英文药名：Bevyxxa(betrixaban capsules) 中文药名：贝曲西班胶囊 生产厂家：Portola制药 药品介绍 近日，由Portola制药公司研发的新药Bevyxxa(betrixaban 中文译名：贝曲沙班)获美国FDA批上市。本品是目前预防急性重症病人的静脉血栓（VTE）及并发症形成的唯一一款口服抗凝血剂。 批准日期：2017年6月23日；公司：Portola Pharmaceuticals Inc. Bevyxxa(贝曲沙班[betrixaban])胶囊 供口服使用 作用机制 Betrixaban是一种口服FXa抑制剂选择性地阻断FXa的活性部位和对活性不需要辅助因子(例如抗-凝血酶III)。Betrixaban抑制游离FXa和凝血酶原酶活性。通过直接地抑制FXa，betrixaban 减低凝血酶生成(TG)。Betrixaban对血小板聚集没有直接作用。 适应证和用途 BEVYXXA是一种因子Xa(FXa)抑制剂适用为静脉血栓栓塞(VTE)的预防在成年患者为急性疾病住院处于对血栓栓塞并发症由于中度或严重活动受限和对VTE其他风险因子的风险。 使用的限制： 尚未在确定人工心脏瓣膜患者BEVYXXA的安全性和疗效因为未曽研究这个人群。 剂量和给药方法 BEVYXXA的推荐的剂量是一个初始单次剂量的160mg，接着用80mg每天1次，在每天相同时间与食物服用。推荐的治疗时间是35至42天。 ●对有严重肾受损患者减低剂量.。 ●对用P-糖蛋白(P-gp)抑制剂患者减低剂量。 剂型和规格 胶囊：40mg和80mg 禁忌证 ●活动性病理学出血。 ●对betrixaban BEVYXXA严重超敏性反应。 警告和注意事项 ●出血的风险：可能致严重，潜在地致命出血。及时评价血液丢失体征和症状。 ●严重肾受损：增加出血事件风险：减低BEVYXXA剂量。 ●同时P-gp抑制剂：增加出血事件风险：减低BEVYXXA剂量。 不良反应 最常见不良反应(发生率 >5%)是出血。 药物相互作用 ●P-gp抑制剂增加betrixaban的血水平。减低BEVYXXA剂量。 ●抗凝剂：避免同时使用。 在特殊人群中使用 ●妊娠：仅使用如潜在地获益胜过对母亲或胎儿潜在风险。 ●肾受损：减低剂量。 ●肝受损：避免使用。 包装规格/贮存和处置 供应 下面列出可得到的BEVYXXA(betrixaban)胶囊： 40 mg大小4粒胶囊是浅灰色印有黑色40，和有一个蓝色盖印有白色PTLA。 ●100粒瓶(NDC 69853-0202-1) 80mg大小2粒胶囊是浅灰色印有黑色80，和有一个蓝色盖印有白色PTLA。 ● 100瓶(NDC 69853-0201-1) 贮存和处置 贮存在室温：20°C至25°C(68°F至77°F). 完整说明书附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ebaa2dd9-257e-4a68-ab6a-fb2791bb62ce U.S. Food and Drug Administration (FDA) has approved Bevyxxa (betrixaban), the first and only anticoagulant for hospital and extended duration prophylaxis (35 to 42 days) of venous thromboembolism (VTE) in adult patients hospitalized for an acute medical illness who are at risk for thromboembolic complications due to moderate or severe restricted mobility and other risk factors for VTE. Bevyxxa, an oral, once-daily Factor Xa inhibitor, was granted a Fast Track designation and approved by the FDA under Priority Review, which is a status given to drugs that may offer significant improvements in treatment or provide a treatment where no adequate therapy exists. Bevyxxa has been approved based on data from Portola's pivotal Phase 3 APEX Study, which enrolled 7,513 patients at more than 450 clinical sites worldwide. "Bevyxxa represents a major advance for the field of thrombosis. It is the first therapy to demonstrate a reduction in the incidence of VTE in these high-risk patients without a significant increase in major bleeding,” said C. Michael Gibson, M.D., APEX Executive Committee Member and Steering Committee Chairman, professor, Harvard Medical School and chairman of the PERFUSE Study Group. “With this approval, we are finally able to help protect these patients from this often fatal, yet preventable condition.” “Our goal as a company is to bring to market important medicines for the benefit of patients,” said Bill Lis, Chief Executive Officer of Portola. “Today’s approval is the ultimate milestone for Portola. We are grateful to the patients who participated in our trials, the FDA, our academic collaborators and investigators, and, importantly, our dedicated employees who have worked tirelessly to achieve this goal.” Acutely ill medical patients are those hospitalized for serious medical conditions, including heart failure, stroke, infection and pulmonary disease. Because of their underlying disorder and immobilization, they are at increased risk of developing deep vein thrombosis (DVT) and pulmonary embolism (PE) blood clots.  In the G7 countries, an estimated 24 million acutely ill medical patients are hospitalized each year and are at risk of VTE, either while in the hospital or following discharge. More than one million VTE events and 150,000 VTE-related deaths occur annually in acutely ill medical patients in the G7 countries, despite the standard use of injectable enoxaparin and other heparins in the hospital. More than half of VTE events occur after patients are discharged from the hospital. No other anticoagulant, including enoxaparin or any of the marketed oral Factor Xa inhibitors, is approved for in-hospital and extended-duration VTE prophylaxis in acutely ill medical patients. The APEX study evaluated oral betrixaban for 35 to 42 days compared with injectable enoxaparin for 6 to 14 days followed by placebo in assessing the prevention of VTE in high-risk acutely ill medical patients. As detailed in the prescribing information, Bevyxxa efficacy was measured in the modified Intent-to-Treat (mITT) analysis, which includes 7,441 patients assessed by a composite outcome score comprising either the occurrence of asymptomatic proximal DVT or symptomatic DVT, non-fatal PE or VTE-related death. Bevyxxa reduced the incidence of DVT and PE blood clots compared with those taking enoxaparin plus placebo (4.4 percent vs. 6.0 percent; relative risk 0.75, 95 percent CI: 0.61, 0.91) with no significant increase in major bleeding (0.67 percent vs. 0.57 percent). The most frequent reason for treatment discontinuation was bleeding, with an incidence rate for all bleeding episodes of 2.4 percent and 1.2 percent for betrixaban and enoxaparin, respectively. BEVYXXA INDICATION AND USE Bevyxxa(betrixaban) is indicated for the prophylaxis of VTE in adult patients hospitalized for an acute medical illness who are at risk for thromboembolic complications due to moderate or severe restricted mobility and other risk factors for VTE. The recommended dose of Bevyxxa is an initial single dose of 160 mg starting on day 1, followed by 80 mg once daily taken for 35 to 42 days at the same time each day with food. Limitations of Use The safety and effectiveness of Bevyxxa have not been established in patients with prosthetic heart valves because this population has not been studied. IMPORTANT SAFETY INFORMATION FOR BEVYXXA Warning: Spinal/Epidural Hematoma Epidural or spinal hematomas may occur in patients treated with betrixaban who are receiving neuraxial anesthesia or undergoing spinal puncture. The risk of these events may be increased by the use of in-dwelling epidural catheters or the concomitant use of medical products affecting hemostasis. These hematomas may result in long-term or permanent paralysis. Consider these risks when scheduling patients for spinal procedures.   CONTRAINDICATIONS Active pathological bleeding; severe hypersensitivity reaction to Bevyxxa. WARNINGS AND PRECAUTIONS Risk of Bleeding Bevyxxa increases the risk of bleeding and can cause serious and potentially fatal bleeding; concomitant use of drugs affecting hemostasis increases the risk of bleeding. These include aspirin and other antiplatelet agents, other anticoagulants, heparin, thrombolytic agents, selective serotonin reuptake inhibitors, serotonin norepinephrine reuptake inhibitors, and nonsteroidal anti-inflammatory drugs (NSAIDs). Advise patients of signs and symptoms of blood loss and to report them immediately or go to an emergency room. Promptly evaluate any signs or symptoms of blood loss and consider the need for blood replacement. Discontinue Bevyxxa in patients with active pathological bleeding. There is no established way to reverse the anticoagulant effect of betrixaban, which can be expected to persist for at least 72 hours after the last dose. Spinal/Epidural Anesthesia or Puncture When neuraxial anesthesia (spinal/epidural anesthesia) or spinal/epidural puncture is employed, patients treated with antithrombotic agents for prevention of thromboembolic complications are at risk of developing an epidural or spinal hematoma which can result in long-term or permanent paralysis. An epidural catheter should not be removed earlier than 72 hours after the last administration of Bevyxxa. The next Bevyxxa dose is not to be administered earlier than 5 hours after the removal of the catheter. If traumatic puncture occurs, delay the administration of Bevyxxa for 7 hours. Monitor patients frequently for signs and symptoms of neurological impairment (e.g., numbness or weakness of the legs, bowel or bladder dysfunction).  If neurological compromise is noted, urgent diagnosis and treatment is necessary. Use in Patients with Severe Renal Impairment Patients with severe renal impairment (CrCl ≥ 15 to < 30 mL/min computed by Cockcroft-Gault) taking Bevyxxa may have an increased risk of bleeding events. Reduce dose of Bevyxxa, monitor patients closely, and promptly evaluate any signs or symptoms of blood loss in these patients. Use in Patients on Concomitant P-glycoprotein (P-gp) Inhibitors Patients on concomitant P-gp inhibitors with Bevyxxa may have an increased risk of bleeding. Reduce dose of Bevyxxa, monitor patients closely, and promptly evaluate any signs or symptoms of blood loss in these patients. Avoid use of Bevyxxa in patients with severe renal impairment receiving concomitant P‑gp inhibitors. ADVERSE REACTIONS The most common adverse reactions with Bevyxxa were related to bleeding (> 5 percent). USE IN SPECIFIC POPULATIONS Hepatic Impairment Bevyxxa has not been evaluated in patients with hepatic impairment, because these patients may have intrinsic coagulation abnormalities. Bevyxxa is not recommended in patients with hepatic impairment. For additional information and full Prescribing Information for Bevyxxa, please visit.