新型化疗止吐新药VARUBI IV（rolapitant）获FDA批准，两种配方使用更方便。
2017年10月29日，TSRO（TESARO,Inc ）宣布，FDA批准VARUBI IV联合其他止吐剂用于治疗癌症化疗出现的呕吐症状。在化疗后的第25到120个小时，延迟恶心和呕吐随时可能发生，而且往往会使人非常虚弱。
VARUBI IV能够特异竞争性结合 P/neurokinin 1 (NK-1)受体，该受体在化疗后延迟性恶心和呕吐（CINV）的发生起着重要的作用。单一剂量VARUBI IV在血浆中的半衰期为7天，接受单一剂量VARUBI IV治疗后能够显著提高CINV的完全缓释率。
VARUBI IV的临床III期试验结果表明，在接受VARUBI IV治疗后，化疗后的第25到120个小时中，病人发生呕吐或使用抢救药物的次数显著减少。此外，接受VARUBI IV治疗的患者表示，他们的恶心程度减轻。生物等效性试验结果显示IV型与原始版本的VARUBI有效性相当。
VARUBI IV不需要冷藏或混合，是即食型药物，给治疗带来了极大的便利。VARUBI IV可与5-HT3受体拮抗剂和地塞米松联合治疗，在化疗前两小时服用。地塞米松是CYP3A4底物，而VARUBI IV是FDA批准的首个不含聚山梨酯80的受体拮抗剂。
TSRO总裁兼COO Mary Lynne Hedley博士说：“VARUBI IV的批准是TSRO的一种重要的里程碑。大多数NK-1受体拮抗剂是静脉注射药物，随着VARUBI IV的批准，能够为医生和患者提供更为便利的治疗方案。
原文链接：TESARO Announces U.S. FDA Approval of VARUBI® IV for Delayed Nausea and Vomiting Associated With Cancer Chemotherapy
Varubi IV Approved for Delayed Chemotherapy-Induced Nausea/Vomiting
The Food and Drug Administration (FDA) has approved an intravenous (IV) formulation of Varubi (rolapitant; Tesaro) for use in combination with other antiemetics in adults to prevent delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy.
Varubi, a highly selective and competitive antagonist of human substance P/neurokinin (NK-1) receptor, is already available as 90mg strength tablets. Clinical data from a bioequivalence trial showed comparability of the oral and IV formulations of Varubi
Varubi IV should be administered intravenously within 2 hours prior to the start of chemotherapy as a 30-minute infusion. Common infusion-related adverse events include sensation of warmth, abdominal pain, dizziness, and paresthesia.
Varubi IV will be available as a single-dose vial containing 166.5mg/92.5mL (1.8mg/mL) strength injectable emulsion. It is anticipated to launch in November 2017.
Varubi(rolapitant) tabs
VARUBI
Nausea Only 4 drugs may be compared at once
Generic Name and Formulations:
Rolapitant 90mg; tabs.
Company:
Tesaro, Inc.
Select therapeutic use: Nausea
Indications for VARUBI:
In combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy.
Adult：
Give Varubi before starting each cycle, but at no less than 2 week intervals. ≥18yrs: Highly emetogenic cisplatin-based chemotherapy: 180mg within 2hrs prior to chemotherapy with dexamethasone 20mg given 30mins prior to chemotherapy and a 5-HT3 receptor antagonist (see drug's full labeling for appropriate dosing) on Day 1, then dexamethasone 8mg twice daily on Days 2–4. Moderately emetogenic chemotherapy and combinations of anthracycline and cyclophosphamide: 180mg within 2hrs prior to chemotherapy with dexamethasone 20mg given 30mins prior to chemotherapy on Day 1 and a 5-HT3 receptor antagonist (see drug's full labeling for appropriate dosing) on Days 1– 4.
Children:
<18yrs: not established.
Contraindications:
Concomitant CYP2D6 substrates with narrow therapeutic index (eg, thioridazine, pimozide): may result in QT prolongation and Torsades de pointes; consider alternatives if use required.
Warnings/
