Target intelligence / Profile preview

Cytochrome P450 and UDP-glucuronosyltransferase Metabolic Enzyme Panel (CYP/UGT Panel)

Target
CYP/UGT Panel
Molecular classification
Enzyme, Cytochrome P450, UDP-glucuronosyltransferase, Oxidoreductase, Transferase
01

Overview

The Cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes listed—specifically CYP2B6, CYP3A4/5, CYP2C9, CYP2C19, UGT1A1, UGT1A9, and UGT2B7—constitute the core machinery for Phase I and Phase II drug metabolism in the human liver and gastrointestinal tract [1]. CYP enzymes are heme-thiolate proteins that catalyze oxidative, peroxidative, and reductive reactions, while UGT enzymes are glycosyltransferases that catalyze the transfer of glucuronic acid to various functional groups, increasing the water solubility of drugs for renal or biliary excretion [2, 5]. These enzymes are critical in determining the pharmacokinetic profile of over 70% of clinically used drugs [4]. Because their activity is highly susceptible to genetic variation and modulation by other drugs through induction or inhibition, they are the primary focus of regulatory drug-drug interaction (DDI) studies [1, 3]. Variations in these enzymes can lead to profound differences in drug efficacy and safety, making them central to the field of pharmacogenomics and personalized medicine [3].

Other names
Phase I and Phase II drug-metabolizing enzymesADME enzyme panelCytochrome P450 and UDP-glucuronosyltransferase panelCYP2B6CYP3A4CYP3A5CYP2C9CYP2C19UGT1A1UGT1A9UGT2B7
02

Mechanism of action

These enzymes facilitate the biotransformation of drugs through Phase I oxidation (Cytochrome P450s) and Phase II glucuronidation (UDP-glucuronosyltransferases) to convert lipophilic compounds into hydrophilic metabolites for excretion [1, 4, 5].

03

Biological functions

Xenobiotic metabolismDrug detoxificationSteroid hormone metabolismBilirubin clearanceFatty acid oxidation
04

Disease associations

Adverse drug reactionsDrug-induced liver injuryGilbert syndrome (UGT1A1)Crigler-Najjar syndrome (UGT1A1)Pharmacogenetic variability
05

Safety considerations

Drug-drug interactions (DDIs) leading to toxicityTherapeutic failure due to rapid metabolismGenetic polymorphisms causing variable drug exposureMetabolite-mediated toxicity
06

Interacting drugs

Warfarin

7 more in the full profile.

07

Biomarkers

CYP2C19*2, *3, *17 (Clopidogrel response)CYP2C9*2, *3 (Warfarin sensitivity)UGT1A1*28 (Irinotecan toxicity risk)CYP2B6*6 (Efavirenz exposure)

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