The U.S. Food and Drug Administration approved rolapitant to prevent delayed phase chemotherapy-induced nausea and vomiting (emesis).
Rolapitant is a substance P/neurokinin-1 (NK-1) receptor antagonist. Activation of NK-1 receptors plays a central role in nausea and vomiting induced by certain cancer chemotherapies, particularly in the delayed phase.
Rolapitant inhibits the CYP2D6 enzyme, which is responsible for metabolizing certain drugs. Rolapitant is contraindicated with the use of thioridazine; a drug metabolized by the CYP2D6 enzyme, because use of the two drugs together may increase the amount of thioridazine in the blood and cause an abnormal heart rhythm that can be serious.
The most common side effects in patients treated with Rolapitant include a low white blood cell count (neutropenia), hiccups, decreased appetite and dizziness.