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Review
. 2017 Feb 22:9:41-50.
doi: 10.2147/CMAR.S97543. eCollection 2017.

Differential pharmacology and clinical utility of rolapitant in chemotherapy-induced nausea and vomiting

Bernardo Leon Rapoport  1
Affiliations
Review

Differential pharmacology and clinical utility of rolapitant in chemotherapy-induced nausea and vomiting

Bernardo Leon Rapoport. Cancer Manag Res. .

Abstract

Chemotherapy-induced nausea and vomiting (CINV) is a debilitating side effect of many cytotoxic chemotherapy regimens. CINV typically manifests during two well-defined time periods (acute and delayed phases). The acute phase is the first 24 hours after chemotherapy and is largely managed with 5-hydroxytryptamine 3 receptor antagonists. The delayed phase, a 5-day at-risk period during which patients are not often in direct contact with their health care provider, remains a significant unmet medical need. Neurokinin-1 (NK-1) receptor antagonists have demonstrated protection against acute and delayed CINV in patients treated with highly emetogenic chemotherapy and moderately emetogenic chemotherapy when used in combination with a 5-hydroxytryptamine 3 receptor antagonist and dexamethasone. Furthermore, recent data indicate that this protection is maintained over multiple treatment cycles. Rolapitant, a selective and long-acting NK-1 receptor antagonist, is approved as oral formulation for the prevention of delayed CINV in adults. This review discusses the differential pharmacology and clinical utility of rolapitant in preventing CINV compared with other NK-1 receptor antagonists.

Keywords: antiemetics; delayed chemotherapy-induced nausea and vomiting; emesis; highly emetogenic chemotherapy; moderately emetogenic chemotherapy; neurokinin-1 receptor antagonists.

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Conflict of interest statement

Disclosure Dr Rapoport has received honoraria to participate at advisory boards for TESARO, Merck, and Heron, and he has received research funding from Merck and TESARO. Medical writing and editorial support were funded by TESARO. The author reports no other conflicts of interest.

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