The Intravenous to Oral Switch of Taxanes: Strategies and Current Clinical Developments

Abstract

The taxanes paclitaxel, docetaxel and cabazitaxel are important anticancer agents that are widely used as intravenous treatment for several solid tumor types. Switching from intravenous to oral treatment can be more convenient for patients, improve cost–effectiveness and reduce the demands of chemotherapy treatment on hospital care. However, oral treatment with taxanes is challenging because of pharmaceutical and pharmacological factors that lead to low oral bioavailability. This review summarizes the current clinical developments in oral taxane treatment. Intravenous parent drugs, strategies in the oral switch, individual agents in clinical trials, challenges and further perspectives on treatment with oral taxanes are subsequently discussed.

Keywords:

• chemotherapy
• clinical trials
• drug delivery
• drug development
• oral administration
• solid tumors
• taxanes

Acknowledgments

The authors thank C Freund for his revision and advice on the intellectual content of this review.

Financial & competing interests disclosure

JH Beijnen is a part-time employee and shareholder of Modra Pharmaceuticals BV and is a patent holder of oral taxane formulations. Modra Pharmaceuticals BV is a spin-off company of the Netherlands Cancer Institute that is focused on the development of the oral taxanes ModraPac and ModraDoc in combination with ritonavir. E van der Putten is a part-time employee and director of Modra Pharmaceuticals BV. He is a partner at Aglaia Oncology Funds, which has investments in Modra Pharmaceuticals BV and Cristal Therapeutics (focused on the nanoparticle version of docetaxel CPC634). MAC Vermunt conducted clinical trials with ModraPac005 and ModraDoc006 in combination with ritonavir and is a first or co-author of (pending) publications related to these treatments. AM Bergman is the principle investigator of a Phase I trial with ModraDoc006 and ritonavir in castration-resistant prostate cancer and co-author of (pending) publications on ModraDoc006 with ritonavir. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.

Additional information

Funding

JH Beijnen is a part-time employee and shareholder of Modra Pharmaceuticals BV and is a patent holder of oral taxane formulations. Modra Pharmaceuticals BV is a spin-off company of the Netherlands Cancer Institute that is focused on the development of the oral taxanes ModraPac and ModraDoc in combination with ritonavir. E van der Putten is a part-time employee and director of Modra Pharmaceuticals BV. He is a partner at Aglaia Oncology Funds, which has investments in Modra Pharmaceuticals BV and Cristal Therapeutics (focused on the nanoparticle version of docetaxel CPC634). MAC Vermunt conducted clinical trials with ModraPac005 and ModraDoc006 in combination with ritonavir and is a first or co-author of (pending) publications related to these treatments. AM Bergman is the principle investigator of a Phase I trial with ModraDoc006 and ritonavir in castration-resistant prostate cancer and co-author of (pending) publications on ModraDoc006 with ritonavir. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.