Cytochrome P450 2C8: substrates, inhibitors, pharmacogenetics, and clinical relevance

Clin Pharmacol Ther. 2005 May;77(5):341-52. doi: 10.1016/j.clpt.2004.12.267.


Cytochrome P450 (CYP) 2C8 [corrected] has been a relatively neglected member of the human CYP2C family. Over the period from 2000 through 2003, PubMed searches with the key word CYP2C8 returned only 10% to 15% of the citations obtained for all of the CYP2C enzymes combined. However, in the past year a crystal structure for CYP2C8 has been described, new inhibitors and probe substrates for the enzyme have been in development, the first case study was published linking CYP2C8 genetic polymorphisms to a disease state, and there has been an increasing awareness of the role that CYP2C8 plays in the disposition of therapeutic agents, especially from the pharmacogenetic and drug-drug interaction perspectives. This report discusses baseline characteristics of the enzyme and summarizes recent developments in these areas and their clinical relevance.

Publication types

  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Aryl Hydrocarbon Hydroxylases / antagonists & inhibitors*
  • Aryl Hydrocarbon Hydroxylases / genetics*
  • Aryl Hydrocarbon Hydroxylases / metabolism
  • Cytochrome P-450 CYP2C8
  • Humans
  • Pharmacogenetics
  • Polymorphism, Genetic / drug effects
  • Polymorphism, Genetic / genetics


  • Aryl Hydrocarbon Hydroxylases
  • CYP2C8 protein, human
  • Cytochrome P-450 CYP2C8