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

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 humanized CYP3A4 transgenic mice. This study illustrates the potential of BAS 100 to increase the low and variable oral bioavailability of erlotinib in cancer patients.

• Authors: N F Smith, S D Baker, F J Gonzalez, J W Harris, W D Figg, A Sparreboom
• Journal: British journal of cancer (Br J Cancer) Vol. 98 Issue 10 Pg. 1630-2 (May 20 2008) ISSN: 1532-1827 [Electronic] England
• PMID: 18475295 (Publication Type: Journal Article, Research Support, N.I.H., Intramural)

Chemical References

• Antineoplastic Agents
• BAS 100
• Cytochrome P-450 CYP3A Inhibitors
• Enzyme Inhibitors
• Esters
• OSI-420
• Protein Kinase Inhibitors
• Quinazolines
• Spiro Compounds
• Erlotinib Hydrochloride

Topics

• Administration, Oral
• Animals
• Antineoplastic Agents (administration & dosage, blood, pharmacokinetics)
• Beverages
• Biological Availability
• Citrus paradisi
• Cytochrome P-450 CYP3A Inhibitors
• Enzyme Inhibitors (pharmacology)
• Erlotinib Hydrochloride
• Esters (pharmacology)
• Female
• Mice
• Mice, Inbred BALB C
• Mice, Transgenic
• Protein Kinase Inhibitors (administration & dosage, blood, pharmacokinetics)
• Quinazolines (administration & dosage, blood, pharmacokinetics)
• Random Allocation
• Spiro Compounds (pharmacology)