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Curr Opin Drug Discov Devel. 2003 Jan;6(1):66-80.

Drug metabolism and pharmacokinetics in drug discovery.

Current opinion in drug discovery & development

Simon A Roberts

Affiliations

  1. Celltech Research and Development Ltd, Drug Metabolism and Pharmacokinetics, Granta Park, Great Abington, Cambridge, CB1 6GS, UK. [email protected]

PMID: 12613278

Abstract

The discovery and development of new drugs seems to be an inefficient process, since too few new chemical entities (NCEs) successfully make it to the market. Because one of the main reasons for failure in development is thought to be poor pharmacokinetics (PK), drug metabolism and PK (DMPK) have assumed a central role within the field of drug discovery. A good development candidate requires a balance of potency, safety and PK; therefore, techniques that can help understand these characteristics are employed to enable researchers to design more robust candidates. A number of new in silico, in vitro and in vivo techniques are available to screen compounds for key absorption, distribution, metabolism and excretion (ADME) characteristics, which, when applied within a rational strategy, can make a major contribution to the design and selection of successful NCEs.

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