2015年9月1日，美国食品和药品监管局(FDA)批准Varubi(rolapitant)片剂预防延迟期化疗诱发恶心和呕吐。Varubi被批准在成年与其他药物(止吐药)联用预防恶心和呕吐伴随开始和重复疗程呕吐诱导(致吐和高度致吐)癌症化疗。恶心和呕吐是癌症患者进行化疗经历的常见副作用。化疗药物给药后症状可能持续数天。化疗开始后恶心和呕吐从24小时发生直至120小时被称为延迟期恶心和呕吐，和它可能导致严重健康合并症。在癌症患者延长恶心和呕吐可导致体重减轻，脱水和营养不良导致住院。
FDA药品评价和研究中心药物评价III室副主任Amy Egan，M.D.，M.P.H.说：“化疗诱发恶心和呕吐仍然可扰乱患者生活和有时他们的治疗重大问题，” 。“今天的批准提供癌症患者另一种治疗选择为预防化疗所致延迟期恶心和呕吐。”
Varubi是一种物质P/神经激肽-1(NK-1)受体拮抗剂。某些癌化疗诱导的恶心和呕吐NK-1受体的激活起中心作用，尤其是在延迟期。Varubi是以片形式提供患者。
在三项随机化，双盲，对照临床试验其中Varubi 与格拉司琼[granisetron]和地塞米松[dexamethasone]联用与一种对照治疗(安慰剂，格拉司琼和地塞米松)比较在2,800例患者接受一种化疗方案包括高度致吐(例如顺铂[cisplatin]和蒽环类药物[anthracycline]和环磷酰胺[cyclophosphamide])联用和中度致吐化疗药物确定Varubi的安全性和疗效。用Varubi治疗患者和对恶心和呕吐延迟期期间抢救药物的使用与接受对照治疗患者比较呕吐有更大减低。Varubi抑制CYP2D6酶，它负责某些药物的代谢。Varubi是禁忌与硫利达嗪[thioridazine]使用，一种被CYP2D6酶代谢的药物，因为两种药物一起使用可能增加血中硫利达嗪的量和致可能严重的异常心节律。
在用Varubi治疗患者中最常见副作用包括低白细胞计数(中性粒细胞减少)，打嗝，食欲减低和眩晕.
Varubi由总部设在马萨诸塞州沃尔瑟姆Tesaro公司销售。

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TESARO Announces U.S. FDA Approval of VARUBI(TM) (rolapitant) for Nausea and Vomiting Associated With Cancer Chemotherapy
 U.S. Food and Drug Administration (FDA) has approved VARUBI™ (rolapitant) 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.  
VARUBI is a selective and competitive antagonist of human substance P/neurokinin 1 (NK-1) receptors, with a plasma half-life of approximately seven days. Results from three Phase 3 trials of VARUBI demonstrated a significant reduction in episodes of vomiting or use of rescue medication during the 25 to 120 hour period following administration of highly emetogenic and moderately emetogenic chemotherapy regimens. In addition, patients who received VARUBI reported experiencing less nausea that interfered with normal daily life and fewer episodes of vomiting or retching over multiple cycles of chemotherapy. A 180 milligram dose of VARUBI is to be administered approximately one to two hours prior to chemotherapy administration in combination with a 5-HT3 receptor antagonist and dexamethasone. No dosage adjustment is required for dexamethasone, a CYP3A4 substrate, when administering VARUBI.  
"The approval of VARUBI, our first product, represents a significant milestone in TESARO's evolution into an integrated biopharmaceutical company with strong development and commercialization capabilities," said Lonnie Moulder, CEO of TESARO.  "Results from the Phase 3 trials of VARUBI demonstrated that patients receiving emetogenic chemotherapy agents, including platinum and cyclophosphamide-containing regimens, benefitted from the addition of VARUBI to their antiemetic regimen. Data from multiple well-controlled trials demonstrate that patients who receive only a 5-HT3 receptor antagonist and dexamethasone often continue to suffer from nausea and vomiting for several days following chemotherapy administration. Patient surveys and our primary market research also point to the high rate of CINV and its potentially debilitating effects. We look forward to expanding the awareness of CINV and working with healthcare providers to make this important medicine available to patients during the fourth quarter."   
"While important strides in preventing nausea and vomiting associated with chemotherapy have been made, still up to half of patients receiving emetogenic cancer chemotherapy can experience delayed CINV," said Richard J. Gralla, M.D., Professor of Medicine at Albert Einstein College of Medicine in New York. "Because NK-1 receptors are key drivers of CINV, especially in the delayed Phase, NK-1 receptor antagonists such as VARUBI, when combined with a 5-HT3 receptor antagonist and a corticosteroid, provide enhanced protection from CINV, and do so in the delayed timeframe where the most help is needed."
The full prescribing information for VARUBI will be available at www.VarubiRx.com.
About Chemotherapy-Induced Nausea and Vomiting (CINV)
Chemotherapy-induced nausea and vomiting is a debilitating, yet often preventable, side effect of chemotherapy.
Up to 50% of patients undergoing highly or moderately emetogenic chemotherapy experience delayed CINV (25 to 120 hours post chemotherapy)—even when prescribed a 5-HT3 receptor antagonist and corticosteroid.
Blocking both 5-HT3 and NK-1 receptors has been shown to offer better control of nausea and vomiting than inhibiting 5-HT3 receptors alone. Adding a single dose of VARUBI to an antiemetic regimen, including a 5-HT3 receptor antagonist and corticosteroid, further improves prevention of CINV in the delayed Phase following chemotherapy.
About the VARUBI (Rolapitant) Clinical Program
The superior efficacy of VARUBI was established in multiple randomized, well-controlled, blinded clinical trials that enrolled more than 2,500 patients. VARUBI, when administered in combination with a 5-HT3 receptor antagonist and dexamethasone, was superior to a 5-HT3 receptor antagonist and dexamethasone in preventing CINV in patients receiving either moderately or highly emetogenic chemotherapy.
The clinical profile of VARUBI in cisplatin-based highly emetogenic chemotherapy (HEC) was confirmed in two identical Phase 3 studies: HEC1 and HEC2. Both trials met their primary endpoint of complete response (CR), and demonstrated statistical superiority of rolapitant 180 mg compared to active control (5-HT3 receptor antagonist + dexamethasone) in the delayed Phase (25–120 hours) of CINV. In HEC1, 264 patients received rolapitant 180 mg and 262 received control. The proportion of patients achieving a CR was 72.7% vs. 58.4% (p=<0.001). In HEC2, 271 patients received rolapitant and 273 received control. The proportion of patients achieving a CR was 70.1% vs. 61.9% (p=0.043). The most common adverse reactions (≥3%) among patients receiving cisplatin-based chemotherapy were neutropenia (9% VARUBI vs. 8% control), hiccups (5% vs. 4%), and abdominal pain (3% vs. 2%).
A Phase 3 trial was also conducted to evaluate rolapitant 180 mg compared to active control in 1,332 patients receiving moderately emetogenic chemotherapy regimens, including anthracycline/cyclophosphamide combinations, carboplatin, irinotecan, pemetrexed, oxaliplatin, and doxorubicin. This trial met its primary endpoint of CR, and demonstrated statistical superiority of rolapitant 180 mg compared to active control (5-HT3 receptor antagonist + dexamethasone) in the delayed Phase of CINV. The proportion of patients achieving a CR was 71.3% vs 61.6% (p=<0.001). The most common adverse reactions (≥3%) among patients receiving these chemotherapies were decreased appetite (9% VARUBI vs. 7% control), neutropenia (7% vs. 6%), dizziness (6% vs. 4%), dyspepsia (4% vs. 2%), urinary tract infection (4% vs. 3%), stomatitis (4% vs. 2%), and anemia (3% vs. 2%).
Primary data from the three Phase 3 studies have recently been published online ahead of print in Lancet Oncology, the analysis of the non-AC MEC population was presented at the 2015 annual meeting for the Multinational Association for Supportive Care in Cancer, and commentary has been provided in Nature Reviews Clinical Oncology.
VARUBI Additional Safety Information
VARUBI is contraindicated in patients receiving thioridazine, a CYP2D6 substrate with a narrow therapeutic index.
Use of VARUBI should be avoided in patients who are receiving pimozide, a CYP2D6 substrate with a narrow therapeutic index. Adverse reactions should be monitored if concomitant use of VARUBI and other CYP2D6 substrates with a narrow therapeutic index cannot be avoided. The inhibitory effect of VARUBI on CYP2D6 lasts for at least 7 days and may last longer after administration of a single dose of VARUBI.
VARUBI is available by prescription only.
About VARUBI
VARUBI is a substance P/neurokinin-1 (NK-1) receptor antagonist indicated 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. NK-1 receptors are highly concentrated in the brain and bind neurokinin substance P. Activation of NK-1 receptors plays a central role in nausea and vomiting induced by emetogenic stimuli, including certain cancer chemotherapies. A Positron Emission Tomography (PET) study with rolapitant in normal, healthy volunteers demonstrated that rolapitant crosses the blood brain barrier and occupies brain NK-1 receptors at high levels for up to 120 hours. VARUBI has a half-life of approximately 7 days, which may contribute to the ability of a single dose of VARUBI to cover the entire delayed CINV Phase (25-120 hours).
An intravenous formulation of rolapitant is also being developed. TESARO licensed exclusive rights for the development, manufacture, commercialization and distribution of VARUBI (rolapitant) from OPKO Health, Inc.