Pharmacogenomics of CYP3A: considerations for HIV treatment.

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Lakhman SS, Ma Q, Morse GD

Pharmacogenomics of CYP3A: considerations for HIV treatment.

Pharmacogenomics. 2009 Aug;10(8):1323-39. doi: 10.2217/pgs.09.53.

PubMed ID

19663676 [ View in PubMed

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Abstract

The understanding of the cytochrome P450 3A SNP in antiretroviral therapy is important, because it is highly inducible, extremely polymorphic and metabolizes many of the drugs that are key components of highly active antiretroviral therapy regimens. This enzyme is prolific and promiscuous towards drug and xenobiotic substrate selection and it is also unpredictable among individuals, having a 5- to 20-fold variability in its ability to contribute to drug clearance. The importance of human CYP3A pharmacogenetics is also gaining attention in other established areas of pharmacotherapy as it may contribute to the goal of predicting efficacy and/or toxicity, specifically with the discovery of null allele CYP3A4*20. This review summarizes the current understanding, implications of genetic variation in the CYP3A enzymes, the central role of CYP3A in linking human genetics, the pharmacokinetics and resulting pharmacodynamic responses to certain antiretroviral drugs, and their eventual place in applied clinical pharmacotherapy.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Efavirenz	Cytochrome P450 3A4	Protein	Humans	Unknown	Substrate Inhibitor Inducer	Details