Cytochrome P450 family 2 subfamily C member 8 (CYP2C8)

Cytochrome P450 family 2 subfamily C member 8 (CYP2C8) is a member of the cytochrome P450 superfamily of enzymes, primarily functioning as a phase I monooxygenase involved in the metabolic biotransformation of a broad range of clinically important drugs and endogenous compounds. It is highly expressed in liver and also present in extrahepatic tissues such as kidney, adrenal gland, brain, ovary, and mammary gland. CYP2C8 plays a major role in the metabolism of xenobiotics, including anticancer agents (e.g., paclitaxel), antidiabetics (e.g., repaglinide, rosiglitazone), cardiovascular drugs, and more. It exhibits epoxygenase activity toward polyunsaturated fatty acids, generating signaling epoxides relevant to inflammation and vascular tone. Polymorphisms in the CYP2C8 gene significantly affect drug response and toxicity, making it both a prominent pharmacogenomic biomarker and a target for adverse drug interactions. Its activity can be modulated by inhibitors, inducers, and genetic variation, posing important safety considerations in clinical pharmacology[1][2][3][4][5][6][7][8][9][10].

Other names

CPC8CYPIIC8CYP2C8DMMP-12/MP-20

Substrate oxidation (monooxygenase activity: hydroxylation, epoxidation); Metabolism inhibition (by competitive or irreversible inhibitors, e.g. gemfibrozil acyl-β-glucuronide, myricetin); Induction or alteration of metabolic capacity via genetic polymorphisms and transcriptional regulation.