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Drugs. 2021 Jul;81(11):1331-1342. doi: 10.1007/s40265-021-01558-2. Epub 2021 Jul 22.
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-HT) 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.
奈妥匹坦/帕洛诺司琼(NEPA;Akynzeo)有口服和静脉(IV)两种剂型,是一种固定剂量组合药物,包含神经激肽 1(NK1)受体拮抗剂奈妥匹坦(或 IV 剂型中的前药福沙奈妥匹坦)和第二代 5-羟色胺 3(5-HT3)受体拮抗剂帕洛诺司琼。单剂量给药时,(福沙)奈妥匹坦/帕洛诺司琼(与地塞米松合用)适用于预防成人急性和延迟性化疗引起的恶心和呕吐(CINV)。在临床试验中,(福沙)奈妥匹坦/帕洛诺司琼加地塞米松在接受高致吐性或中致吐性化疗的患者的急性期、延迟期和总期均与高完全缓解率(无恶心和无解救药物)相关,且疗效在多个周期中保持。此外,在个别试验中,口服奈妥匹坦/帕洛诺司琼在预防 CINV 方面优于帕洛诺司琼,且与阿瑞匹坦联合格拉司琼相当。该药的口服和静脉两种剂型均具有良好的耐受性。这种固定剂量组合符合指南建议,为接受高致吐性或中致吐性化疗的患者提供了一种预防急性和延迟性 CINV 的简单方便的选择。