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Rolapitant: A Review in Chemotherapy-Induced Nausea and Vomiting

Abstract

Oral rolapitant (Varubi™; Varuby®), a long-acting neurokinin-1 (NK1) receptor antagonist (RA), is indicated in the USA and EU as part of an antiemetic regimen to prevent delayed chemotherapy-induced nausea and vomiting (CINV) in adults receiving highly or moderately emetogenic chemotherapy (HEC or MEC). In randomized, phase III trials, a single oral dose of rolapitant 180 mg was effective in preventing delayed CINV compared with placebo, when each was used in combination with a 5-HT3 RA plus dexamethasone, in adults receiving their first course of HEC or MEC. The benefits of rolapitant were maintained over multiple cycles of chemotherapy. The tolerability profile of rolapitant is similar to that of placebo and consistent with that of other NK1 RAs. However, rolapitant differs from other existing NK1 RAs in that it does not interact with CYP3A4, thereby negating the need for dexamethasone dose adjustments and potentially making rolapitant a more suitable option for patients receiving CYP3A4 substrates. Thus, oral rolapitant is an effective and well tolerated NK1 RA that expands the treatment options for preventing delayed CINV in adults receiving HEC or MEC.

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Acknowledgements

During the peer review process, the manufacturer of rolapitant was also offered an opportunity to review this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

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Correspondence to Young-A Heo.

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The preparation of this review was not supported by any external funding.

Conflict of interest

Young-A Heo and Emma Deeks are salaried employees of Adis/Springer, are responsible for the article content and declare no relevant conflicts of interest.

Additional information about this Adis Drug Review can be found at http://www.medengine.com/Redeem/5ED8F0606A685C8C.

Additional information

The manuscript was reviewed by: J. Kolesar, Department of Pharmacy Practice & Science, University of Kentucky, Lexington, KY, USA; M. Markman, Eastern Regional Medical Center, Cancer Treatment Centers of America, Philadelphia, PA, USA; R. M. Navari, Division of Hematology Oncology, University of Alabama Birmingham School of Medicine, Birmingham, AL, USA; I. N. Olver, Sansom Institute for Health Research, University of South Australia, Adelaide, Australia.

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Heo, YA., Deeks, E.D. Rolapitant: A Review in Chemotherapy-Induced Nausea and Vomiting. Drugs 77, 1687–1694 (2017). https://doi.org/10.1007/s40265-017-0816-z

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  • DOI: https://doi.org/10.1007/s40265-017-0816-z