1. ¹Medical Oncology Branch, Center for Cancer Research, National Cancer Institute, 9000 Rockville Pike, Bethesda, MD 20892, USA
2. ²The Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, 1650 Orleans Street, Baltimore, MD 21231, USA
3. ³Laboratory of Metabolism, Centre for Cancer Research, National Cancer Institute, 9000 Rockville Pike, Bethesda, MD 20892, USA
4. ⁴Bioavailability Systems, LLC, 2210 S Atlantic Avenue, Cocoa Beach, FL 32931, USA

Correspondence: Dr WD Figg, Medical Oncology Branch, Center for Cancer Research, National Cancer Institute, Building 10, Room 5A01, 9000 Rockville Pike, Bethesda, MD 20892, USA. E-mail: wdfigg@helix.nih.gov

⁵Current address: Department of Pharmaceutical Sciences, St Jude Children's Research Hospital, Memphis, TN, USA

Revised 27 February 2008; Accepted 18 March 2008; Published online 6 May 2008.

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.