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  • Title: Netupitant/Palonosetron: A Review in Chemotherapy-Induced Nausea and Vomiting.
    Author: Shirley M.
    Journal: Drugs; 2021 Jul; 81(11):1331-1342. PubMed ID: 34292534.
    Abstract:
    Netupitant/palonosetron (NEPA; Akynzeo®), available in oral and intravenous (IV) formulations, is a fixed-dose combination of the neurokinin 1 (NK1) receptor antagonist netupitant (or the prodrug, fosnetupitant, in the IV formulation) and the second-generation serotonin 3 (5-HT3) receptor antagonist palonosetron. Administered as a single dose, (fos)netupitant/palonosetron (in combination with dexamethasone) is indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) in adults. In clinical trials, (fos)netupitant/palonosetron plus dexamethasone was associated with high complete response rates (no emesis and no rescue medication) in the acute, delayed and overall phases in patients receiving highly or moderately emetogenic chemotherapy, with efficacy maintained over multiple cycles. Further, oral netupitant/palonosetron was found to be superior to palonosetron and non-inferior to aprepitant plus granisetron in preventing CINV in individual trials. Both the oral and IV formulations of the drug combination are well tolerated. The fixed-dose combination is concordant with guideline recommendations and provides a simple and convenient option for prophylaxis against acute and delayed CINV in patients receiving highly or moderately emetogenic chemotherapy. Chemotherapy-induced nausea and vomiting (CINV) is a common problem during cancer treatment. Netupitant/palonosetron (NEPA; Akynzeo®) is a fixed-dose combination of two drugs (netupitant, a neurokinin 1 receptor antagonist; and palonosetron, a serotonin 3 receptor antagonist) which target two different signalling pathways involved in the induction of vomiting. Approved for use in the prevention of acute and delayed CINV in adults, netupitant/palonosetron is given orally or via intravenous infusion as a single dose prior to chemotherapy. In clinical trials, high proportions of patients who received netupitant/palonosetron (used in combination with the corticosteroid dexamethasone) prior to chemotherapy reported no vomiting, no requirement for rescue medication, and no significant nausea in the 5 days post chemotherapy. Both the oral and intravenous formulations of the drug combination are well tolerated. In conclusion, netupitant/palonosetron is a simple, convenient and effective drug combination for the prevention of acute and delayed CINV in patients receiving chemotherapy that has a moderate to high potential to cause nausea and vomiting.
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