Target intelligence / Profile preview

Cytochrome P450 3A subfamily (CYP3A)

Target
CYP3A
Molecular classification
Enzyme, Monooxygenase, Member of the cytochrome P450 superfamily
01

Overview

Cytochrome P450 3A subfamily enzymes, collectively referred to as CYP3A, are the most abundant cytochrome P450 enzymes in humans, especially in liver and intestines. CYP3A enzymes (mainly CYP3A4, but also CYP3A5, CYP3A7, and CYP3A43) are responsible for metabolizing more than half of all clinically used drugs, as well as multiple endogenous substrates including steroid hormones, bile acids, cholesterol, and vitamin D. CYP3A-mediated metabolism can significantly affect drug efficacy and safety, leading to numerous clinically significant drug-drug interactions. Both genetic and environmental factors (including diet and co-administered medications) contribute to interindividual variability in CYP3A activity. Pharmacological modulation or dysfunction of CYP3A enzymes is implicated in disease risk, drug toxicity, and therapeutic outcome, especially when CYP3A inhibition or induction alters drug or hormone levels.

Other names
CYP3ACytochrome P450, family 3, subfamily ACytochrome P-450 3A subfamily
02

Mechanism of action

Drug metabolism via oxidation (increases drug polarity for excretion) Activation or inactivation of drugs and xenobiotics Many drug interactions occur due to enzyme inhibition or induction, influencing drug plasma levels and effects

03

Biological functions

Drug metabolismSynthesis and catabolism of cholesterol, steroid hormones, bile acids, vitamin D, and other lipidsDetoxification of endogenous and exogenous compounds
04

Disease associations

CancerCardiovascular diseaseHormonal disordersDrug-induced liver injuryInfection (through drug interactions with antimicrobials)
05

Safety considerations

Variable drug response due to genetic and physiological differencesSevere drug-drug interactions: inhibition can lead to increased toxicity (e.g., terfenadine-induced cardiac arrhythmia); induction can cause therapeutic failureGrapefruit juice and certain supplements (e.g., St. John’s wort) can cause clinically relevant changes in CYP3A activity
06

Interacting drugs

Midazolam, triazolam, diazepam (sedatives)

7 more in the full profile.

07

Biomarkers

CYP3A4 activity (measured via probe drugs such as midazolam)Genetic polymorphisms of CYP3A genes (especially CYP3A5 and CYP3A4)Expression levels in liver and intestine tissue

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