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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

ADME Optimization and Toxicity Assessment in Early- and Late-Phase Drug Discovery

Author(s): Gary W. Caldwell, Zhengyin Yan, Weimin Tang, Malini Dasgupta and Becki Hasting

Volume 9, Issue 11, 2009

Page: [965 - 980] Pages: 16

DOI: 10.2174/156802609789630929

Price: $65


Integrating physicochemical, drug metabolism, pharmacokinetics, ADME, and toxicity assays into drug discovery in order to reduce the attrition rates in clinical development is reviewed. The review is organized around three main decision points used in discovery including hit generation, lead optimization and final candidate selection stages. The preclinical strategies used at each decision point are discussed from a drug discovery perspective. Typically, preclinical data produced at these stages use lower throughput assays, smaller amounts of compounds and operate within a timeframe that is consistent with the iterative cycle of most drug discovery research projects. Understanding the false positive rates of these drug discovery preclinical assays is a must in reducing attrition rates in development.

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