Editorial [Hot Topic: Perspectives of Pharmacokinetics and Metabolism in Drug Design (Executive Editor: Yunsheng Hsieh)]

Efficacy in preclinical models alone is insufficient for advancing compounds to drug development. This fact has led to the incorporation of drug metabolism and pharmacokinetics (DMPK) as one of the key components along with medicinal chemistry and biology during the lead optimization and characterization processes. Exploratory DMPK plays a key role in the drug discovery paradigm by assisting in selecting and designing therapeutic drug candidates with strong potency and favorable human pharmacokinetic properties. This special issue of Current Pharmaceutical Design focuses on the fundamentals and the applications of DMPK in early drug discovery research and acknowledges the efforts from contributors in making this issue possible. Tang W. and Lu AYH. [1] at the Department of Drug Metabolism & Pharmacokinetics, Merck Research Laboratories and the Department of Chemical Biology, Rutgers University, respectively, outline a brief overview on several DMPK strategies employed during the lead optimization processes. The authors describe several case studies and provide future directions of overcoming deficiencies in the current practice by developing tools enabling better prediction of clinical outcomes. Di L, Kerns EH and Carter GT. [2] from the Department of Chemical Technologies, Wyeth Research, introduce the concept of drug-like properties as an integrated part of the drug discovery process which is able to offer an early alert to potential issues, to guide structural modification, to prioritize chemical series and to diagnose in vivo PK and pharmacology.