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

S. L.W. Koolen; J. H. Beijnen; J. H.M. Schellens

doi:10.1038/clpt.2009.233

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 journal › Short survey › Academic › peer-review

46 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 language	English
Pages (from-to)	126-129
Number of pages	4
Journal	Clinical Pharmacology and Therapeutics
Volume	87
Issue number	1
DOIs	https://doi.org/10.1038/clpt.2009.233
Publication status	Published - Jan 2010
Externally published	Yes

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AB - 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.

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

Abstract

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