CYP3A4 binds CYP3A4 inhibitors

Stable Identifier
R-HSA-9678766
Type
Reaction [binding]
Species
Homo sapiens
Compartment
cytosol, endoplasmic reticulum membrane
ReviewStatus
5/5
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CYP3A4 binds CYP3A4 inhibitors
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These compounds are inhibitors of cytochrome P450 3A enzymes (von Moltke et al. 1999, Yeo & Yeo 2001, Xu et al. 2010, Temesgen 2013, Greenblatt & Harmatz 2015). Cytochrome P450 3A4 (CYP3A4) is the most broadly active drug-metabolizing enzyme in humans. It oxidizes and clears over half of all administered pharmaceuticals due to its promiscuity. By inhibiting CYP3A4, these drugs can enhance bioavailability and prolong the plasma half-life of antiretroviral drugs such as those used to treat HIV infection.
Literature References
PubMed ID Title Journal Year
10445380 Nefazodone, meta-chlorophenylpiperazine, and their metabolites in vitro: cytochromes mediating transformation, and P450-3A4 inhibitory actions

Schmider, J, Greenblatt, DJ, Shader, RI, Harmatz, JS, Granda, BW, von Moltke, LL, Grassi, JM

Psychopharmacology (Berl.) 1999
24900196 Cobicistat (GS-9350): A Potent and Selective Inhibitor of Human CYP3A as a Novel Pharmacoenhancer

Strickley, RG, Hong, A, Desai, MC, Murray, BP, Liu, H, Tsai, LK, Rhodes, GR, Stray, KM, Xu, L, Wang, Y, Lee, MS, Callebaut, C

ACS Med Chem Lett 2010
11422004 Inhibitory effects of verapamil and diltiazem on simvastatin metabolism in human liver microsomes

Yeo, KR, Yeo, WW

Br J Clin Pharmacol 2001
25923589 Ritonavir is the best alternative to ketoconazole as an index inhibitor of cytochrome P450-3A in drug-drug interaction studies

Harmatz, JS, Greenblatt, DJ

Br J Clin Pharmacol 2015
23616950 Cobicistat, a pharmacoenhancer for HIV treatments

Temesgen, Z

Drugs Today 2013
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Authored
Jassal, B  (2020-03-23)
Reviewed
Huddart, R  (2022-03-01)
Created
Jassal, B  (2020-03-23)
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