Transl Clin Pharmacol.  2014 Jun;22(1):3-7.

CYP3A5*3 Polymorphism and Its Clinical Implications and Pharmacokinetic Role

Affiliations
  • 1Department of Clinical Pharmacology and Toxicology, Anam Hospital, Korea University College of Medicine, Seoul 136-705, Korea. jypark21@korea.ac.kr

Abstract

The cytochrome P450 (CYP) 3A subfamily is estimated to participate in the biotransformation of 50% of the currently prescribed drugs. Four members of the CYP3A subfamily have been identified in humans: CYP3A4, CYP3A5, CYP3A7, and CYP3A43. Initial data suggested that CYP3A5 accounts for only a small proportion of the total hepatic CYP3A in about 20% of samples, but it was later revealed that CYP3A5 represents more than 50% of the total CYP3A amount in some individuals. Several genetic variants have been described for the CYP3A5 gene, of which the CYP3A5*3 allele (gA6986G), the most common form and leading to the loss of CYP3A5 activity, has been extensively investigated in the aspect of pharmacokinetics and disease risk. This review summarized the molecular characteristics of the CYP3A5 gene, and discusses the association of the CYP3A5*3 polymorphism with disease risks such as cancer and hypertension, along with its role in the pharmacokinetics of CYP3A substrates.

Keyword

CYP3A5*3; Cytochrome P450; Cancer; Pharmacokinetics; Pharmacogenetics

MeSH Terms

Alleles
Biotransformation
Cytochrome P-450 CYP3A
Cytochrome P-450 Enzyme System
Humans
Hypertension
Pharmacogenetics
Pharmacokinetics
Cytochrome P-450 CYP3A
Cytochrome P-450 Enzyme System

Reference

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