Enhanced oral bioavailability of paclitaxel in mice treated with the P-glycoprotein blocker SDZ PSC 833

J van Asperen; O van Tellingen; A Sparreboom; A H Schinkel; P Borst; W J Nooijen; J H Beijnen

doi:10.1038/bjc.1997.530

Enhanced oral bioavailability of paclitaxel in mice treated with the P-glycoprotein blocker SDZ PSC 833

Br J Cancer. 1997;76(9):1181-3. doi: 10.1038/bjc.1997.530.

Authors

J van Asperen¹, O van Tellingen, A Sparreboom, A H Schinkel, P Borst, W J Nooijen, J H Beijnen

Affiliation

¹ Department of Clinical Chemistry, The Netherlands Cancer Institute, Amsterdam.

Abstract

Inhibition of intestinal P-glycoprotein might enhance the absorption of orally administered P-glycoprotein substrate drugs. We show here a 10-fold increased oral bioavailability of paclitaxel in mice treated with the P-glycoprotein blocker SDZ PSC 833. These results encourage further research on the development of a clinically useful oral formulation of paclitaxel.

MeSH terms

ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors*
Administration, Oral
Animals
Biological Availability
Cyclosporins / administration & dosage*
Drug Combinations
Female
Mice
Mice, Inbred Strains
Paclitaxel / administration & dosage
Paclitaxel / blood
Paclitaxel / pharmacokinetics*
Time Factors

Substances

ATP Binding Cassette Transporter, Subfamily B, Member 1
Cyclosporins
Drug Combinations
Paclitaxel
valspodar