Cytochrome P450 3A4, 2C9, 2D6, and 2B6 (CYP3A4, CYP2C9, CYP2D6, CYP2B6)

Cytochrome P450 3A4, 2C9, 2D6, and 2B6 are heme-containing enzymes encoded by their respective genes and predominantly located in the liver[1][2][5][8][10]. They oxidize a wide variety of exogenous substrates including pharmaceuticals and toxins, as well as some endogenous compounds. CYP3A4 and CYP2D6 in particular are responsible for the metabolism of the majority of prescription drugs, with CYP3A4 known for its broad substrate specificity and high potential for drug-drug interactions due to its ability to bind multiple compounds simultaneously[6][7]. Genetic variability in CYP2D6 and CYP2B6 explains significant differences in drug response and therapy outcomes between patients[5][8]. These enzymes represent major nodes for safety and efficacy concerns in drug development and precision medicine.

Other names

CYP3A4CYP2C9CYP2D6CYP2B6drug-metabolizing cytochromes P450

Substrate oxidation (drugs are metabolized, activated, or deactivated), competitive inhibition, enzyme induction or repression, allosteric/cooperative substrate binding.