%0 Journal Article
%T Lead Optimization in Discovery Drug Metabolism and Pharmacokinetics/Case study: The Hepatitis C Virus (HCV) Protease Inhibitor SCH 503034
%A K.-C. Cheng
%A Walter A. Korfmacher
%A Ronald E. White and F. George Njoroge
%J Perspectives in Medicinal Chemistry
%D 2012
%I 
%X : Lead optimization using drug metabolism and pharmacokinetics (DMPK) parameters has become one of the primary focuses of research organizations involved in drug discovery in the last decade. Using a combination of rapid in vivo and in vitro DMPK screening procedures on a large array of compounds during the lead optimization process has resulted in development of compounds that have acceptable DMPK properties. In this review, we present a general screening paradigm that is currently being used as part of drug discovery at Schering-Plough and we describe a case study using the Hepatitis C Virus (HCV) protease inhibitor program as an example. By using the DMPK optimization tools, a potent HCV protease inhibitor, SCH 503034, was selected for development as a candidate drug.
%U http://www.la-press.com/lead-optimization-in-discovery-drug-metabolism-and-pharmacokineticscas-article-a289