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

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 l...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	British journal of cancer 2008-05, Vol.98 (10), p.1630-1632
Hauptverfasser:	Smith, N F, Baker, S D, Gonzalez, F J, Harris, J W, Figg, W D, Sparreboom, A
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Antineoplastic Agents - administration & dosage Antineoplastic Agents - blood Antineoplastic Agents - pharmacokinetics Beverages Bioavailability Biological and medical sciences Biological Availability Biomedical and Life Sciences Biomedicine Cancer Research Citrus paradisi Cytochrome Cytochrome P-450 CYP3A Inhibitors Drug Resistance Enzyme Inhibitors - pharmacology Epidemiology Erlotinib Hydrochloride Esters - pharmacology Female Kinases Medical research Medical sciences Metabolism Metabolites Mice Mice, Inbred BALB C Mice, Transgenic Molecular Medicine Oncology Oral administration Pharmacokinetics Plasma Protein Kinase Inhibitors - administration & dosage Protein Kinase Inhibitors - blood Protein Kinase Inhibitors - pharmacokinetics Quinazolines - administration & dosage Quinazolines - blood Quinazolines - pharmacokinetics Random Allocation Spiro Compounds - pharmacology Transgenic animals Translational Therapeutics Tumors
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	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.
ISSN:	0007-0920 1532-1827
DOI:	10.1038/sj.bjc.6604353