P‐glycoprotein and cytochrome P450 3A act together in restricting the oral bioavailability of paclitaxel

Paclitaxel is avidly transported by P‐glycoprotein (P‐gp/MDR1/ABCB1). This results in low oral bioavailability, which can be boosted by coadministration of P‐gp inhibitors. Unlike paclitaxel, docetaxel is extensively metabolized by CYP3A4 and its oral bioavailability can be enhanced in mice and huma...

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Veröffentlicht in:	International journal of cancer 2013-05, Vol.132 (10), p.2439-2447
Hauptverfasser:	Hendrikx, Jeroen J.M.A., Lagas, Jurjen S., Rosing, Hilde, Schellens, Jan H.M., Beijnen, Jos H., Schinkel, Alfred H.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Antineoplastic Agents, Phytogenic - administration & dosage Antineoplastic Agents, Phytogenic - blood Antineoplastic Agents, Phytogenic - pharmacokinetics Area Under Curve ATP Binding Cassette Transporter, Subfamily B ATP Binding Cassette Transporter, Subfamily B, Member 1 - antagonists & inhibitors ATP Binding Cassette Transporter, Subfamily B, Member 1 - deficiency ATP Binding Cassette Transporter, Subfamily B, Member 1 - genetics ATP Binding Cassette Transporter, Subfamily B, Member 1 - metabolism Bioavailability Biological and medical sciences Biological Availability Cancer Chemotherapy CYP3A4 Cytochrome P-450 CYP3A - metabolism Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Enzyme System - deficiency Cytochrome P-450 Enzyme System - genetics Cytochrome P-450 Enzyme System - metabolism Docetaxel Enzyme Inhibitors - administration & dosage Enzyme Inhibitors - pharmacology Enzyme Inhibitors - therapeutic use Glycoproteins Humans Infusions, Intravenous Intestinal Absorption Male Medical research Medical sciences Mice Mice, Knockout oral bioavailability paclitaxel Paclitaxel - administration & dosage Paclitaxel - blood Paclitaxel - pharmacokinetics P‐glycoprotein (P‐gp/MDR1) ritonavir Ritonavir - administration & dosage Ritonavir - pharmacology Ritonavir - therapeutic use Rodents Taxoids - administration & dosage Taxoids - blood Taxoids - pharmacokinetics Tumors
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