新型化疗止吐药VARUBI获FDA批准上市，静脉注射+片剂（两种配方）使用更方便。

近日，TESARO公司宣布其新药VARUBI（rolapitant）IV获得美国FDA批准，用于和其它止吐药物一起治疗由于癌症化疗导致的延迟恶心和呕吐（CINV）。
化疗副作用严重影响患者生活
CINV通常在化疗后的25-120小时内发生，这些症状会让患者非常虚弱，对患者的生活质量造成很大影响。有高达50％的接受化疗的患者可能出现CINV，即便他们已经接受了5-HT3 受体拮抗剂和皮质类固醇的治疗，这些症状仍然可能出现。
Rolapitant是一种具备高度选择性的人类神经激肽（NK-1）受体的竞争性拮抗剂，NK-1受体CINV的延迟期阶段起着重要作用。Rolapitant在血液中的半衰期长达7天，因此只需要在止吐疗法中加入一剂rolapitant，就能显著提高延迟期CINV患者的完全缓解（CR）率。Rolapitant的口服配方在2015年就获得了FDA的批准，此次获批的是rolapitant的静脉注射配方。这种配方不需要冷藏和另用溶剂溶解，可以直接使用，让医护人员可以选择以口服或者静脉注射的方式为患者施用药物。这给在繁忙的医院中工作的医护人员带来诸多便利，让他们更容易将rolapitant的使用整合到化疗疗程中去。
两种配方达到同等效果
在三项总计包含超过2500名患者的临床3期试验中，口服rolapitant药片能够显著降低接受高度或中度致吐化疗的患者在治疗后25-120小时内呕吐的频率和使用救援药物的次数。另外，服用rolapitant的患者报告的影响日常生活的恶心次数也有所减少。而且接受多个化疗周期的患者在整个治疗过程中呕吐的次数也显著减少。TESARO公司进行的3期临床生物等效性试验表明，rolapitant的口服配方和静脉注射配方能够在健康志愿者体内达到同样的药物水平。
“VARUBI IV获得FDA批准是TESARO公司的一个重要的里程碑。在美国，大多数NK-1受体拮抗剂是通过静脉注射来施用的。VARUBI IV提供给医疗工作者一个独特、便捷的选择，它很容易被整合到化疗诊所或医院的标准治疗程序中，”TESARO公司的总裁兼首席运营官Mary Lynne Hedley博士说：“我们将继续努力提高大众对化疗导致的延迟恶心和呕吐的认识。我们计划将在下个月将这一重要药物推向市场。”

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/Precautions:
Consider interactions with CYP2D6 substrates before starting treatment. Avoid in severe hepatic impairment; monitor if use cannot be avoided. Pregnancy. Nursing mothers.
Interactions:
See Contraindications. Potentiates CYP2D6 substrates (eg, dextromethorphan) and possibly others; see full labeling. Antagonized by strong CYP3A4 inducers (eg, rifampin); avoid. Tabs: potentiates BCRP substrates (eg, methotrexate, topotecan, irinotecan) and P-gp substrates (eg, digoxin) with narrow therapeutic index; monitor if use cannot be avoided. Use lowest effective dose of rosuvastatin (see drug's full labeling for dosing). Monitor INR and PT with concomitant warfarin; adjust dose as needed.
Pharmacological Class:
Substance P/NK1 receptor antagonist.
Adverse Reactions:
Neutropenia, hiccups, abdominal pain, decreased appetite, dizziness, dyspepsia, UTI, stomatitis, anemia.
Generic Availability:
NO
How Supplied:
Single dose pack—1 (2 x 90mg tabs)