Book Review of Enzyme Inhibition in Drug Discovery and Development. The Good and the Bad Enzyme Inhibition in Drug Discovery and Development. The Good and the Bad. Edited by Chuang Lu and Albert P. Li . John Wiley & Sons, Inc. , Hoboken, NJ . 2010 . xiii + 854 pp. 16 × 24 cm. ISBN 978-0-470-28174-1 . $175.00.

2010 ◽  
Vol 53 (11) ◽  
pp. 4560-4560
Author(s):  
John M. Rimoldi
Keyword(s):  
Drug Discovery ◽  
Enzyme Inhibition ◽  
Drug Discovery And Development

Cytochrome P450 enzymes: a review on drug metabolizing enzyme inhibition studies in drug discovery and development

Bioanalysis ◽  
2021 ◽  
Vol 13 (17) ◽  
pp. 1355-1378
Author(s):  
Siva Nageswara Rao Gajula ◽  
Megha Sajakumar Pillai ◽  
Gananadhamu Samanthula ◽  
Rajesh Sonti
Keyword(s):  
Cytochrome P450 ◽  
Drug Discovery ◽  
Enzyme Inhibition ◽  
In Vitro Study ◽  
Cytochrome P450 Enzymes ◽  
Drug Discovery And Development ◽  
Drug Candidates ◽  
Cyp Enzymes ◽  
Cyp Inhibition

Assessment of drug candidate's potential to inhibit cytochrome P450 (CYP) enzymes remains crucial in pharmaceutical drug discovery and development. Both direct and time-dependent inhibition of drug metabolizing CYP enzymes by the concomitant administered drug is the leading cause of drug–drug interactions (DDIs), resulting in the increased toxicity of the victim drug. In this context, pharmaceutical companies have grown increasingly diligent in limiting CYP inhibition liabilities of drug candidates in the early stages and examining risk assessments throughout the drug development process. This review discusses different strategies and decision-making processes for assessing the drug–drug interaction risks by enzyme inhibition and lays particular emphasis on in vitro study designs and interpretation of CYP inhibition data in a stage-appropriate context.

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