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- Title
Intravenous-to-Oral Switch in Anticancer Chemotherapy: A Focus on Docetaxel and Paclitaxel.
- Authors
Koolen, S. L. W.; Beijnen, J. H.; Schellens, J. H. M.
- 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.
- Subjects
CANCER chemotherapy; CLINICAL medicine research; P-glycoprotein; CYTOCHROME P-450; DOCETAXEL; PACLITAXEL
- Publication
Clinical Pharmacology & Therapeutics, 2010, Vol 87, Issue 1, p126
- ISSN
0009-9236
- Publication type
Article
- DOI
10.1038/clpt.2009.233