Intravenous-to-oral switch in anticancer chemotherapy: A focus on docetaxel and paclitaxel

S. L.W. Koolen, J. H. Beijnen, J. H.M. Schellens*

*Corresponding author for this work

Research output: Contribution to journalShort surveyAcademicpeer-review

43 Citations (Scopus)

Abstract

Oral administration of the taxanes docetaxel and paclitaxel is hampered by their affinity for drug transporters, especially ABCB1 (P-glycoprotein, Pgp); extensive first-pass metabolism by cytochrome P450 3A (CYP3A); and poor drug solubility. Preclinical studies in Pgp-deficient and wild-type mice demonstrated that modulation of either Pgp or CYP3A resulted in high systemic exposure to docetaxel or paclitaxel. This concept could successfully be translated to clinical trials.

Original languageEnglish
Pages (from-to)126-129
Number of pages4
JournalClinical Pharmacology and Therapeutics
Volume87
Issue number1
DOIs
Publication statusPublished - Jan 2010
Externally publishedYes

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