Target intelligence / Profile preview

Cytochrome P450 family 3 subfamily A member 4 (CYP3A4)

Target
CYP3A4
Molecular classification
Enzyme, Oxidoreductase
01

Overview

Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) is the most abundant phase I drug-metabolizing enzyme in the liver and intestine and is responsible for the metabolism of roughly 30-50% of clinically used drugs as well as numerous endogenous substrates, including steroid hormones and bile acids. It functions as a monooxygenase, catalyzing a wide range of oxidative reactions such as hydroxylation, dealkylation, and epoxidation, thereby facilitating detoxification, activation, or elimination of drugs and xenobiotics. CYP3A4 activity can be induced or inhibited by various substances, causing significant drug interactions, toxicity, or altered therapeutic efficacy. Genetic polymorphisms, environmental exposure (diet, drugs), and disease states all contribute to inter-individual variability in CYP3A4 expression and function, making it a critical factor in drug safety and personalized medicine.

Other names
Cytochrome P-450 CYP3ACytochrome P450 3A4CYP3A4Albendazole monooxygenaseNifedipine oxidaseQuinine 3-monooxygenaseTaurochenodeoxycholate 6-α-hydroxylaseAlbendazole sulfoxidaseCytochrome P450, subfamily IIIA (nifedipine oxidase), polypeptide 4
02

Mechanism of action

Substrate oxidation (mainly via monooxygenation, hydroxylation, dealkylation, epoxidation, etc.); Inactivation (deactivation) of drugs through oxidative metabolism; Bioactivation of prodrugs and protoxins into active or toxic metabolites.

03

Biological functions

Drug metabolismXenobiotic detoxificationSteroid metabolismBiosynthesis of cholesterol, steroids, and other lipidsMetabolism of carcinogensEpoxygenase activity (e.g., production of epoxyeicosatrienoic acids)
04

Disease associations

Cancer (roles in promoting cancer cell growth via EETs, affecting drug response)Other (adverse drug reactions, pharmacogenetic disorders)
05

Safety considerations

Drug-drug interactions (many drugs inhibit or induce CYP3A4 activity)Variable patient response due to genetic and environmental factorsDrug toxicity (CYP3A4 may activate protoxins or increase toxic metabolite levels)Impact of food components (e.g., grapefruit juice inhibits CYP3A4)
06

Interacting drugs

Acetaminophen (paracetamol)

10 more in the full profile.

07

Biomarkers

CYP3A4 enzyme activity (phenotyping with drug probes like midazolam)CYP3A4 genetic polymorphisms (pharmacogenetic testing)

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