Modulation of erlotinib pharmacokinetics in mice by a novel cytochrome P450 3A4 inhibitor, BAS 100

N. F. Smith, S. D. Baker, F. J. Gonzalez, J. W. Harris, W. D. Figg, A. Sparreboom

Research output: Contribution to journalArticlepeer-review

26 Scopus citations

Abstract

Administration of BAS 100, a novel mechanism-based CYP3A4 inhibitor isolated from grapefruit juice, resulted in a 2.1-fold increase in erlotinib exposure following oral administration to wild-type and humanised CYP3A4 transgenic mice. This study illustrates the potential of BAS 100 to increase the low and variable oral bioavailability of erlotinib in cancer patients.

Original languageEnglish
Pages (from-to)1630-1632
Number of pages3
JournalBritish Journal of Cancer
Volume98
Issue number10
DOIs
StatePublished - 20 May 2008
Externally publishedYes

Keywords

  • CYP3A4 transgenic
  • Grapefruit
  • Metabolism
  • OSI-420
  • OSI-774
  • Tarceva

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