Target intelligence / Profile preview

Etoposide metabolism

Molecular classification
Enzyme, Other
01

Overview

Etoposide metabolism is the enzymatic biotransformation of the chemotherapy drug etoposide, which primarily targets DNA topoisomerase II (StatPearls, 2023). The process is}

Other names
Etoposide biotransformationEtoposide metabolic pathwayBiotransformation of etoposide
02

Mechanism of action

Etoposide metabolism involves the CYP3A4/5-mediated O-demethylation of the parent drug to a catechol metabolite, which can be bioactivated to a reactive quinone by peroxidases or detoxified via UGT1A1-mediated glucuronidation (PubMed, PMID: 12130547, 15616150).

03

Biological functions

Drug metabolismXenobiotic biotransformationDetoxificationBioactivation
04

Disease associations

CancerSecondary acute myeloid leukemia
05

Safety considerations

Secondary leukemogenesis (via quinone metabolites)Severe myelosuppressionDrug-drug interactions with CYP3A4 modulatorsIncreased toxicity in UGT1A1-deficient patients
06

Interacting drugs

Etoposide

6 more in the full profile.

07

Biomarkers

CYP3A4 activityCYP3A5*3 polymorphismUGT1A1*28 allele status

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