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Cytochrome P450 Enzymes: CYP19A1, CYP1A2, CYP1B1, CYP2C9, and CYP3A4 (CYP19A1, CYP1A2, CYP1B1, CYP2C9, CYP3A4)

Target
CYP19A1, CYP1A2, CYP1B1, CYP2C9, CYP3A4
Molecular classification
Enzyme, Cytochrome P450 monooxygenase, Oxidoreductase
01

Overview

These five enzymes—CYP19A1 (aromatase), CYP1A2, CYP1B1, CYP2C9, and CYP3A4—are cytochrome P450 monooxygenases that catalyze the oxidative metabolism of endogenous and exogenous compounds. They play pivotal roles in drug metabolism, hormone biosynthesis/breakdown, the generation or detoxification of carcinogens, and are directly implicated in clinically relevant pharmacogenetic variation and disease risk. CYP19A1 is especially critical for estrogen biosynthesis, CYP1A2 and CYP1B1 for carcinogen metabolism, CYP2C9 and CYP3A4 for the metabolism of numerous drugs, with CYP3A4 handling over half of all clinically used drugs. Genetic polymorphisms in these enzymes alter drug efficacy, safety, and disease susceptibility.

Other names
AromataseEstrogen synthetase
02

Mechanism of action

Enzyme inhibition (competitive/non-competitive, e.g., azoles, macrolides, aromatase inhibitors); Enzyme induction (notably by some antiepileptics, rifampin, St. John's wort)

03

Biological functions

Drug metabolismSteroid biosynthesisXenobiotic metabolismCarcinogen activationHormone regulation
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Disease associations

CancerCardiovascular diseaseEndocrine and metabolic disordersPharmacogenetic disorders/adverse drug reactions
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Safety considerations

Drug–drug interactionsAdverse drug reactions due to genetic polymorphismsVariability in hormone or drug exposurePotential for carcinogen bioactivation
06

Interacting drugs

Letrozole

15 more in the full profile.

07

Biomarkers

CYP genetic polymorphisms (CYP2C9, CYP2C19, CYP3A4 for drug metabolism phenotypes)CYP19A1 genotype variants for breast cancer risk, response to aromatase inhibitors

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