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Population Pharmacokinetics: Guidance for Industry

FinalCenter for Drug Evaluation and Research Center for Biologics Evaluation and Research02/03/2022
Model ValidationQuality Control

Description

This guidance is intended to assist sponsors and applicants of new drug applications (NDAs), biologics license applications (BLAs), abbreviated new drug applications (ANDAs), and investigational new drugs (IND) applications in the application of population pharmacokinetic (PK) analysis. Population PK analysis is frequently used to guide drug development and inform recommendations on therapeutic individualization (e.g., through tailored dosing) (Marshall et al. 2015; Lee et al. 2011; Bhattaram et al. 2005). Adequate population PK data collection and analyses submitted in marketing applications have in some cases alleviated the need for postmarketing requirements or postmarketing commitments.

Key Topics

Terms and concepts identified from this document

Scope & Applicability

Product Classes

4
Long-acting injectables

alternative for evaluating the bioequivalence of long-acting injectables

Generic Drug

Subject of GDUFA and related meeting processes.

Therapeutic Proteins

Proteins that reduce proinflammatory cytokines and affect CYP enzyme expression

Study drug

prior PK knowledge about the study drug

Stakeholders

1
Sponsor

Entity responsible for submitting applications under section 524B

Regulatory Context

Regulatory Activities

6
NDA

New Drug Application

New Drug Applications

Drug approval process under section 505 of the FD&C Act.

Regulatory review

facilitate the regulatory review of population PK models

BLA

Biologics License Application

ANDA

Abbreviated New Drug Application

IND

Investigational New Drug submissions

Document Types

8
Labeling

Cybersecurity information should be included in device labeling

Structured population PK report

Recommended format for accompanying population PK analysis results

electronic common technical document

promotional materials in module 1 of the electronic common technical document (eCTD); eCTD format for submissions; eCTD submission standards and operations; Format for electronic submissions.

Protocol

Defines the standard of veterinary practice and limits for anesthetic regimens

Data analysis plan

Document specifying analytic methods, sample size, and plans for resolving discrepancies

Population PK analysis report

preliminary examination of the data should be described in the report

Population PK Study Report

format and content for population PK reports submitted to the Agency

Population PK data analysis plan

Prespecified questions in the population PK data analysis plan

Attributes

6
Genetic Polymorphisms

intrinsic factor contributing to variability

Fixed-effect estimates

Typical estimates used to illustrate drug-concentration profiles

Between-subject variability

Parameter accounted for in simulations to show range of individual predictions

Parameter shrinkage

When parameter shrinkage is high, EBEs might be less reliable

Between-occasion variability

design should be sufficient to assess the presence and magnitude of effect

Body weight

relationship between body weight and drug exposure

Technical Details

Substances

3
Anti-drug antibodies

variations in the pharmacokinetics of a drug over time due to anti-drug antibodies

Creatinine

measurement of creatinine for renal function assessment

Proton pump inhibitors

Acid-reducing medications generally not permitted as concomitant use

Testing Methods

10
Population Pharmacokinetic Analysis

Pharmacokinetic Data Analysis method; standard analysis approach for nested DDI studies; Method typically used to evaluate nested DDI studies.

NONMEM

Software used for assessment of type I error rates and covariate effects

Bayesian Analysis

General concepts and software for population PK/PD models

Nonlinear Mixed-Effects Models

Used for diagnosing and modeling population pharmacokinetics

E-R analyses

Exposure-response analyses for safety and efficacy

Non-compartmental analysis

scenarios when non-compartmental analysis (NCA) becomes challenging

Stepwise covariate analysis

approaches for covariate analysis

Lasso

approaches for covariate analysis

Sensitivity analysis

Used to examine the influence of a QC algorithm assuming a worst-case scenario.

Visual Predictive Check

simulation-based diagnostics; Type of GOF plot used for model validation

Processes

7
Drug Absorption

effects of food on drug absorption

Metabolism

Impaired renal function can alter drug metabolism

Population PK analysis

Sponsors can combine sparse sampling with intensive PK data for population PK analysis.

ADME

Absorption, distribution, metabolism, and excretion properties evaluated for extrapolation.

Model development

Model development methods and best practice recommendations

Model validation

Determining suitability of a model by challenging it with independent test data.

Covariate analysis

covariate analysis can be performed based on several approaches

Clinical Concepts

10
Renal Impairment

Comorbidity affecting pharmacokinetics

Drug-Drug Interactions

Assessing uncontrolled drug-drug interactions in population PK analyses

CYP polymorphisms

GOF plots stratified by cytochrome (CYP) polymorphisms

Anti-drug antibodies

influence of anti-drug antibodies on drug exposure

Adverse events

Safety findings including deaths and post-mortem examinations

Liver Impairment

intrinsic factor affecting drug concentrations

Dosing regimens

inform dosing regimens for testing in clinical trials

Drug-drug interaction

Conducting drug-drug interaction evaluations early in drug development may inform selective dosing.

Pediatric patients

Guidance does not address the development of drugs for the prevention of PONV in pediatric patients.

Hepatic impairment

Condition assessed in clinical studies for PK/PD influence

Standards & References

Specifications

5
Cmax

Maximal concentration used as a PK parameter for BE

Area under the concentration time curve

Exposure metric used in forest plots to illustrate covariate effects

Tmax

PK measure mentioned in context of multiplicative models

Empirical Bayes Estimates

Individual patient exposure metrics are generated based on Empirical Bayes Estimates (EBEs)

Limit of quantification

data below the limit of quantification (LOQ)

Related MFDS Guidelines

Korean regulatory guidelines covering similar topics

See Also (8)