Target intelligence / Profile preview

Cytochrome P450 family 3 subfamily A enzyme system (CYP3A)

Target
CYP3A
Molecular classification
Enzyme, Monooxygenase, Cytochrome P450 superfamily
01

Overview

The **Cytochrome P450 family 3 subfamily A enzyme system** (CYP3A) is a major subfamily in the cytochrome P450 superfamily of monooxygenase enzymes, primarily localized to the liver and small intestine[1][2][4]. This family comprises multiple highly homologous isoenzymes—CYP3A4, CYP3A5, CYP3A7, and CYP3A43—that collectively account for the metabolism of approximately half of all marketed drugs[1][2][4]. These enzymes catalyze the oxidation (hydroxylation and epoxidation) of structurally diverse endogenous and exogenous compounds, promoting their detoxification and elimination from the body[2][3][6]. CYP3A enzymes also play critical roles in steroid hormone metabolism, bile acid homeostasis, and vitamin metabolism[2][6]. Substantial genetic and non-genetic variability in CYP3A activity impacts drug efficacy and safety, making the enzyme system essential for pharmacogenetics, personalized medicine, and drug-drug interaction risk assessment in therapeutic contexts[4].

Other names
Cytochrome P450 3ACYP3A4CYP3A5CYP3A7CYP3A43CYP3A enzyme system
02

Mechanism of action

Substrate metabolism (hydroxylation/oxidation of drugs and xenobiotics for elimination), Enzyme inhibition (drugs/compounds blocking enzyme activity increasing substrate drug levels), Enzyme induction (compounds increasing enzyme expression/activity reducing substrate drug levels)

03

Biological functions

Drug metabolismXenobiotic detoxificationSteroid hormone metabolismBile acid metabolismFatty acid metabolismVitamin metabolism
04

Disease associations

CancerInfectionOther (due to involvement in drug efficacy and toxicity, links to chemotherapy resistance, adverse drug reactions, liver disease)
05

Safety considerations

High interindividual variabilityDrug-drug interactions (due to inhibition/induction)Grapefruit juice interactionsAdverse effects from altered drug clearanceGenetic polymorphism leading to variable exposureImpact on chemotherapy drugs and immunosuppressants
06

Interacting drugs

Midazolam

13 more in the full profile.

07

Biomarkers

CYP3A4/5 genetic polymorphisms (e.g., CYP3A4*22, CYP3A5*3)Enzyme activity tests (midazolam clearance)Drug plasma levels (surrogates for CYP3A activity)Metabolite profiling

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