Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes Academic Article uri icon

Overview

MeSH Major

  • Cytochrome P-450 Enzyme System
  • Protein Kinase Inhibitors
  • Quinazolines

abstract

  • Gefitinib is more susceptible to CYP3A-mediated metabolism than erlotinib, which may contribute to the higher apparent oral clearance observed for gefitinib. Metabolism by hepatic and extrahepatic CYP1A may represent a determinant of pharmacokinetic variability and response for both drugs. The differential metabolizing enzyme profiles suggest that there may be differences in drug-drug interaction potential and that stimulation of CYP3A4 may likely play a role in drug interactions for erlotinib and gefitinib.

publication date

  • June 15, 2007

Research

keywords

  • Academic Article

Identity

Language

  • eng

Digital Object Identifier (DOI)

  • 10.1158/1078-0432.CCR-07-0088

PubMed ID

  • 17575239

Additional Document Info

start page

  • 3731

end page

  • 7

volume

  • 13

number

  • 12