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UDP-glucuronosyltransferase 1A4 (UGT1A4)
- Target
- UGT1A4
- Molecular classification
- Enzyme, Transferase, Phase II drug-metabolizing enzyme
01
Overview
UDP-glucuronosyltransferase 1A4 (UGT1A4) is an enzyme belonging to the UGT1A subfamily, involved in phase II metabolism in humans. It catalyzes glucuronidation, a conjugation reaction that attaches glucuronic acid to lipophilic drugs, steroids, hormones, and endogenous metabolites, thus making them water-soluble and facilitating their elimination from the body via urine or bile. UGT1A4 plays a key role in the detoxification and clearance of drugs such as the anticonvulsant lamotrigine, certain antipsychotics, tricyclic antidepressants, and endogenous steroids. The enzyme is known for significant inter-individual variability in expression, which can affect drug efficacy and toxicity. UGT1A4 is primarily expressed in the liver but also in other tissues, and its activity may be induced or inhibited by various drugs, leading to clinically relevant drug-drug interactions
- Other names
- UDP-glucuronosyltransferase 1-4UGT1A4UDPGT 1-4Bilirubin-specific UDPGT isozyme 2hUG-BR2UGT1*4UGT1-04UGT1.4UGT1-4UGT-1DUGT1DUGT-1AGNT1HUG-BR2
02
Mechanism of action
Catalyzes glucuronidation (adding glucuronic acid to substrate), increasing solubility and enabling excretion Involved in biotransformation and clearance of therapeutic drugs Reduces plasma concentration and pharmacologic activity of labile drugs
03
Biological functions
Glucuronidation of drugs and xenobioticsConjugation of endogenous compounds (e.g., steroids, bilirubin, hormones)Detoxification and elimination of lipophilic substancesRegulation of vitamin D metabolismEicosanoid biotransformation (e.g., arachidonic acid derivatives)
04
Disease associations
Variable drug metabolism and responseDrug toxicity (e.g., related to lamotrigine, clozapine, other amines and steroids)Pharmacogenetic variation impacting risk of adverse drug reactionsOther (mainly plays indirect roles in disease-modifying drug levels and toxicity)
05
Safety considerations
Inter-individual variability leading to differences in drug clearance and toxicityDrug-drug interactions (e.g., inhibitors or inducers of UGT1A4 affecting substrate metabolism)Risk of adverse drug reactions with drugs primarily metabolized by UGT1A4
06
Interacting drugs
Lamotrigine
7 more in the full profile.
07
Biomarkers
UGT1A4 expression/activity level as a biomarker for drug metabolism rate (especially lamotrigine)Genetic polymorphisms affecting drug response or toxicity risk
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