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The development of chiral drugs
1Servier Research & Development Limited, Fulmer, Slough, United Kingdom.
Acta Pharmaceutica Nordica
|January 1, 1990
Summary
Drug development is increasingly focusing on single enantiomers due to new synthesis methods. While stereochemistry impacts pharmacology and toxicology, its pharmacokinetic role varies, with exceptions like NSAIDs.
Area of Science:
- Medicinal Chemistry
- Drug Development
- Stereochemistry
Background:
- Historically, drug development overlooked stereochemistry's 3D effects due to synthesis and analytical challenges.
- Advancements in resolving racemic mixtures now drive demand for single-enantiomer drug synthesis.
Purpose of the Study:
- To highlight the growing importance of stereochemistry in drug development.
- To discuss the implications of synthesizing single enantiomers versus racemates.
- To examine the role of stereospecificity in drug pharmacology, toxicology, and pharmacokinetics.
Main Methods:
- Review of new techniques for resolving racemic mixtures.
- Analysis of stereospecificity in pharmacological and toxicological studies.
- Discussion of pharmacokinetic differences between enantiomers.
- Case study: dextro fenfluramine from rac-fenfluramine.
Main Results:
- New techniques facilitate the synthesis of single enantiomers.
- Stereospecificity is common in pharmacology and toxicology but less so in pharmacokinetics, with notable exceptions like Non-Steroidal Anti-Inflammatory Drugs (NSAIDs).
- Regulatory guidelines for stereoisomers are anticipated, increasing developmental studies on racemates.
Conclusions:
- The field of drug development must address the 3D consequences of stereochemistry.
- Single-enantiomer drugs offer potential advantages, though pharmacokinetic differences can be minor.
- Further research and regulatory clarity are needed for chiral drug development and registration.