Target intelligence / Profile preview

Cytochrome P450 3A4 (None)

Target
None
Molecular classification
Enzyme, Cytochrome P450, Monooxygenase
01

Overview

Cytochrome P450 3A4 (CYP3A4) is a key enzyme in the cytochrome P450 superfamily, responsible for metabolizing approximately 50-60% of all prescribed drugs and many endogenous compounds, including steroids and fatty acids. It is predominantly expressed in the liver and intestine. Due to its broad substrate specificity, CYP3A4 is a major contributor to drug-drug interactions, with many drugs acting as inhibitors or inducers of its activity. This can lead to altered plasma concentrations of co-administered medications, resulting in therapeutic failure or toxicity. It also has epoxide activity, converting arachidonic acid into epoxyeicosatrienoic acids (EETs) which have roles including cancer cell growth promotion.

Other names
CP33CP34CYP3ACYP3A3CYPIIIA3CYPIIIA4HLPNF-25P450C3P450PCN1VDDR3
02

Mechanism of action

CYP3A4 catalyzes monooxygenation reactions, primarily involved in the metabolism of a vast array of xenobiotics and endogenous compounds. It can be inhibited or induced by drugs, altering the metabolism of its substrates.

03

Biological functions

Drug metabolismSteroid synthesisFatty acid metabolismBile acid synthesisDetoxificationSteroid hormone inactivationEpoxygenase activity
04

Disease associations

CancerDrug toxicitySteroid hormone imbalance
05

Safety considerations

Drug-drug interactions due to inhibition or inductionTherapeutic failure due to accelerated drug metabolismDrug toxicity due to reduced drug metabolismPotential for bioactivation of pro-toxic compounds
06

Interacting drugs

Acetaminophen (paracetamol)

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