Enzyme Inhibition in Drug Discovery and Development: The Good and the Bad

The science and applied approaches of enzyme inhibition in drug discovery and development

Offering a unique approach that includes both the pharmacologic and pharmaco-kinetic aspects of enzyme inhibition, Enzyme Inhibition in Drug Discovery and Development examines the scientific concepts and experimental approaches related to enzyme inhibition as applied in drug discovery and drug development.

With chapters written by over fifty leading experts in their fields, Enzyme Inhibition in Drug Discovery and Development fosters a cross-fertilization of pharmacology, drug metabolism, pharmacokinetics, and toxicology by understanding the "good" inhibitions―desirable pharmacological effects―and "bad" inhibitions―drug–drug interactions and toxicity. The book discusses:

• The drug discovery process, including drug discovery strategy, medicinal chemistry, analytical chemistry, drug metabolism, pharmacokinetics, and safety biomarker assessment

• The manipulations of drug metabolizing enzymes and transporters as well as the negative consequences, such as drug–drug interactions

• The inhibition of several major drug target pathways, such as the GPCR pathway, the NFkB pathway, and the ion channel pathway

Through this focused, single-source reference on the fundamentals of drug discovery and development, researchers in drug metabolism and pharmacokinetics (DMPK) will learn and appreciate target biology in drug discovery; discovery biologists and medicinal chemists will also broaden their understanding of DMPK.

Chuang Lu, PhD, is the Associate Director in the Drug Safety and Disposition Department of Millennium Pharmaceuticals. His current research interests include drug-metabolizing enzymes, drug–drug interaction, and in vitro–in vivo correlation.

Albert P. Li, PhD, is the President and CEO of In Vitro ADMET Laboratories, LLC and Advanced Pharmaceutical Sciences, Inc., and the cofounder, Chairman, and CSO of the ADMET Group. His experience spans over twenty-five years in the drug development industry, with over 150 publications. He is the editor of several books, including Drug–Drug Interactions in Pharmaceutical Development, published by Wiley.