Publications
Oral taxanes, oral docetaxel, oral paclitaxel ...
Oral taxanes
The intravenous to oral switch of taxanes
The intravenous to oral switch of taxanes: strategies and current clinical developments. Vermunt MAC , Bergman AM , Van der Putten, Beijnen JH. Future Oncology. Published Online:24 Dec 2020 https://doi.org/10.2217/fon-2020-0876
Modulation of oral bioavailability of anticancer drugs
Modulation of oral bioavailability of anticancer drugs: from mouse to man. Schellens JH, Malingré MM, Kruijtzer CM, Bardelmeijer HA, van Tellingen O, Schinkel AH, Beijnen JH. Eur J Pharm Sci. 2000 Dec;12(2):103-10. Review. PMID: 11102737
Oral docetaxel
Phase I study with once weekly oral docetaxel - solid tumors
De Weger VA et al.: A Phase I Dose Escalation Study of Once-Weekly Oral Administration of Docetaxel as ModraDoc001 Capsule or ModraDoc006 Tablet in Combination with Ritonavir. Clin Cancer Res. 2019;25:5466–74.
Phase I study with bi-daily once weekly oral docetaxel - solid tumors
De Weger VA et al.: A dose-escalation study of bi-daily once weekly oral docetaxel either as ModraDoc001 or ModraDoc006 combined with ritonavir. Eur J Cancer. 2017 Nov;86:217-225.
Ritonavir inhibits intratumoral docetaxel metabolism
Ritonavir inhibits intratumoral docetaxel metabolism and enhances docetaxel antitumor activity in an immunocompetent mouse breast cancer model. Hendrikx JJ, Lagas JS, Song JY, Rosing H, Schellens JH, Beijnen JH, Rottenberg S, Schinkel AH. Int J Cancer. 2016 Feb 1;138(3):758-69. doi: 10.1002/ijc.29812. Epub 2015 Sep 21. PMID: 26297509
Pharmacokinetics and toxicities of oral docetaxel
Vermunt M, Marchetti S, Beijnen J. Pharmacokinetics and Toxicities of Oral Docetaxel Formulations Co-Administered with Ritonavir in Phase I Trials. Clin Pharmacol. 2021;13:21-32
Ritonavir enhances the oral bioavailability of docetaxel
Coadministration of ritonavir strongly enhances the apparent oral bioavailability of docetaxel in patients with solid tumors. Oostendorp RL, Huitema A, Rosing H, Jansen RS, Ter Heine R, Keessen M, Beijnen JH, Schellens JH. Clin Cancer Res. 2009 Jun 15;15(12):4228-33. doi: 10.1158/1078-0432.CCR-08-2944. Epub 2009 Jun 9. PMID: 19509162
Ritonavir boosts systemic exposure of oral docetaxel
Low systemic exposure of oral docetaxel in mice resulting from extensive first-pass metabolism is boosted by ritonavir. Bardelmeijer HA, Ouwehand M, Buckle T, Huisman MT, Schellens JH, Beijnen JH, van Tellingen O. Cancer Res. 2002 Nov 1;62(21):6158-64.PMID: 12414642
Phase I study with bi-daily once weekly oral docetaxel - prostate cancer.
Vermunt MAC, Robbrecht DGJ, Devriese LA et al.: ModraDoc006, an oral docetaxel formulation in combination with ritonavir (ModraDoc006/r), in metastatic castration‐resistant prostate cancer patients: A phase Ib study. Cancer Rep March 2021, PMID: 33709626
Oral paclitaxel
Phase I study with oral paclitaxel - solid tumors
De Weger VA et al.: A Phase 1 Dose-Escalation Study of Low-Dose Metronomic Treatment With Novel Oral Paclitaxel Formulations in Combination With Ritonavir in Patients With Advanced Solid Tumors. Clin Pharmacol Drug Dev. 2020 Oct 5. doi: 10.1002/cpdd.880. Online ahead of print.