The importance of metabolism in drug design

[摘要] It is widely recognized that pharmacokinetic optimization needs to be addressed early in drug discovery to reduce the high failure rate in bringing drugs to market. Poor absorption, too short duration of action due to high elimination rate, or the presence of active metabolites are examples of properties that can potentially lead to unsuccessful clinical programmes. Here I describe a brief overview of advantages and molecular strategies for improving metabolic and pharmacokinetic properties applied to the discovery of fluconazol, b-blockers, ritonavir and ezetimibe and to the development of the prodrugs enalapril and bambuterol.

[学科分类] 化学（综合）

[关键词] drug metabolism;drug design;structure-metabolism relationship.