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Drugs. 2017 Oct;77(15):1687-1694. doi: 10.1007/s40265-017-0816-z.
Oral rolapitant (Varubi™; Varuby), a long-acting neurokinin-1 (NK) receptor antagonist (RA), is indicated in the USA and EU as part of an antiemetic regimen to prevent delayed chemotherapy-induced nausea and vomiting (CINV) in adults receiving highly or moderately emetogenic chemotherapy (HEC or MEC). In randomized, phase III trials, a single oral dose of rolapitant 180 mg was effective in preventing delayed CINV compared with placebo, when each was used in combination with a 5-HT RA plus dexamethasone, in adults receiving their first course of HEC or MEC. The benefits of rolapitant were maintained over multiple cycles of chemotherapy. The tolerability profile of rolapitant is similar to that of placebo and consistent with that of other NK RAs. However, rolapitant differs from other existing NK RAs in that it does not interact with CYP3A4, thereby negating the need for dexamethasone dose adjustments and potentially making rolapitant a more suitable option for patients receiving CYP3A4 substrates. Thus, oral rolapitant is an effective and well tolerated NK RA that expands the treatment options for preventing delayed CINV in adults receiving HEC or MEC.
口服洛哌丁胺（VarubiTM；Varuby），一种长效神经激肽-1（NK）受体拮抗剂（RA），在美国和欧盟被批准用于成人接受高致吐性化疗（HEC）或中度致吐性化疗（MEC）时，作为止吐方案的一部分，预防迟发性化疗引起的恶心和呕吐（CINV）。在随机、III 期试验中，与安慰剂相比，当洛哌丁胺 180mg 单药与 5-HT3RA 和地塞米松联合使用时，在接受首次 HEC 或 MEC 治疗的成人中，可有效预防迟发性 CINV。洛哌丁胺的益处可维持多个化疗周期。洛哌丁胺的耐受性与安慰剂相似，与其他 NK RAs 一致。然而，洛哌丁胺与其他现有 NK RAs 不同的是，它不与 CYP3A4 相互作用，从而无需调整地塞米松剂量，这可能使洛哌丁胺成为接受 CYP3A4 底物的患者更合适的选择。因此，口服洛哌丁胺是一种有效的、耐受性良好的 NK RA，为接受 HEC 或 MEC 治疗的成人预防迟发性 CINV 提供了更多的治疗选择。
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