Target intelligence / Profile preview

Cytochrome P450 2C8 and Cytochrome P450 3A4 (CYP2C8 and CYP3A4)

Target
CYP2C8 and CYP3A4
Molecular classification
Enzyme, Cytochrome P450, Oxidoreductase
01

Overview

Cytochrome P450 2C8 (CYP2C8) and Cytochrome P450 3A4 (CYP3A4) are members of the cytochrome P450 enzyme superfamily, responsible for the oxidative metabolism of a wide variety of endogenous and exogenous compounds, including many clinically important drugs[3][5]. CYP2C8 is a key hepatic phase I enzyme participating in the biotransformation of xenobiotics and polyunsaturated fatty acids, while CYP3A4 is one of the most abundant P450 enzymes in the liver and intestines, playing a central role in the metabolism of more than half of all marketed drugs[3][5][6]. Both enzymes are critical determinants of drug clearance, efficacy, and drug-drug interactions, and are clinically relevant therapeutic targets in the context of predicting metabolism, safety, and efficacy of substrate drugs[1][4].

Other names
CYP2C8Cytochrome P4502C8P450 2C8CYP3A4Cytochrome P4503A4P450 3A4
02

Mechanism of action

Metabolic clearance via oxidation (phase I metabolism); Conversion of drugs to metabolites with variable activity or toxicity

03

Biological functions

Xenobiotic metabolismDrug metabolismFatty acid metabolismBiotransformation
04

Disease associations

CancerCardiovascular diseaseDrug metabolism disordersOther
05

Safety considerations

Drug-drug interactions due to inhibition or induction of CYP2C8 or CYP3A4 (e.g., increased risk of toxicity or reduced efficacy)[7]Polymorphisms leading to altered metabolism ratesOverlapping substrate specificity causing unpredictable effects when multiple drugs are co-administered[4]
06

Interacting drugs

Repaglinide

14 more in the full profile.

07

Biomarkers

CYP2C8 and CYP3A4 activity as pharmacogenetic markers for drug dosing and drug-drug interaction risk assessment[5]

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