Rolapitant i.v. Approved by FDA for Delayed Nausea and Vomiting Associated With Cancer Chemotherapy

Rolapitant injectable emulsion features a ready-to-use, single-dose vial for intravenous administration

On 25 October 2017, TESARO, Inc. announced that the US Food and Drug Administration (FDA) has approved rolapitant i.v. (VARUBI®) in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy. Availability of new formulation offers healthcare providers the flexibility to choose oral or i.v. administration. It provides enhanced control of delayed chemotherapy-induced nausea and vomiting (CINV) as part of an antiemetic regimen, particularly for patients receiving cisplatin, carboplatin or anthracycline/cyclophosphamide-based chemotherapy. US commercial launch is planned for November.

Delayed nausea and vomiting can occur anytime between 25 and 120 hours following chemotherapy, and is often extremely debilitating.

Rolapitant is a highly selective and competitive antagonist of human substance P/neurokinin 1 (NK-1) receptors, which play an important role in the delayed phase of CINV. With a long plasma half-life of approximately seven days, a single dose of rolapitant, as part of an antiemetic regimen, significantly improved complete response rates in the delayed phase of CINV.

Results from three phase III trials of rolpaitant oral tablets demonstrated a significant reduction in episodes of vomiting or use of rescue medication during the 25- to 120-hour period following administration of highly emetogenic and moderately emetogenic chemotherapy regimens. In addition, patients who received rolapitant reported experiencing less nausea that interfered with normal daily life and fewer episodes of vomiting or retching over multiple cycles of chemotherapy. Results from a bioequivalence trial demonstrated comparability of the i.v. and oral formulations of rolapitant.

Rolapitant i.v. is supplied in ready-to-use vials and does not require refrigerated storage or mixing. As a result, utilization in busy chemotherapy clinics is straightforward and easily adopted into existing practice patterns for administration of antiemetic regimens associated with emetogenic chemotherapy.

Rolapitant i.v. is to be administered up to two hours before chemotherapy administration in combination with a 5-HT3 receptor antagonist and dexamethasone. No dosage adjustment is required for dexamethasone, a CYP3A4 substrate, and rolapitant is the first intravenously administered NK-1 receptor antagonist approved by the FDA that does not contain polysorbate 80.

The press release of TESARO contains forward-looking statements.