Minimizing the potential for metabolic activation as an integral part of drug design.
The formation of drug-protein adducts carries a risk of clinical toxicities that may not be predicted by preclinical safety studies. The process of minimizing the potential for metabolic activation at the lead optimization stage could therefore be viewed as a step for building quality into future generations of drug products.
Evans
David C
DC
Merck & Co Inc, Drug Metabolism, Rahway, NJ 07065, USA. david_c_evans@merck.com
Baillie
Thomas A
TA
D000818:Animals; D001711:Biotransformation / Q000502:physiology*; D015195:Drug Design; D064420:Drug-Related Side Effects and Adverse Reactions; D006801:Humans; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D013329:Structure-Activity Relationship
D004364:Pharmaceutical Preparations