Target intelligence / Profile preview

Cytochrome P450 3A (CYP3A)

Target
CYP3A
Molecular classification
Enzyme, Cytochrome P450, Monooxygenase
01

Overview

Cytochrome P450 3A (CYP3A) refers to a subfamily within the cytochrome P450 superfamily of enzymes. These are heme-thiolate monooxygenases that play a central role in the oxidative metabolism of both endogenous and exogenous compounds, including drugs, hormones, toxins, and carcinogens. The CYP3A subfamily is the most abundant group of CYP enzymes in human liver and intestine. CYP3A4 is the most prevalent and clinically significant isoform in adults. They are highly expressed in the liver and small intestine. CYP3A enzymes catalyze monooxygenation reactions using NADPH as an electron donor. Because they metabolize so many pharmaceuticals, drug-drug interactions involving inhibition or induction of CYP3As are common clinical concerns.

Other names
CYP3A subfamilyCytochrome P450 family 3 subfamily A
02

Mechanism of action

Oxidative metabolism of drugs and endogenous compounds, leading to their inactivation or activation.

03

Biological functions

Drug metabolismSteroid hormone metabolismBile acid metabolismFatty acid metabolismXenobiotic detoxificationArachidonic acid metabolism
04

Disease associations

CancerDrug toxicityHormone-related disorders
05

Safety considerations

Drug-drug interactions due to CYP3A inhibition or inductionInter-individual variability in CYP3A activity leading to altered drug responsePotential for increased toxicity of drugs metabolized by CYP3A if the enzyme is inhibitedPotential for decreased efficacy of drugs metabolized by CYP3A if the enzyme is induced
06

Interacting drugs

Acetaminophen

5 more in the full profile.

07

Biomarkers

CYP3A4 expression levelsCYP3A5 genotypeMetabolic ratios of CYP3A substrates

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