development ConsideraƟons ...................................................................................... 4 a. Pharmacology/toxicology development consideraƟons ......................................................... 4 b. Nonclinical virology development consideraƟons .................................................................. 6 c. Clinical pharmacology consideraƟons ..................................................................................... 9 2. Drug Development PopulaƟon ....................................................................................................... 9 3. Safety ConsideraƟons ................................................................................................................... 11 B. Phase 3 Efficacy Trial ConsideraƟons ..................................................................................... 12 1. Trial Design................................................................................................................................... 12 a. Chronic suppressive therapy ................................................................................................. 12 b. Finite duraƟon therapy ......................................................................................................... 13 2. Trial PopulaƟon ............................................................................................................................ 15 3. Entry Criteria ................................................................................................................................ 15 4. RandomizaƟon, StraƟficaƟon, and Blinding ................................................................................ 16 5. Specific PopulaƟons ..................................................................................................................... 16 a. PaƟents with HBV/HIV-1 coinfecƟon ..................................................................................... 16 b. PaƟents with HBV/HDV coinfecƟon ...................................................................................... 16 c. Pediatric paƟents .................................................................................................................. 17 6. Dose SelecƟon .............................................................................................................................. 19 7. Efficacy Endpoints ........................................................................................................................ 19 8. Trial Procedures and Timing of Assessments ............................................................................... 21 9. StaƟsƟcal ConsideraƟons ............................................................................................................. 21 a. Analysis populaƟons.............................................................................................................. 22 b. Efficacy analyses .................................................................................................................... 23 c. Handling missing data ........................................................................................................... 23 10. Accelerated Approval (Subpart H/I) ConsideraƟons ................................................................ 23 11. Benefit-Risk ConsideraƟons ..................................................................................................... 24
C. Other ConsideraƟons ............................................................................................................ 24 1. Clinical Virology ConsideraƟons ................................................................................................... 24 2. PharmacokineƟc/Pharmacodynamic ConsideraƟons .................................................................. 27 3. Labeling ConsideraƟons ............................................................................................................... 28 GLOSSARY OF ACRONYMS ................................................................................................................. 29 REFERENCES...................................................................................................................................... 30
Contains Nonbinding RecommendaƟons 1 Chronic HepaƟƟs B Virus InfecƟon: Developing Drugs for Treatment Guidance for Industry1 This guidance represents the current thinking of the Food and Drug AdministraƟon (FDA or Agency) on this topic. It does not establish any rights for any person and is not binding on FDA or the public. You can use an alternaƟve approach if it saƟsfies the requirements of the applicable statutes and regulaƟons. To discuss an alternaƟve approach, contact the FDA office responsible for this guidance as listed on the Ɵtle page. I. INTRODUCTION The purpose of this guidance is to assist sponsors in the clinical development of drugs and biologics for the treatment of chronic hepaƟƟs B virus (HBV) infecƟon from the iniƟal invesƟgaƟonal new drug applicaƟon (IND) through the new drug applicaƟon (NDA)/biologics license applicaƟon (BLA) and postmarkeƟng phases. 2 Sponsors are also encouraged to communicate with the Division of AnƟvirals through the pre-IND consultaƟon program to obtain advice in the development of drugs with unique consideraƟons based on mechanism of acƟon, novel treatment approaches, or the use of novel biomarkers. 3 This guidance does not address development of vaccines or blood-derived products, which are regulated by the Center for Biologics EvaluaƟon and Research. This guidance also does not discuss general issues of staƟsƟcal analysis or clinical trial design. Those topics are addressed in the ICH guidances for industry 1 This guidance has been prepared by the Division of Antivirals in the Center for Drug Evaluation and Research at the Food and Drug Administration. 2 For the purposes of this guidance, all references to drugs include both human drugs and therapeutic biological products unless otherwise specified. 3 See the Division of Antivirals Pre-IND Letter of Instruction web page at https://www.fda.gov/drugs/pre-ind- consultation-program/division-anti-viral-dav-pre-ind-letter-instruction.
Contains Nonbinding RecommendaƟons 2 E9 StaƟsƟcal Principles for Clinical Trials (September 1998) and E10 Choice of Control Group and Related Issues in Clinical Trials (May 2001), respecƟvely. 4 The contents of this document do not have the force and effect of law and are not meant to bind the public in any way, unless specifically incorporated into a contract. This document is intended only to provide clarity to the public regarding exisƟng requirements under the law. FDA guidance documents, including this guidance, should be viewed only as recommendaƟons, unless specific regulatory or statutory requirements are cited. The use of the word should in Agency guidances means that something is suggested or recommended, but not required. II. BACKGROUND HBV is an enveloped DNA virus belonging to the Hepadnavirus family. The highly stable covalently closed circular viral DNA (cccDNA) funcƟons as a nonreplicaƟve minichromosome and persists throughout the lifespan of infected hepatocytes. The cccDNA is not eliminated by currently approved therapies that include drugs from the nucleoside/nucleoƟde reverse transcriptase inhibitor (NrtI) class, and pegylated interferon. Chronic HBV (CHB) infecƟon results in progressive liver disease ranging from asymptomaƟc to severe disease with complicaƟons including cirrhosis, liver failure, and the development of hepatocellular carcinoma (HCC). In untreated adults with CHB, the cumulaƟve 5-year incidence of cirrhosis is 8 to 20 percent; and among those with cirrhosis, the 5-year cumulaƟve risk of hepaƟc decompensaƟon is 20 percent, and risk of HCC is 2 to 5 percent (Terrault et al. 2016). An effecƟve vaccine and anƟviral therapies are approved for the prevenƟon of HBV infecƟon and treatment of CHB, respecƟvely. Currently available therapies achieve sustained suppression of HBV DNA while on treatment, but rates of HBV surface anƟgen (HBsAg) loss with or without seroconversion to anƟ-HBsAg (HBsAb) remain low. Sustained HBV DNA suppression is associated with serum alanine aminotransferase (ALT) normalizaƟon and improvement in liver histology including regression of hepaƟc fibrosis and cirrhosis (Chang et al. 2010; Marcellin et al. 2013; BuƟ et al. 2015). EffecƟve anƟviral therapy for CHB reduces disease-related complicaƟons, such as hepaƟc decompensaƟon and liver failure, and decreases risk of HCC (Lok et al. 2016; Papatheodoridis et al. 2017). Clearance of HBsAg is associated with reduced risk of hepaƟc decompensaƟon and improved survival (Terrault et al. 2016). HBsAg loss is considered the best predictor of sustained remission off-treatment (Terrault et al. 2016). New finite duraƟon therapies target 4 We update guidances periodically. For the most recent version of a guidance, check the FDA guidance web page at https://www.fda.gov/regulatory-information/search-fda-guidance-documents.
Contains Nonbinding RecommendaƟons 3 treatment regimens that can achieve sustained suppression of HBV DNA off-treatment with HBsAg loss (with or without HBsAb seroconversion) with low risk of virologic relapse (as defined by HBV DNA) and minimal risk of liver disease progression aŌer the treatment is stopped (Lok et al. 2017). III. DEVELOPMENT PROGRAM A. General Drug Development ConsideraƟons This secƟon discusses nonclinical and early phase clinical development consideraƟons, followed by issues related to the target populaƟon for drug development, assessment of acƟvity in early phase trials, and safety consideraƟons.
Contains Nonbinding RecommendaƟons 4 1. Early Phase Development ConsideraƟons Early clinical evaluaƟon should provide sufficient data to establish safety and evidence of anƟviral acƟvity to support the phase 3 trials. a. Pharmacology/toxicology development consideraƟons Pharmacology/toxicology development consideraƟons for single invesƟgaƟonal drugs intended to treat CHB should follow the approaches outlined in exisƟng guidances for drug development. 5 When a combinaƟon of two or more early stage invesƟgaƟonal drugs to treat CHB is being developed, sponsors should discuss with the FDA whether combinaƟon toxicology studies are needed (including the design of such studies) to support clinical trials for the intended combinaƟon. When combinaƟon toxicology studies are conducted, usually no more than two drugs should be tested simultaneously in a parƟcular arm of a toxicology study. Nonclinical combinaƟon studies of an invesƟgaƟonal drug plus an approved drug or licensed biological product generally are not needed unless data from nonclinical studies of an invesƟgaƟonal drug suggest a potenƟal for serious synergisƟc toxicity with an approved drug or licensed biological product. In general, sponsors developing drugs intended to treat CHB with proposed treatment duraƟons of 6 months or more should conduct carcinogenicity studies. 6 Sponsors should submit carcinogenicity studies with an iniƟal NDA. However, under limited circumstances and with prior wriƩen agreement, the FDA may consider allowing sponsors to submit the completed carcinogenicity studies during the postmarkeƟng period under secƟon 505(o)(3) of the Federal Food, Drug, and CosmeƟc Act (FD&C Act) 7 , as long as the studies have been iniƟated before NDA submission. 5 See the ICH guidances for industry M3(R2) Nonclinical Safety Studies for the Conduct of Human Clinical Trials and Marketing Authorization for Pharmaceuticals (January 2010) and S6(R1) Preclinical Safety Evaluation of Biotechnology-Derived Pharmaceuticals (May 2012). 6 See the ICH guidance for industry S1A The Need for Long-Term Rodent Carcinogenicity Studies of Pharmaceuticals (March 1996). 7 See also the draft guidance for industry Postmarketing Studies and Clinical Trials—Implementation of Section 505(o)(3) of the Federal Food, Drug, and Cosmetic Act (October 2019). When final, this guidance will represent the FDA’s current thinking on this topic. For the most recent version of a guidance, check the FDA guidance web page at https://www.fda.gov/regulatory-information/search-fda-guidance-documents.
Contains Nonbinding RecommendaƟons 5 Sponsors developing biological products should follow approaches outlined in ICH S6(R1) and discuss their proposals for a carcinogenicity risk assessment with the FDA during clinical development to facilitate a final assessment needed to support a BLA.
Contains Nonbinding RecommendaƟons 6 b. Nonclinical virology development consideraƟons Sponsors should consider recommendaƟons for general anƟviral drug development in the draŌ guidance for industry AnƟviral Product Development—ConducƟng and Submiƫng Virology Studies to the Agency (February 2014).8 The FDA encourages detailed study reports describing the mechanism of acƟon, anƟviral acƟvity in cell culture, cytotoxicity, and mitochondrial toxicity (Marroquin et al. 2007; Arnold et al. 2012), animal models,9 and resistance studies. AddiƟonally, sponsors are advised to provide the following nonclinical virology data for invesƟgaƟonal drugs developed specifically for the treatment of CHB. Resistance and cross-resistance HBV is differenƟated into 10 genotypes (A through J) with many different subtypes. Drugs targeƟng viral proteins or sequence targets will likely be impacted by genotype- and subtype-specific variaƟons that occur in the drug target as well as variaƟons that evolve in the presence of the drug that allow the virus to develop resistance. Therefore, characterizing resistance pathways and their relaƟonship to HBV genomic variaƟons helps idenƟfy subjects who will benefit from the drug and also helps idenƟfy potenƟal cross-resistance with other drugs having a similar mechanism of acƟon. HBV does not generally grow well enough in cell culture to select for resistant virus in the presence of drug. When possible, we recommend that resistance assessments be performed for all animal studies that assess the anƟviral acƟvity of an invesƟgaƟonal drug in infected animals receiving the drug that experience viral breakthrough. In addiƟon, a resistance monitoring plan for idenƟfying changes in viral targets associated with treatment failure should be included in the protocols or can be submiƩed separately for each clinical trial that will treat subjects with CHB. Amino acid subsƟtuƟons or nucleoƟde mutaƟons associated with the development of resistance (i.e., changes from baseline) to an invesƟgaƟonal drug should be determined by sequencing the drug target and validated by introducing resistance-associated subsƟtuƟons or mutaƟons into the HBV reference genome using site-directed mutagenesis and determining the fold-shiŌ in 8 When final, this guidance will represent the FDA’s current thinking on this topic. 9 We support the principles of the 3Rs (reduce/refine/replace) for animal use in tesƟng when feasible. FDA encourages sponsors to consult with review divisions when considering a nonanimal tesƟng method believed to be suitable, adequate, validated, and feasible. FDA will consider if the alternaƟve method could be assessed for equivalency to an animal test method.
Contains Nonbinding RecommendaƟons 7 suscepƟbility. Results from these studies help idenƟfy resistance pathways and support the drug’s proposed mechanism of acƟon. Lack of a shiŌ in suscepƟbility does not exclude a resistance associaƟon for a specific subsƟtuƟon or mutaƟon that occurs in two or more independent events. Cross-resistance should be assessed to determine if resistance against approved HBV drugs with the same target confers resistance to the drug being developed and vice versa. The development of cross- resistance to epitopes of approved HBV vaccines should be assessed. ConsideraƟons for oligonucleoƟde-based invesƟgaƟonal drugs Knockdown of viral protein expression via oligonucleoƟde-based therapeuƟcs is an acƟve area for the development of anƟviral drugs. These drugs, which have a nucleic acid target, present potenƟal off- target binding at mismatched sequences that could lead to species-specific toxiciƟes not necessarily detected in toxicology studies. Therefore, we recommend that sequence-dependent off-target assessments be conducted for such drugs using appropriate in silico and in vitro methodologies to idenƟfy potenƟal off-target mismatches that can be invesƟgated and potenƟally monitored during clinical development. The Division recognizes that many addiƟonal factors, such as temporal and cell type specific expression, pharmacokineƟc (PK) properƟes, and hybridizaƟon-dependent efficiencies may be considered in the overall risk assessment of potenƟal off-target effects (refer to Lindow et al. 2012 for a general approach). The following points should be considered when designing sequence-dependent off-target assessments: Several different classes of oligonucleoƟde-based therapeuƟcs (small interfering RNAs and anƟsense oligonucleoƟdes, etc.) exist. The criteria for defining high-risk off-target mismatches are expected to differ for each class; appropriate criteria should be provided and jusƟfied for each drug. All elements of the oligonucleoƟde drug product that are potenƟally available for mismatch binding should be assessed, including both the sense and anƟsense strands, overlapping ends, etc. There are mulƟple in silico approaches that may be considered, and we recommend sponsors jusƟfy the methods and approaches used. In silico studies can be used to do the following:
Contains Nonbinding RecommendaƟons 8 – IdenƟfy all potenƟal off-target mismatches, regardless of Ɵssue expression, in the human transcriptome, including the mitochondrial transcriptome; for each of these, describe available informaƟon on mouse knockouts and human geneƟc diseases. Sponsors should specify and jusƟfy the criteria for defining a potenƟal off-target mismatch. – Determine whether each off-target site in the human transcriptome is conserved in the animal species in which anƟviral assessments and pivotal toxicology studies are performed. – Determine the variaƟon within the off-target mismatches in the transcriptomes of different ethnic populaƟons in the United States, when feasible, to assess whether certain populaƟons may be more suscepƟble to off-target effects than others. In vitro assessments of possible off-target binding (cell-based analysis, RNA-seq, etc.) should be conducted to confirm or eliminate the importance of each off-target mismatch determined via in silico assessments. An overall risk assessment of potenƟal off-target effects should be provided along with the off- target assessment data. ConsideraƟons for drugs developed to modulate innate and adapƟve immune responses Drugs developed to modulate innate and adapƟve immune responses to chronic HBV infecƟon are likely to target host factors and induce or repress immune biomarkers before having an impact on HBV replicaƟon or clearance of HBV infected hepatocytes. Nonclinical studies should describe the specific mechanism of acƟon of the drug and demonstrate that immune modulaƟon in cell culture and animal models of HBV infecƟon results in suppression of HBV replicaƟon, as measured by HBV DNA or HBsAg loss, or that the HBV cccDNA reservoir is reduced by assessing cccDNA levels. In addiƟon, given that these drugs may target host factors, it is important to determine that the target of the drug is conserved, having similar affinity between the animal species being assessed and the human target. TargeƟng host factors For drugs targeƟng host factors, polymorphisms in the gene encoding the target should be assessed to determine whether the drug will be more effecƟve or less effecƟve in different populaƟons. Sponsors should idenƟfy key racial and ethnic groups in the United States who will be part of the proposed
Contains Nonbinding RecommendaƟons 9 indicaƟon at the iniƟaƟon of drug development. If a nonclinical assay to assess the drug effect is available, mulƟple samples from each of these groups in the United States should be evaluated to determine whether race or ethnicity may be a factor contribuƟng to efficacy (Forde et al. 2013). Samples should be collected during clinical trials to determine the virus genotype of subjects who respond less favorably to treatment. c. Clinical pharmacology consideraƟons In general, dose selecƟon for early efficacy trials should be predicted to provide plasma drug exposures that exceed by severalfold the protein binding-adjusted, cell culture EC 50 value of the drug for the relevant HBV genotype/subtype. In cases where either total (protein bound plus unbound) or free (unbound) drug concentraƟons in plasma may not be related to anƟviral acƟvity, sponsors may provide jusƟficaƟon for dose selecƟon based on drug concentraƟon in other relevant Ɵssues. The dose selecƟon should also consider the safety data from the previous phase 1 trials and animal studies. Sponsors should refer to the appropriate clinical pharmacology guidances for industry to inform the need and design of drug-drug interacƟon studies and PK studies in paƟents with renal or hepaƟc impairment. 10 We encourage sponsors to conduct these studies, if needed, early in development to inform the management of drug interacƟons and the inclusion of paƟents with renal and hepaƟc impairment in phase 3 trials as appropriate. See secƟon III. B. 6., Dose SelecƟon, for dose selecƟon for phase 2 and 3 trials and secƟon III. C. 2., PharmacokineƟc/Pharmacodynamic ConsideraƟons, for other PK and pharmacodynamic consideraƟons. 2. Drug Development PopulaƟon Therapies should be developed for use in a wide range of paƟents with CHB, including pediatric populaƟons. Early phase clinical trials should focus on the adult populaƟon without cirrhosis. IniƟal trials can be conducted in HBV e anƟgen posiƟve (HBeAg-posiƟve) or HBV e anƟgen negaƟve (HBeAg-negaƟve) 10 See the guidance for industry Pharmacokinetics in Patients With Impaired Hepatic Function: Study Design, Data Analysis, and Impact on Dosing and Labeling (May 2003). See also the guidances for industry Clinical Drug Interaction Studies—Cytochrome P450 Enzyme- and Transporter-Mediated Drug Interactions (January 2020), In Vitro Drug Interaction Studies—Cytochrome P450 Enzyme- and Transporter-Mediated Drug Interactions (January 2020), and the draft guidance for industry Pharmacokinetics in Patients With Impaired Renal Function—Study Design, Data Analysis, and Impact on Dosing (September 2020). When final, this guidance will represent the FDA’s current thinking on these topics.
Contains Nonbinding RecommendaƟons 10 paƟents with acƟve disease who are treatment-naïve, or those who were previously treated but currently viremic, off-treatment. Trials can also be conducted in HBeAg-posiƟve or HBeAg-negaƟve paƟents who are virally suppressed on NrtIs. In addiƟon to endpoints discussed in secƟon III. B., sponsors can evaluate exploratory endpoints in early phase trials to gather data to inform and support the choice of appropriate endpoints in late phase trials, parƟcularly those evaluaƟng treatments of finite duraƟons. Some of these exploratory endpoints may include the following: • Change in quanƟtaƟve HBsAg (qHBsAg) concentraƟon at various Ɵme points on treatment • QuanƟtaƟve HBeAg levels • QuanƟtaƟve HBV RNA levels • QuanƟtaƟve HBV core-related anƟgen (HBcrAg) levels • cccDNA quanƟficaƟon • QuanƟtaƟve HBsAg levels from integrated HBV genome fragments • QuanƟtaƟve HBsAg-anƟ-HBs immune complex levels Also depending on the drug’s mechanism of acƟon, liver biopsy findings can be used in certain proof-of- concept studies to further understand the effect of the drug on the cccDNA reservoir and/or to help beƩer understand potenƟal surrogate markers of anƟviral acƟvity. CHB is a global disease, and clinical trials are oŌen conducted in mulƟple countries. FDA will accept a well-designed and well-conducted foreign clinical study not conducted under an IND as support for an IND or applicaƟon for markeƟng approval if the trial was conducted in accordance with good clinical pracƟce and if the FDA is able to validate the data from the trial through an onsite inspecƟon if the Agency deems it necessary.11 When sponsors rely on foreign data, these should be supported with informaƟon about predominant HBV genotypes and subtypes in the region or regions (Schweitzer et al. 2015). Development programs should include a sufficient number of U.S. paƟents to ensure prevalent genotypes in the U.S. populaƟon are represented. FDA strongly encourages sponsors to provide a plan to address inclusion of clinically relevant subpopulaƟons with regard to age, sex, race, and ethnicity in the clinical trials to support an NDA or BLA, no later than the end-of-phase 2 meeƟng.12 11 See 21 CFR 312.120; 21 CFR 314.106. 12 See the guidance for industry CollecƟon of Race and Ethnicity Data in Clinical Trials (October 2016).
Contains Nonbinding RecommendaƟons 11 3. Safety ConsideraƟons In general, we recommend that iniƟal markeƟng applicaƟons for drugs intended to treat CHB contain a total safety database of about 1,000 to 1,500 subjects exposed to the proposed dose and duraƟon of treatment. Depending on the drug safety profile and concerns idenƟfied during the development process, a larger database or long duraƟons of posƩreatment follow-up may be needed. In addiƟon to rouƟne safety monitoring, the safety monitoring plans should consider the mechanism of acƟon of the drug, as there may be different safety concerns associated with specific drugs both during treatment and aŌer treatment cessaƟon. Some of the notable safety concerns associated with immune modulatory therapies are immune-mediated hepaƟƟs flares and autoimmunity (e.g., immune-related adverse events observed with checkpoint inhibitors). The specific criteria for defining and monitoring for hepaƟƟs flares during treatment and aŌer stopping therapy should be prespecified in the clinical trial protocols. The safety profile observed in early phase trials should guide the monitoring plan for late phase trials. Severe acute exacerbaƟons of HBV infecƟon may occur aŌer disconƟnuaƟon of anƟ-HBV therapy, parƟcularly in the absence of HBsAg loss. Subjects should be monitored closely with both laboratory and clinical follow-up aŌer disconƟnuaƟon of anƟ-HBV therapy. The duraƟon of follow-up should consider the mechanism of acƟon and the half-life of the specific invesƟgaƟonal drug. In certain circumstances, resumpƟon of anƟ-HBV therapy may be warranted. The detailed plan and criteria for treatment reiniƟaƟon should be prespecified in the clinical trial protocols. Clinical trial protocols should include predefined algorithms for data collecƟon in the seƫng of significant hepaƟc events to ensure that the relevant data are available for further assessment and adjudicaƟon of these cases to differenƟate between potenƟal eƟologies. The outcomes for all serious hepaƟc events should be systemaƟcally evaluated during clinical development. EvaluaƟon by an independent adjudicaƟon commiƩee is encouraged. For a drug approved for use in paƟents without cirrhosis or with compensated cirrhosis, the database needed to extend use to the decompensated cirrhoƟc populaƟon would depend on the safety profile of the invesƟgaƟonal drug and the overall benefit-risk profile for the indicated populaƟon. Similarly, obtaining safety data in other subpopulaƟons, such as in paƟents coinfected with hepaƟƟs D virus (HDV), may be important for certain clinical development programs. We encourage sponsors to discuss with the FDA safety-related consideraƟons, including but not limited to the size of the safety database, before the iniƟaƟon of phase 3 trials.
Contains Nonbinding RecommendaƟons 12 B. Phase 3 Efficacy Trial ConsideraƟons Sponsors can submit an NDA/BLA to support markeƟng approval of a drug in a single paƟent populaƟon (e.g., treatment-naïve paƟents or paƟents who are virally suppressed on NrtIs). Such an applicaƟon should include at least two adequate and well-controlled trials conducted in the proposed populaƟon. AlternaƟvely, sponsors can choose to pursue an indicaƟon for different populaƟons (e.g., a trial in treatment-naïve subjects and a second trial in subjects who are virally suppressed on NrtIs). In these situaƟons, the NDA/BLA should contain at least one adequate and well-controlled trial in each paƟent populaƟon, with adequate supporƟng data. 1. Trial Design Randomized controlled trials are recommended to establish efficacy because of the heterogeneity of the natural course of CHB. Appropriate trial designs depend on whether the therapeuƟc is intended for chronic suppressive therapy or therapy of finite duraƟon as discussed below. a. Chronic suppressive therapy Sponsors developing drugs for chronic suppressive therapy of CHB should consider the following trial design opƟons: A randomized controlled noninferiority (NI) (or superiority) trial comparing the invesƟgaƟonal drug with an approved acƟve control arm—The primary efficacy endpoint should be undetectable HBV DNA13 aŌer 48 weeks on-treatment in HBeAg-posiƟve subjects, HBeAg- negaƟve subjects, or both. The acƟve comparator should be an anƟviral drug that is recommended for treatment of CHB and reflects current pracƟce at the Ɵme of trial iniƟaƟon. The paƟent populaƟon may be treatment-naïve or previously treated subjects with detectable HBV DNA. PotenƟal concerns related to the development of resistance when evaluaƟng an invesƟgaƟonal drug with a low barrier to resistance as a monotherapy should be addressed. For an NI design, determinaƟon of the NI margin should be discussed with the FDA. 13 Defined as less than the lower limit of quanƟficaƟon (LLOQ), specifying if the results are target detected (TD) or target not detected (TND).
Contains Nonbinding RecommendaƟons 13 A randomized controlled add-on superiority trial comparing an invesƟgaƟonal drug plus an approved NrtI with an NrtI alone—However, for this trial design, it is not clear what the most appropriate primary endpoint should be to demonstrate the invesƟgaƟonal drug’s clinical contribuƟon. Presently, HBV DNA is not recommended as a primary endpoint for an add-on trial because it is unclear what incremental numerical benefits in HBV DNA, over the substanƟal HBV DNA suppression achieved by an NrtI alone, are predicƟve of clinical benefit. Other endpoints such as HBsAg clearance or another surrogate found to be predicƟve of clinical benefit may be considered; however, the trial design and endpoints should be discussed with the FDA in advance of trial iniƟaƟon. b. Finite duraƟon therapy The appropriate trial design depends on the paƟent populaƟon being studied and the treatment regimen being evaluated. See secƟon III. B. 7., Efficacy Endpoints for a descripƟon of efficacy endpoints that could be used for evaluaƟon of finite duraƟon therapies in clinical trials. Sponsors developing drugs for finite duraƟon therapy of CHB should consider the following trial design opƟons: Virally suppressed on NrtIs To evaluate the primary efficacy outcome of sustained HBV DNA suppression off-treatment with HBsAg loss in subjects with acƟve disease (HBeAg-posiƟve or HBeAg-negaƟve CHB) who are virally suppressed on NrtIs, sponsors can consider an add-on superiority trial against placebo with a current NrtI treatment regimen as the background therapy. The co-primary efficacy endpoints14 of HBsAg loss and sustained HBV DNA suppression should be assessed at the 6-month posƩreatment Ɵme point with addiƟonal follow-up to monitor for durability of response (i.e., sustained HBV DNA suppression and HBsAg loss) off- treatment. In general, off-treatment refers to disconƟnuaƟon of all therapies (i.e., invesƟgaƟonal agent and background NrtI regimen). To demonstrate sustained response off-treatment, sponsors should systemaƟcally assess the duraƟon of a treatment consolidaƟon period, defined as the duraƟon of conƟnued treatment needed aŌer achieving HBsAg loss, during late phase trials. This may vary based on the mechanism of acƟon and half-life of the specific invesƟgaƟonal drug. 14 See draŌ guidance for industry MulƟple Endpoints in Clinical Trials (January 2017). When final, this guidance will represent the FDA’s current thinking on this topic.
Contains Nonbinding RecommendaƟons 14 Sponsors should use the following criteria for stopping NrtI therapy at the end of the invesƟgaƟonal treatment period when evaluaƟng a finite duraƟon therapy: (1) applied equally across treatment arms, as applicable; (2) well-defined in the protocol; and (3) stringent, such as HBsAg loss or substanƟal HBsAg decline or marked reducƟon in other important biomarkers idenƟfied in phase 2 trials. It is expected that few subjects would meet such criteria on the placebo arm. The criteria for stopping NrtI therapy should be based on clinical evidence that also reflects current pracƟce guidelines recommended by the authoritaƟve scienƟfic bodies to ensure that the disconƟnuaƟon of NrtI therapy does not pose undue safety risk to the trial parƟcipants. Sponsors should discuss with the FDA the use of biomarkers as a trigger for treatment interrupƟon in advance of trial iniƟaƟon. AlternaƟvely, an outcome of sustained HBV DNA suppression off-treatment without HBsAg clearance can be evaluated aŌer a finite treatment duraƟon using a superiority trial design comparing the invesƟgaƟonal drug plus an NrtI with an NrtI alone. Treatment-naïve An outcome of sustained HBV DNA suppression off-treatment with HBsAg loss can be evaluated in treatment-naïve subjects by demonstraƟng superiority to an acƟve control, or, in paƟents in whom treatment is currently not indicated per treatment guidelines, superiority to placebo. In certain paƟent populaƟons (e.g., for paƟents in the immune-tolerant phase with mild necroinflammaƟon or fibrosis) comparison with placebo may be feasible as current treatment guidelines do not recommend treatment for these paƟents. In some of the trial design scenarios, subjects in the placebo group may be rolled over to an acƟve invesƟgaƟonal drug before the compleƟon of the trial based on a prespecified interim analysis. Sponsors should prospecƟvely plan these analyses15 and should discuss with the FDA before trial enrollment. Sponsors considering an NI trial design should discuss in advance with the FDA their trial designs and jusƟficaƟons of the proposed NI margin based on historical evidence of treatment effect of the acƟve control. In general, the acƟve comparator in an NI trial should be an FDA-approved drug that is considered the standard of care for the specific indicaƟon and populaƟon being studied. A detailed protocol and staƟsƟcal analysis plan (SAP) should be submiƩed for review. 15 See the guidance for industry AdapƟve Designs for Clinical Trials of Drugs and Biologics (November 2019).
Contains Nonbinding RecommendaƟons 15 2. Trial PopulaƟon PaƟents fulfilling one of the following two criteria for CHB should be enrolled (Centers for Disease Control and PrevenƟon 2012): (1) NegaƟve immunoglobulin M (IgM) anƟbodies to HBV core anƟgen and a posiƟve result on one of the following tests: HBsAg, HBeAg, or nucleic acid test for hepaƟƟs B virus DNA (including qualitaƟve, quanƟtaƟve, and genotype tesƟng); or (2) PosiƟve HBsAg result or posiƟve nucleic acid test for HBV DNA (including qualitaƟve, quanƟtaƟve, and genotype tesƟng) or posiƟve HBeAg on two occasions at least 6 months apart (any combinaƟon of these tests performed 6 months apart is acceptable). Sponsors should consider evaluaƟng drug efficacy in key CHB subpopulaƟons, including but not limited to the following: • HBeAg-posiƟve and HBeAg-negaƟve subjects • Subjects with cirrhosis • Subjects with decompensated liver disease 3. Entry Criteria The presence or absence of cirrhosis at study entry should be documented based on clinical assessment or previous liver biopsy, when available. As the criteria for diagnosing cirrhosis using noninvasive methods are not yet well defined, parƟcularly in paƟents who are virally suppressed, the use of a noninvasive modality to define presence or absence of cirrhosis in a trial protocol should be supported by references that summarize performance characterisƟcs and sensiƟvity and specificity of the modality for idenƟfying paƟents with cirrhosis.
Contains Nonbinding RecommendaƟons 16 4. RandomizaƟon, StraƟficaƟon, and Blinding Sponsors should conduct randomized, double-blind trials whenever feasible to reduce the likelihood of potenƟal biases. In general, trials should be designed to evaluate the effect of invesƟgaƟonal therapies in subjects with key disease characterisƟcs. PaƟent subpopulaƟons could be evaluated in separate trials or as separate strata in a single trial. If mulƟple paƟent populaƟons are included in a single trial, sponsors should consider straƟfying groups at randomizaƟon based on baseline variables (e.g., HBeAg status, HBsAg level, presence or absence of cirrhosis, and HBV DNA level) and ensure that an adequate number of subjects are in each stratum to provide informaƟve data. 5. Specific PopulaƟons a. PaƟents with HBV/HIV-1 coinfecƟon The overall treatment goals for paƟents with HBV/HIV coinfecƟon remain idenƟcal to those described for the HBV-monoinfected populaƟon. Sponsors should consider including subjects coinfected with HIV in the clinical trials evaluaƟng finite duraƟon HBV therapies. In cases where there is a strong raƟonale for exclusion of paƟents with HBV/HIV coinfecƟon, the raƟonale should be addressed in the trial protocol. The concurrent use of HIV anƟretroviral drugs that are also effecƟve against HBV (e.g., HIV nucleoside/nucleoƟde reverse transcriptase inhibitors) may have implicaƟons for treatment cessaƟon when evaluaƟng finite duraƟon HBV therapies and possibly confound interpretaƟon of efficacy outcome as subjects conƟnue their HIV nucleoside/nucleoƟde reverse transcriptase inhibitor -based anƟretroviral regimen. Because of the various interacƟons between HIV and HBV therapies, we recommend sponsors discuss their plans with and obtain feedback from the FDA. b. PaƟents with HBV/HDV coinfecƟon InfecƟon with HDV only occurs in the seƫng of concurrent HBV infecƟon (Wranke and Wedemeyer 2016). According to the World Health OrganizaƟon, an esƟmated 15 million to 20 million people worldwide are living with HBV/HDV coinfecƟon (World Health OrganizaƟon 2017). A meta-analysis reported a much higher worldwide HBV/HDV coinfecƟon prevalence of 62 million to 72 million (Chen et al. 2019). RelaƟve to HBV monoinfecƟon, HBV/HDV coinfecƟon leads to more severe liver disease resulƟng in a greater risk of cirrhosis, HCC, and hepaƟc decompensaƟon/failure. The ulƟmate goal of treatment in paƟents with HBV/HDV coinfecƟon is clearance or long-term suppression of both viruses. CHB treatment leading to loss of HBsAg may ulƟmately lead to the clearance of HDV infecƟon (Wranke and Wedemeyer 2016). HDV superinfecƟon frequently leads to spontaneous suppression of HBV (Huang and Lo 2014), and the effect of specific HBV therapies on the
Contains Nonbinding RecommendaƟons 17 interplay between the two viruses cannot be predicted. The possibility of HBV reacƟvaƟon needs to be considered when HDV is suppressed aŌer HDV treatment iniƟaƟon. To miƟgate the risk of HBV reacƟvaƟon and associated hepaƟƟs flares, it is preferred to have paƟents on NrtI suppressive therapy before they receive HDV treatment. RecommendaƟons for trials in paƟents with HBV/HDV coinfecƟon are beyond the scope of this guidance and are included in a separate draŌ guidance.16 Sponsors should discuss development plans directly with the FDA. c. Pediatric paƟents Pediatric assessments are required under secƟon 505B of the FD&C Act as part of the overall drug development program for a “new acƟve ingredient, new indicaƟon, new dosage form, new dosing regimen, or new route of administraƟon,” 17 unless those assessments are waived. 18 Sponsors should discuss their plans for pediatric assessments with the review division and be aware of Ɵming and content requirements for pediatric study plans under secƟon 505B(e) of the FD&C Act. Sponsors are required to submit pediatric study plans no later than 60 days aŌer an end-of-phase 2 meeƟng or such other Ɵme as may be agreed upon by the FDA and the sponsor. 19 Because progressive liver disease is uncommon in young children with HBV infecƟon, it is generally not recommended to include paƟents younger than 2 years of age in most development programs. Further, treatment generally is not recommended in children younger than 2 years of age, as per current treatment guidelines (Terrault et al. 2016). In general, pediatric clinical trials can be iniƟated aŌer phase 2 adult data characterizing the safety profile and preliminary evidence of efficacy are available. Given the natural history of CHB infecƟon, the dynamic relaƟonship between viral replicaƟon and the host immune response in pediatric paƟents may differ from that observed in adults, hence extrapolaƟon of efficacy may not be possible in all scenarios and could be considered on a case-by-case basis depending on the mechanism of acƟon of the invesƟgaƟonal drug or drugs and the pediatric age group being evaluated. 16 See the draŌ guidance for industry Chronic HepaƟƟs D Virus InfecƟon: Developing Drugs for Treatment (November 2019). When final, this guidance will represent the FDA’s current thinking on this topic. 17 See section 505B(a)(1)(A) of the FD&C Act; 21 U.S.C. 355c(a)(1)(A). 18 See section 505B(a)(5) of the FD&C Act. 19 See section 505B(e)(2)(A)(ii) of the FD&C Act; see also the guidance for industry Pediatric Study Plans: Content of and Process for Submitting Initial Pediatric Study Plans and Amended Initial Pediatric Study Plans (July 2020).
Contains Nonbinding RecommendaƟons 18 In cases in which extrapolaƟon of efficacy from adults to pediatrics is possible, aŌer criƟcal PK parameters of a drug are idenƟfied in adults, pediatric development programs can focus on idenƟfying dosing regimen(s) that achieve pediatric exposures similar to adults to demonstrate effecƟveness in pediatric populaƟons in which treatment is indicated as per current treatment guidelines. AddiƟonal clinical data should be obtained to assess whether anƟviral acƟvity is comparable to that observed in adult trials. Early discussion with the FDA on the appropriate endpoints and pediatric trial design is encouraged. In the absence of a serious safety signal in adults, sponsors should enroll adolescents20 in phase 3 adult trials or conduct a dedicated adolescent trial concurrently with the phase 3 adult trials. Confirmatory PK, safety, and efficacy data from this age group should be included as part of the data included at the Ɵme of filing of the original NDA/BLA.21 Typically, the nonadolescent pediatric populaƟon (for the purpose of this guidance, 2 to younger than 12 years of age) is divided into several groups or cohorts according to age or weight for enrollment into trials. Weight, rather than age, is the preferred criterion for enrollment because dosing recommendaƟons for most anƟviral drugs are weight-based. In addiƟon, within clinical studies, sponsors should enroll the cohorts in parallel rather than in series, unless a drug has a specific safety or drug disposiƟon factor that warrants a different approach. Dose selecƟon for pediatric treatment trials (e.g., phase 2 or 3) should be supported by PK data generated from the iniƟal PK/safety phase of the pediatric study and results of available modeling and simulaƟon. Sponsors should discuss the dose selecƟon with the FDA before iniƟaƟng the phase 2 or 3 pediatric trials. The pediatric trials should also obtain data to support safety in pediatric populaƟons. In general, a safety database of about 100 subjects receiving the proposed dose and treatment duraƟon is recommended. The parƟcipants should be adequately distributed across the pediatric age group for which studies are required. Long-term follow-up data should be collected from pediatric trials to assess long-term safety as well as durability of treatment response. If clinical trials in adults have demonstrated differences in safety profile or dosing based on fibrosis stage, pediatric subjects should be assessed for presence or absence of cirrhosis using the most appropriate modality for each study locaƟon. 20 For the purpose of this guidance, adolescents are defined as age 12 to younger than 18 years of age. 21 We note that, for applicaƟons to which secƟon 505B applies, all pediatric assessments must be submiƩed with the applicaƟon unless those assessments have been deferred (secƟon 505B(a)(1)(A)).
Contains Nonbinding RecommendaƟons 19 SecƟon 505B of the FD&C Act also mandates that the requisite pediatric assessments be conducted using a formulaƟon of the drug that is appropriate for each pediatric group being studied.22 Adult formulaƟons generally are considered appropriate for adolescent paƟents (Momper et al. 2013), but younger paƟents, who may not be able to swallow pills, may require different formulaƟons. Therefore, pediatric formulaƟon development should begin as early as possible to enable the development of appropriate pediatric formulaƟons of invesƟgaƟonal drugs. 6. Dose SelecƟon The results from proof-of-concept anƟviral acƟvity trials can be used to guide the selecƟon of doses to be evaluated in subsequent trials. Sponsors are encouraged to use various quanƟtaƟve clinical pharmacology approaches that leverage the totality of available informaƟon on exposure and pharmacodynamic assessments such as biomarkers that measure target engagement, HBsAg decline, HBV DNA decline, HBV RNA decline, and HBcrAg decline to select doses for phase 3 trials. 7. Efficacy Endpoints New finite duraƟon therapies could be evaluated in clinical trials using any of the following efficacy endpoints: • Sustained suppression (6 months or longer) of HBV DNA (less than LLOQ, TD, or TND) off- treatment aŌer a finite duraƟon of therapy • Sustained suppression (6 months or longer) of HBV DNA (less than LLOQ, TD, or TND) off- treatment with HBsAg loss (less than 0.05 internaƟonal unit/milliliter (IU/mL)) with or without HBsAb seroconversion aŌer a finite duraƟon of therapy At present, uƟlity of reducƟon in HBsAg from baseline (without complete clearance) for assessing response to CHB therapies is unclear because of inconsistent correlaƟons between qHBsAg and clinical response (Hu et al. 2018; Thompson et al. 2010; Chan et al. 2011). 22 See secƟon 505B(a)(2)A) of the FD&C Act.
Contains Nonbinding RecommendaƟons 20 A limited number of secondary endpoints (e.g., HBeAg loss, anƟ-HBe seroconversion in HBeAg posiƟve paƟents, ALT normalizaƟon) should be considered for tesƟng using appropriate staƟsƟcal methods for mulƟplicity. Biochemical serum markers such as ALT values vary between laboratories, and lack of normalizaƟon of ALT may oŌen be confounded by the presence of other chronic liver diseases such as nonalcoholic faƩy liver disease. Other important endpoints: Assessing progression of liver disease Except for paƟents with advanced or decompensated cirrhosis, a staƟsƟcally rigorous evaluaƟon of endpoints of liver progression can be challenging because these events occur infrequently unƟl late in the course of CHB. However, treatment effects on these endpoints provide useful clinical informaƟon, and trials evaluaƟng them could be used to support an expanded indicaƟon or paƟent populaƟon and could be summarized in appropriate secƟons of the label. Some of the parameters or clinical outcomes that sponsors can consider include the following: • Change in Model for End Stage Liver Disease scores • Change in Child-TurcoƩe-Pugh scores • Progression to liver failure requiring transplantaƟon or resulƟng in death • Occurrence of HCC Treatment-related regression of fibrosis or cirrhosis, as assessed by liver biopsy or noninvasive methods, may be appropriate for display in the label. However, sponsors should discuss with the Division plans for labeling and performance characterisƟcs of the noninvasive modality when protocols evaluaƟng these endpoints are being designed.
Contains Nonbinding RecommendaƟons 21 PaƟent-Reported Outcome Measures Sponsors who are considering incorporaƟng paƟent-reported outcome measures23 as endpoints in clinical trials to measure treatment benefit should discuss paƟent-reported outcome instruments with the Agency during the clinical development process. 8. Trial Procedures and Timing of Assessments Biochemical, serological, virological, and histological endpoints can be used to assess the effecƟveness of therapy. For drugs with finite treatment duraƟons, the opƟmal Ɵme point to assess the primary efficacy endpoint of sustained virologic response is 6 months or longer aŌer cessaƟon of therapy. AddiƟonally, the most appropriate Ɵme point to assess efficacy endpoints depends on the mechanism of acƟon and half-life of the drug. Longer term follow-up may be useful to confirm durability of treatment response and to measure clinical outcomes. 9. StaƟsƟcal ConsideraƟons In general, a detailed protocol and SAP staƟng the trial hypotheses, analysis methods, and all other relevant details should be provided to the Division of AnƟvirals before trial iniƟaƟon. To improve the precision of treatment effect esƟmaƟon and inference, sponsors should consider adjusƟng for prespecified baseline factors that are anƟcipated to be prognosƟc of the outcome (e.g., HBeAg status, HBV DNA level, and HBsAg level). If randomizaƟon is straƟfied by baseline covariates, the analysis should account for the straƟficaƟon factors. A discussion of how the analyses will account for the straƟfied randomizaƟon should be included in the protocol. For details see the draŌ guidance for industry AdjusƟng for Covariates in Randomized Clinical Trials for Drugs and Biological Products (May 2021).24 For staƟsƟcal analysis methods and issues, see the guidances for industry Providing Clinical Evidence of EffecƟveness for Human Drug and Biological Products (May 1998), Non-Inferiority Clinical Trials to Establish EffecƟveness (November 2016), and AdapƟve Designs for Clinical Trials of Drugs and Biologics and the FDA white paper StaƟsƟcal ConsideraƟons on Subgroup Analysis in Clinical Trials (Alosh et al. 2015). 23 See the guidance for industry PaƟent-Reported Outcome Measures: Use in Medical Product Development to Support Labeling Claims (December 2009). 24 When final, this guidance will represent the FDA’s current thinking on this topic.
Contains Nonbinding RecommendaƟons 22 a. Analysis populaƟons All subjects who are randomized and received at least one dose of assigned therapy during the trial should be included in the primary efficacy analysis for all fully blinded trials. For unblinded/parƟally blinded trials, all randomized subjects should be considered. Any possibility of randomized subjects who do not receive treatment in either or both arms should be minimized.
Contains Nonbinding RecommendaƟons 23 b. Efficacy analyses The primary analysis should compare the proporƟon of responders across trial treatment arms. This analysis determines whether effecƟveness has been demonstrated. For subgroup analyses, the analysis of the primary efficacy endpoint should be performed within important demographic and baseline characterisƟcs (e.g., geographic region, sex, race, age group, HBV genotype, HBeAg status, screening HBV DNA, baseline weight, body mass index, baseline ALT, baseline fibrosis/cirrhosis, and (if applicable) prior response to previous treatment regimens). The purpose of these analyses is to explore the consistency of the primary efficacy endpoint result across these subgroups. Treatment-by-region interacƟon should be invesƟgated and reported to assess consistency of the efficacy results. Treatment-by-HBeAg status interacƟon should also be invesƟgated if HBeAg-posiƟve and HBeAg- negaƟve subjects are enrolled in the trial. c. Handling missing data Sponsors should make every aƩempt to limit disconƟnuaƟon of subjects from the trial. When the loss is unavoidable, sponsors should explain the causes of missing data and aƩempt to determine the final status of a subject who does not complete the protocol. Analyses excluding subjects with missing data or other posƩreatment outcomes can be biased because subjects who do not complete the trial may differ substanƟally in both measured and unmeasured ways compared with subjects who remain in the trial. The primary method of handling missing data in the analysis should be prespecified in the protocol and SAP. SensiƟvity analyses should demonstrate that the primary analysis results are robust to the assumpƟons regarding missing data. 10. Accelerated Approval (Subpart H/I) ConsideraƟons For CHB, HBV DNA suppression with or without HBsAg loss is considered a validated surrogate endpoint that has been demonstrated to predict clinical outcomes, and this endpoint could be used to support a tradiƟonal approval. Sponsors should discuss with the FDA plans to use any other surrogate endpoints that are reasonably likely to predict clinical benefit to support accelerated approval. 25 Accelerated 25 See section 506(c) of the FD&C Act; 21 CFR part 314, subpart H; 21 CFR part 601, subpart E.
Contains Nonbinding RecommendaƟons 24 approval is subject to the requirement that postmarkeƟng confirmatory trials are conducted to verify and describe the anƟcipated effect on irreversible morbidity or mortality or other clinical benefit. 26 11. Benefit-Risk ConsideraƟons A thorough and comprehensive benefit-risk assessment ensures that the benefits outweigh potenƟal risks to the intended populaƟon. A benefit-risk assessment takes into consideraƟon the demonstrated therapeuƟc effect of the new drug and observed safety profile in the context of underlying disease and current treatment opƟons available for the indicaƟon. C. Other ConsideraƟons 1. Clinical Virology ConsideraƟons Samples for HBV quanƟficaƟon, genotypic, and phenotypic analysis should be obtained at different Ɵme points during treatment and follow-up. Timing of sample collecƟon should be based on iniƟal observaƟons of potency and on-treatment and off-treatment durability. The genotypes and phenotypes of baseline and virologic failure isolates should be determined (virologic failure defined as a confirmed increase of greater than or equal to 1 log 10 HBV DNA copies/mL above nadir, quanƟfiable HBV DNA of greater than or equal to 1 log10 copies/mL above LLOQ aŌer being less than LLOQ, or never achieved HBV DNA levels less than LLOQ for two consecuƟve visits). Transient increases in HBV DNA aŌer the compleƟon of treatment with a finite regimen may occur before sustained suppression. A strategy for disƟnguishing treatment failures from subjects experiencing a temporary increase should be agreed upon with the Division during protocol development. Clinical assessment during the development of acƟvators of the immune system is likely to be challenging, given that the greatest impact of these types of drugs will likely be a reducƟon in infected cells resulƟng in depleƟon of the cccDNA reservoir. Complete depleƟon of the cccDNA reservoir to below the limit of detecƟon may take a long Ɵme and will vary depending on the mechanism of acƟon of the drug. Currently, the only biomarker sufficient to predict a sustained response off-treatment is HBsAg loss, the assessment of which may be complicated by HBsAg expressed from integrated HBV DNA genome fragments. In addiƟon to host immune markers and serum HBV DNA, clinical trial protocols should assess several exploratory HBV endpoints (HBcrAg, HBV RNA, etc.) early in the development program in an aƩempt to idenƟfy potenƟal markers that correlate with the drug’s acƟvity and may predict response to therapy. 26 See 21 CFR 314.510; 21 CFR 601.41.
Contains Nonbinding RecommendaƟons 25 Genotypes of baseline and on-therapy virologic failure isolates should be compared and newly emerged drug resistance-associated subsƟtuƟons/mutaƟons should be idenƟfied. HBV DNA from subjects with genotypic resistance to the invesƟgaƟonal drug should be cloned in an HBV genome background and suscepƟbility to the invesƟgaƟonal drug should be determined. • There are 10 recognized HBV genotypes (genotypes A through J) as well as subtypes idenƟfied for genotypes A through F. The different HBV genotypes/subtypes encode disƟnct viral proteins and may exhibit differenƟal responses to an invesƟgaƟonal drug, which could confound efficacy results in clinical trials if the drug is only effecƟve against some genotypes/subtypes (Congly et al. 2013). Therefore, we recommend determining the genotypes/subtypes of HBV infecƟon present at baseline to determine if the invesƟgaƟonal drug exhibits anƟviral acƟvity against all HBV genotypes/subtypes. For subjects with suppressed HBV DNA at baseline, historical genotype assessments may be used if available. The assay, with performance characterisƟcs, used to genotype the HBV samples in enrolled subjects should be included with the clinical trial protocol. It may be important to confirm the genotype/subtype by phylogeneƟc analysis. • For resistance analyses, any changes, including mixtures, in the amino acid sequence of the target protein or DNA sequence for genome targeƟng drugs, present in on-treatment or follow- up samples but not in the baseline sample, can be reported as having developed during therapy. In addiƟon, baseline samples should be analyzed to idenƟfy HBV geneƟc polymorphisms that are associated with differenƟal anƟviral acƟvity against the invesƟgaƟonal drug. Sponsors should consult the FDA early for the most current format for submission of resistance data and if Next GeneraƟon Sequencing (NGS) will be used. • There is a risk of developing resistance against an anƟviral drug that targets similar viral proteins in different virus species in paƟents coinfected with HIV and HBV. Because of this risk, we recommend assessing for the development of resistance and cross-resistance in the viral proteins of both HIV-1 and HBV when appropriate. • For all virologic assessments in clinical trials, we recommend the use of FDA-approved or FDA- cleared assays, when available, and a central laboratory. Sponsors can collect results from local lab tests, idenƟfying the assays used. If invesƟgaƟonal assays are used, performance characterisƟcs of the assays determined from analyƟcal validaƟon studies using geographically and temporally disƟnct isolates should be provided in addiƟon to detailed descripƟons of the methodology. 27 Drugs that require assays to idenƟfy the infected populaƟon benefiƟng from 27 See the IDE (Investigational Device Exemption) web page, available at https://www.fda.gov/MedicalDevices/DeviceRegulationandGuidance/HowtoMarketYourDevice/InvestigationalDevi ceExemptionIDE/ucm046164.htm.
Contains Nonbinding RecommendaƟons 26 treatment (e.g., specific genotypes or resistant populaƟons) may require a companion diagnosƟc. AddiƟonal recommendaƟons can be found in the draŌ guidance for industry and Food and Drug AdministraƟon staff Principles for Codevelopment of an In Vitro Companion DiagnosƟc Device with a TherapeuƟc Product (July 2016). 28 • Sponsors are encouraged to submit a resistance monitoring plan early in development. If resistance evaluaƟon in clinical trials involves NGS, we recommend that sponsors discuss details of the NGS approach with the FDA. Submission of NGS data in FASTQ format is strongly encouraged. AddiƟonal recommendaƟons can be found in the guidance for industry technical specificaƟons document Submiƫng Next GeneraƟon Sequencing Data to the Division of AnƟviral Products (July 2019). • HBV should be genotyped for any instances where HBV DNA is detected in long-term follow-up to disƟnguish relapse from reinfecƟon. 28 When final, this guidance will represent the FDA’s current thinking on this topic.
Contains Nonbinding RecommendaƟons 27 2. PharmacokineƟc/Pharmacodynamic ConsideraƟons Trials conducted in HBV-infected subjects should include assessment of PK and the relaƟonship between drug exposure (e.g., minimum or maximum plasma concentraƟon (C min or C max ), area under the curve) and virologic success and toxicity in all subjects. Sponsors can use a combinaƟon of intensive and sparse sampling throughout development to characterize the PK of the invesƟgaƟonal drug. For example, sponsors should implement an intensive sampling schedule in early phase monotherapy trials. In longer term trials, an intensive sampling schedule might not be feasible. AlternaƟvely, sponsors can combine sparse sampling from these trials with intensive PK data from earlier trials for populaƟon PK analysis. Sponsors should obtain mulƟple sparse PK samples from as many subjects as possible, including at the Ɵme of key virologic assessments. It is important to document dosing Ɵmes and plasma sampling Ɵmes. Sponsors can use the following two broad approaches to characterize the relaƟonship between drug exposure and viral kineƟcs or virologic suppression of the invesƟgaƟonal drug, depending on the development stage and purpose of the analysis. Both approaches allow for exploraƟon of relevant covariates. (1) To aid the design of phase 2b or phase 3 trials, with respect to selecƟon of the dosage regimen, a mechanisƟc approach relaƟng drug concentraƟons and viral kineƟcs should be considered. A mechanisƟc modeling approach should also account for the development of resistance to the invesƟgaƟonal drug and the intended paƟent populaƟon. For combinaƟon therapy, the potenƟal of addiƟve or synergisƟc anƟviral effects can be incorporated in the model to assist opƟmizaƟon of the dose combinaƟon. (2) A simplified analysis relaƟng the proporƟon of subjects with virologic suppression or virologic failure and appropriate exposure variable (e.g., minimum concentraƟon or area under the plasma drug concentraƟon versus Ɵme curve) can be used to support evidence of acƟvity and to support dose selecƟon. Exposure-response safety analyses should consider the mechanisƟc on-target and off-target effects of the invesƟgaƟonal drug and adverse events that are more frequent in the invesƟgaƟonal drug arm. The appropriate exposure parameter and modeling approach depends on the invesƟgaƟonal drug and toxicity.
Contains Nonbinding RecommendaƟons 28 3. Labeling ConsideraƟons Severe acute exacerbaƟons of CHB may occur aŌer disconƟnuaƟon of anƟ-HBV therapy. HepaƟc funcƟon should be monitored closely with both clinical and laboratory follow-up for at least several months in subjects who disconƟnue anƟ-HBV therapy. In certain circumstances, resumpƟon of anƟ-HBV therapy may be warranted. These concerns should be adequately conveyed in drug labeling. Development of HIV-1 resistance against anƟ-HBV drugs with acƟvity against HIV-1 is a potenƟal risk that should be conveyed in labeling.
Contains Nonbinding RecommendaƟons 29 GLOSSARY OF ACRONYMS ALT alanine aminotransferase CC 50 concentraƟon inhibiƟng 50 percent cell growth cccDNA covalently closed circular DNA CHB chronic hepaƟƟs B EC 50/90 effecƟve drug concentraƟon inhibiƟng 50 or 90 percent virus replicaƟon FD&C Act Federal Food, Drug, and CosmeƟc Act HBeAg HBV e-anƟgen HBsAb anƟbody specific to HBsAg HBsAg HBV surface anƟgen HBV hepaƟƟs B virus HBV DNA hepaƟƟs B virus DNA HCC hepatocellular carcinoma HDV hepaƟƟs delta virus HIV human immunodeficiency virus IFN interferon IgM immunoglobulin M IU internaƟonal unit LLOQ lower limit of quanƟficaƟon mL NRTI milliliter HIV nucleoside/nucleoƟde reverse transcriptase inhibitor NrtI HBV nucleoside/nucleoƟde reverse transcriptase inhibitor NGS Next GeneraƟon Sequencing NI noninferiority PK pharmacokineƟc qHBsAg quanƟtaƟve HBsAg RNA ribonucleic acid rt reverse transcriptase SAP TD staƟsƟcal analysis plan target detected TND target not detected
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