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Cytochrome P450 2C9 (abbreviated CYP2C9), a member of the cytochrome P450 mixed-function oxidase system, is involved in the metabolism of xenobiotics in the body. It is involved in the metabolism of several important groups of drugs including many non-steroidal anti-inflammatory drugs (NSAIDs) and sulfonylureas.
Genetic polymorphism exists for CYP2C9 expression because the CYP2C9 gene is highly polymorphic. At least 30 CYP2C9 alleles have been identified to date. Among them, CYP2C9*3, with an Ile359Leu mutation, has been most widely studied. In vitro studies show it has significantly impaired catalytic activity to various CYP2C9 substrates relative to the wild type. In vivo investigations show that individuals heterozygous and homozygous for CYP2C9*3 have reduced intrinsic clearance of warfarin, phenytoin, lornoxicam and glipizide and are more at risk of clinical toxicity from these drugs. So, approximately 1–3% of Caucasian populations with homozygous CYP2C9*3 are poor metabolisers with no CYP2C9 function.
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CYP2C9 Ligands
| Substrates | Inhibitors | Inducers |
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Often mentioned [2]:
Other: |
Strong [3]:
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Often mentioned [2]:
Other:
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See also
References
- ^ Where classes of agents are listed, there may be exceptions within the class
- ^ a b Mentioned both in the reference named FASS and were previously mentioned in Wikipedia. Further contributions may follow other systems
- ^ Swedish environmental classification of pharmaceuticals Facts for prescribers (Fakta för förskrivare)
Further reading
- Goldstein JA, de Morais SM (1995). "Biochemistry and molecular biology of the human CYP2C subfamily.". Pharmacogenetics 4 (6): 285–99. PMID 7704034.
- Miners JO, Birkett DJ (1998). "Cytochrome P4502C9: an enzyme of major importance in human drug metabolism.". British journal of clinical pharmacology 45 (6): 525–38. PMID 9663807.
- Smith G, Stubbins MJ, Harries LW, Wolf CR (1999). "Molecular genetics of the human cytochrome P450 monooxygenase superfamily.". Xenobiotica 28 (12): 1129–65. PMID 9890157.
- Henderson RF (2001). "Species differences in the metabolism of olefins: implications for risk assessment.". Chem. Biol. Interact. 135-136: 53–64. PMID 11397381.
- Xie HG, Prasad HC, Kim RB, Stein CM (2003). "CYP2C9 allelic variants: ethnic distribution and functional significance.". Adv. Drug Deliv. Rev. 54 (10): 1257–70. PMID 12406644.
- Palkimas MP, Skinner HM, Gandhi PJ, Gardner AJ (2004). "Polymorphism induced sensitivity to warfarin: a review of the literature.". J. Thromb. Thrombolysis 15 (3): 205–12. doi:. PMID 14739630.
- Daly AK, Aithal GP (2004). "Genetic regulation of warfarin metabolism and response.". Seminars in vascular medicine 3 (3): 231–8. doi:. PMID 15199455.
- García-Martín E, Martínez C, Ladero JM, Agúndez JA (2007). "Interethnic and intraethnic variability of CYP2C8 and CYP2C9 polymorphisms in healthy individuals.". Molecular diagnosis & therapy 10 (1): 29–40. PMID 16646575.
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- This page was last modified on 8 July 2008, at 02:15.
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