Cytochrome P450 2C8: Substrates, Inhibitors, Pharmacogenetics, and Clinical Relevance

Cytochrome P450 (CYP) 2C9 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. Clinical Pharmacology & Therapeutics (2005) 77, 341–352; doi: 10.1016/j.clpt.2004.12.267