On 2 September 2015, the US Food and Drug Administration (FDA) approved rolapitant (Varubi) to prevent delayed phase of chemotherapy-induced nausea and vomiting (emesis). Rolapitant is approved in adults in combination with other antiemetic agents that prevent nausea and vomiting associated with emetogenic and highly emetogenic cancer chemotherapy.
Nausea and vomiting that occurs from 24 hours to up to 120 hours after the start of chemotherapy is referred to as delayed phase nausea and vomiting, and it can result in serious health complications. Prolonged nausea and vomiting can lead to weight loss, dehydration and malnutrition in cancer patients leading to hospitalisation.
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 is provided to patients in tablet form.
The safety and efficacy of rolapitant were established in three randomised, double-blind, controlled clinical trials where rolapitant in combination with granisetron and dexamethasone was compared with a control therapy (placebo, granisetron and dexamethasone) in 2,800 patients receiving a chemotherapy regimen that included highly emetogenic (such as cisplatin and the combination of anthracycline and cyclophosphamide) and moderately emetogenic chemotherapy drugs. Those patients treated with rolapitant had a greater reduction in vomiting and use of rescue medication for nausea and vomiting during the delayed phase compared to those receiving the control therapy.
Rolapitant inhibits the CYP2D6 enzyme, which is responsible for metabolising certain drugs. Rolapitant is contraindicated with the use of thioridazine, a drug metabolised 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 neutropaenia, hiccups, decreased appetite and dizziness.