Cytochrome P450 1A2; Cytochrome P450 2C11; Cytochrome P450 3A1 (CYP1A2; CYP2C11; CYP3A1)

Cytochrome P450 1A2, Cytochrome P450 2C11, and Cytochrome P450 3A1 are key members of the cytochrome P450 enzyme family involved in the metabolism of drugs, steroids, and toxins. CYP1A2 is primarily expressed in the liver and metabolizes substances such as caffeine, theophylline, and clozapine; CYP2C11 and CYP3A1 are major rat liver P450 isoforms with roles in drug (e.g., tegafur) biotransformation and are often used as preclinical models for human drug metabolism. Genetic and environmental factors modulate their activity, impacting therapeutic efficacy and drug safety. The enzymes also contribute to endogenous processes including steroid and fatty acid metabolism, and altered activity is linked to carcinogenesis, liver diseases, and inter-individual drug response variability.

Other names

Cytochrome P450 1A2 (CYP1A2)Cytochrome P450 2C11 (CYP2C11)Cytochrome P450 3A1 (CYP3A1)P450 1A2P450 2C11P450 3A1

Drugs act as substrates, inducers, or inhibitors of P450 enzymes—altering the metabolic rates and plasma levels of other drugs (phenotyping via probe drugs such as caffeine for CYP1A2). Prodrugs converted into active metabolites by P450 enzymes (e.g., conversion of tegafur to 5-fluorouracil).