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Assessing the absorption of new pharmaceuticals
1Absorption Systems, LP, Exton, PA 19341, USA. hidalgo@absorption.com
Current Topics in Medicinal Chemistry
|March 20, 2002
Summary
Drug development requires assessing oral absorption early. This review covers various in vitro, in vivo, and computational methods to predict and optimize drug absorption, highlighting the need for combined approaches.
Area of Science:
- Pharmacology
- Drug Discovery
- Medicinal Chemistry
Background:
- Increasingly efficient synthesis and screening yield more chemical leads.
- Poor oral absorption is a major cause of drug development failure.
- Early assessment of absorption characteristics improves drug development success rates.
Purpose of the Study:
- To review and compare diverse techniques for evaluating drug absorption.
- To discuss the advantages and disadvantages of various absorption assessment models.
- To emphasize the importance of selecting drug candidates with adequate absorption.
Main Methods:
- Cell culture models of intestinal permeability (e.g., Caco-2, HT-29, MDCK).
- Physicochemical methods like immobilized artificial membrane (IAM) columns and parallel artificial membrane permeation assay (PAMPA).
- Computational methods for predicting drug absorption.
- In vitro and in vivo model systems.
Main Results:
- No single method is sufficient; a combination of techniques is necessary.
- High-throughput methods can identify 'loser' compounds early.
- Accurate methods are crucial for optimizing lead compounds and understanding absorption mechanisms.
Conclusions:
- A multi-method approach is essential for comprehensive drug absorption evaluation.
- Understanding absorption limitations (e.g., efflux, metabolism) aids medicinal chemists.
- Strategic selection of drug candidates based on absorption potential increases development success.
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