CYP2C9

From PubPK

CYP2C9 ranks amongst the most important drug metabolizing enzymes in humans (Miners & Birkett 1998).

Contents 1 Function 2 Pharmacogenomics 3 Substrates 4 Inhibitors 5 Inducers 6 See also 7 References

Function

CYP2C9 is an important cytochrome P450 enzyme with a major role in the oxidation of both xenobiotic and endogenous compounds. CYP2C9 makes up about 18% of the cytochrome P450 protein in liver microsomes.

Pharmacogenomics

Polymorphisms in the coding region of the CYP2C9 gene produce variants at amino acid residues 144 (Arg144Cys) and 359 (Ile359Leu) of the CYP2C9 protein. Individuals homozygous for Leu359 have markedly diminished metabolic capacities for most CYP2C9 substrates, although the frequency of this allele is relatively low (Miners & Birkett 1998).

Substrates

• Glibenclamide
• Tolbutamid
• S-warfarin

Inhibitors

• Fluconazole
• Sulfaphenazole

Inducers

• Carbamazepine
• Rifampicin

See also

• Cytochrome P450s (CYPs)
• CYP2C8
• CYP2C19

References

• Miners JO, Birkett DJ (1998) Cytochrome P4502C9: an enzyme of major importance in human drug metabolism Br J Clin Pharmacol 45:525-38.