Rolapitant is a substance P/neurokinin 1 (NK1) receptor antagonist indicated for use in combination with other antiemetic agents for the prevention of delayed nausea and vomiting associated with emetogenic chemotherapy. The U.S. Food and Drug Administration approved Varubi (Rolapitant) to prevent delayed phase chemotherapy-induced nausea and vomiting (emesis). Varubi is approved in adults in combination with other drugs (antiemetic agents) that prevent nausea and vomiting associated with initial and repeat courses of vomit-inducing (emetogenic and highly emetogenic) cancer chemotherapy.
NK-1 receptors are highly concentrated in the brain and bind neurokinin substance P. Activation of NK-1 receptors plays a central role in nausea and vomiting induced by emetogenic stimuli, including certain cancer chemotherapies. A Positron Emission Tomography (PET) study with Rolapitant in normal,…
