TESARO Inc has announced that rolapitant (Varubi), a neurokinin-1 (NK-1) receptor antagonist, is now available in the United States. Rolapitant was approved by the US Food and Drug Administration (FDA) in September 2015 for the prevention of delayed chemotherapy-induced nausea and vomiting in combination with other antiemetic agents.

“Blocking both 5-HT3 and NK-1 receptors has been shown to offer better control of nausea and vomiting than by inhibiting 5-HT3 receptors alone,” said Lee S. Schwartzberg, MD, FACP, executive director of West Cancer Center.

Rolapitant is to be administered as a single dose consisting of two 90-mg tablets approximately 1 to 2 hours prior to chemotherapy administration in combination with a 5-HT3 receptor antagonist and dexamethasone.

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“Adding a single dose of Varubi to an antiemetic regimen, including a 5-HT3 receptor antagonist and corticosteroid, may result in fewer episodes of vomiting or use of rescue medication, as well as less nausea that interferes with normal daily life in the days following chemotherapy. In addition, no dosage adjustment is required for dexamethasone, a CYP3A4 substrate, when administering Varubi.”

The National Comprehensive Cancer Network (NCCN) Clinical Practice Guidelines in Oncology for Antiemesis already recommend rolapitant as an option for CINV, in combination with other antiemetic agents, for patients receiving highly emetogenic or moderately emetogenic chemotherapy. Category 1 designation was granted to rolapitant for both uses.

“Varubi represents a meaningful option in cancer supportive care, for both patients and physicians,” Schwartzberg said.


  1. TESARO announces the launch of Varubi (rolapitant) in the United States [news release]. Waltham, MA: TESARO Inc; November 16, 2015. http://www.multivu.com/players/English/7647751-tesaro-varubi-rolapitant-u-s/. Accessed November 20, 2015.