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Exposure-Response Relationships — Study Design, Data Analysis, and Regulatory Applications

FinalCenter for Drug Evaluation and Research Center for Biologics Evaluation and Research05/05/2003

Description

This document provides recommendations for sponsors of investigational new drugs (INDs) and applicants submitting new drug applications (NDAs) or biologics license applications (BLAs) on the use of exposure-response information in the development of drugs, including therapeutic biologics. It can be considered along with the International Conference on Harmonisation (ICH) E4 guidance on Dose-Response Information to Support Drug Registration and other pertinent guidances (see Appendix A).

Scope & Applicability

Product Classes

4
Therapeutic Biologics

Products for which this guidance provides clinical development assistance.

Biological drugs

A bracketing approach can be applied for stability testing; Drugs made by living organisms or cells.

Controlled-release dosage forms

suggest benefits of controlled-release dosage forms based on concentration-response

Stereoisomeric Drugs

drugs with one or more chiral centers

Stakeholders

5
Sponsor

Entity responsible for submitting applications under section 524B

Adults

reference population for pediatric study assumptions

Pediatrics

population for which PK/PD studies are conducted in the decision tree

Patient

Way questions are framed is critical to collecting unbiased patient input

Applicant

Entity submitting development data and knowledge; Entity performing the work process for change

Regulatory Context

Attributes

9
Cmax

Cmax may be more informative for safety

Therapeutic range

factor indicating drug sensitivity to ethnic factors

Extrinsic Factors

Diet, environmental factors, cultural or socioeconomic factors; Environmental or cultural factors affecting drug response; Factors known to affect the treatment response

Intrinsic Factors

genetic differences or different distribution of gene polymorphisms; Factors like genetics affecting drug response; Factors known to affect the treatment response

Protein binding

Renal or hepatic diseases can alter the binding of drugs to plasma proteins

Hysteresis

exposure-response relationship with considerable hysteresis

Steady state

Condition during chronic maternal dosing for milk sampling

AUC

AUC or Cmin may correlate with efficacy

Bioavailability

Biological property that may be altered by manufacturing changes; safety narrative should address bioavailability of the ingredients

Identified Hazards

Hazards

1
Dose-related toxicity

Unexpected and unrecognized risks associated with excessive dosing.

Related CFR Sections (2)

See Also (8)

Exposure-Response Relationships — Study Design, Data Analysis, and Regulatory Applications | Guideline Explorer | BioRegHub