英文药名：AKYNZEO(netupitant/palonosetron capsules) 中文药名：奈妥吡坦/帕洛诺司琼复方胶囊 生产厂家：Eisai Inc 药品简介 Akynzeo(netupitant and palonosetron)由Helsinn公司生产并研发，于2014年获美国FDA批准上市。 Akynzeo是netupitant，P物质/神经激肽1（NK 1）受体拮抗剂，以及帕洛诺司琼，5-羟色胺3（5-HT 3）受体拮抗剂的固定组合。口服帕洛诺司琼防止在急性期的恶心和呕吐以及netupitant防止恶心和呕吐期间都癌症化疗后的急性和延迟相位。 Akynzeo是专用于预防急性和迟发性恶心和与癌症化疗的初始和重复场，包括相关的呕吐的说明，但不限于，高致吐化疗。 Akynzeo是提供一个胶囊用于口服给药。Akynzeo应的化疗，woth或不与食物开始之前施用约1小时。 AKYNZEO(netupitant和帕诺斯琼 palonosetron) 胶囊为化疗使用 批准日期：2014年10月10日；公司：Helsinn组和Eisai Inc 美国初次批准：2014 适应证和用途 AKYNZEO是netupitant和帕诺斯琼固定组合，前者是一种物质P/神经激肽1(NK1)受体拮抗剂，后者一种5-羟色胺-3(5-HT3)受体拮抗剂适用为预防伴随癌症化疗的初始和重复疗程的急性和延迟恶心和呕吐，包括，但不限于，高度致吐化疗。口服帕诺斯琼预防癌症化疗后急性相期间恶心和呕吐和netupitant预防急性和延迟相二者期间恶心和呕吐。 剂量和给药方法 化疗开始前约1小时给予一粒AKYNZEO胶囊。 AKYNZEO可有或无食物服用。 剂型和规格 胶囊：300mg netupitant/0.5mg帕诺斯琼。 禁忌证 无 警告和注意事项 ⑴ 在接受帕诺斯琼对其他5-HT3受体拮抗剂有或无已知超敏性患者中曾报道超敏性反应，包括过敏反应。 ⑵用单独5-HT3受体拮抗剂曾报道5-羟色胺综合征但特别是同时使用5-羟色胺激活药物。 不良反应 最常见不良反应(发生率≥3%和大于帕诺斯琼)是头痛，无力，消化不良，疲乏，便秘和红斑。 药物相互作用 ⑴ CYP3A4底物：CYP3A4被netupitant的抑制作用可能导致同时药物血浆浓度增高，可能持续至少4天和可能持续较长于单次剂量给予AKYNZEO；谨慎使用。 ⑵ CYP3A4诱导剂(如，利福平[rifampin])：netupitant血浆浓度减低；避免使用。 特殊人群中使用 ⑴ 肝受损：在有严重肝受损患者中避免使用。 ⑵ 肾受损：在有严重肾受损或肾病终末期患者中避免使用。 供应/贮存和处置 NDC 62856-796-01，AKYNZEO (300 mg netupitant/0.5mg帕诺斯琼)。AKYNZEO以硬明胶胶囊有白色体和焦糖帽在体部印有“HE1”，每吸塑一粒胶囊供应。 贮存 贮存在20 °C至25 °C(68 °F至77 °F)；外出允许从15 °C至30 °C(59 °F至86 °F)[见USP控制室温]。 完整说明书附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8e47618e-af46-4d82-94e8-1507c042252d 包装规格 AKYNZEO 300MG/0.5MG CAP 1/EA  NETUPITANT/PALONOSETRON  EISAI INC.  62856-0796-01 AKYNZEO CAP 300MG/0.5 MG 1  NETUPITANT/PALONOSETRON HCL  EISAI INC  62856-0796-01 AKYNZEO 300MG/0.5MG CAP 1/EA  NETUPITANT/PALONOSETRON  HELSINN THERAPEUTICS  69639-0101-01 AKYNZEO CAP 300MG/0.5MG 1  NETUPITANT/PALONOSETRON HCL  HELSINN THERAPEUTICS INC  69639-0101-01 AKYNZEO CAP 235mg/0.25MG 1  NETUPITANT/PALONOSETRON HCL  HELSINN THERAPEUTICS INC 69639-102-01 FDA Approves AKYNZEO(netupitant/palonosetron) for the Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV) 13, 2014 /PRNewswire/ -- Helsinn Group and Eisai Inc. announced today that the Food and Drug Administration (FDA) approved AKYNZEO® for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy. AKYNZEO is the first approved fixed combination oral agent that targets two critical signaling pathways associated with CINV by combining netupitant, an NK1 receptor antagonist, and palonosetron, a 5-HT3 receptor antagonist, in a single capsule for the prevention of CINV. "Patients receiving chemotherapy face a significant burden due to CINV. AKYNZEO may help alleviate part of that burden of chemotherapy by better managing nausea and vomiting up to five days following chemotherapy," said Paul J. Hesketh, M.D., AKYNZEO pivotal study lead author and chair, Lahey Health Cancer Institute and director of Thoracic Oncology, Lahey Hospital & Medical Center. "The results from the pivotal trials show that AKYNZEO provides superior prevention against nausea and vomiting compared with oral palonosetron. As a result, physicians may be able to help patients manage CINV with a treatment that works both at the time of chemotherapy administration, and up to five days following treatment." The approval of AKYNZEO was based on the submission of Phase 2 and Phase 3 trials with AKYNZEO in patients undergoing treatment with moderately and highly emetogenic chemotherapy regimens for a variety of tumor types. The most common adverse events reported with AKYNZEO were headache, asthenia, fatigue, dyspepsia, constipation and erythema. CINV is one of the most common side effects of chemotherapy. Its management has been refined over the past several decades, but despite the existence of effective treatments and clear antiemetic guidelines, many patients still suffer from CINV, particularly during the delayed phase after chemotherapy. Studies show that patients often receive antiemetic drug regimens that are inconsistent with CINV treatment guidelines, which call for multiple-pathway targeted antiemetic prophylaxis. AKYNZEO provides cancer care teams with two antiemetics in a single oral fixed combination capsule. A combination of an NK1 receptor antagonist, a 5-HT3 receptor antagonist and dexamethasone meets guideline recommendations for optimal antiemetic therapy following highly emetogenic chemotherapy. "Helsinn is delighted with the FDA approval of AKYNZEO and we look forward to a successful launch in the United States. We are proud of our long-standing partnership with Eisai and AKYNZEO is the newest development in our combined efforts," said Riccardo Braglia, Helsinn's Group Chief Executive Officer. "This approval offers patients access to a new treatment option for CINV prevention that is effective in preventing both nausea and vomiting, particularly in the delayed phase, following emetogenic chemotherapy regimens." "The approval of AKYNZEO represents an important development in the prevention of acute and delayed nausea and vomiting for patients," said Yuji Matsue, Chairman and Chief Executive Officer, Eisai Inc. "We are proud to achieve this milestone with AKYNZEO as we work to further our human health care mission to provide patients going through what we know can be emotionally- and physically-demanding cancer treatment with an additional option for CINV prevention." About the AKYNZEO® (netupitant/palonosetron) Pivotal Clinical Trials The efficacy of AKYNZEO was established in a pivotal, Phase 2, randomized, double-blind, dose-ranging study in 694 patients undergoing cisplatin-based chemotherapy for a variety of tumor types. The efficacy of AKYNZEO was assessed in 135 chemotherapy-naive patients who received AKYNZEO (netupitant 300 mg/palonosetron 0.5 mg), and 136 patients who received oral palonosetron 0.5 mg. For the key efficacy endpoints of complete response (CR), defined as no emetic episode and no use of rescue medication, for the delayed phase (25-120 hour interval), the acute phase (0-24 hour interval), and the overall phase (0-120 hours) after the start of chemotherapy administration, AKYNZEO showed significantly higher complete response rates compared with oral palonosetron in all phases (90.4% versus 80.1%; P=0.032; 98.5% versus 89.7%; P=0.002; 89.6% versus 76.5%; P=0.003, respectively). The clinical efficacy profile was further established in a multinational, randomized, double-blind, parallel-group, Phase 3 study in 1455 chemotherapy-naive patients receiving anthracycline and cyclophosphamide-based chemotherapy. Patients were randomized to receive a single oral dose of either AKYNZEO plus dexamethasone or palonosetron plus dexamethasone prior to chemotherapy. The percentage of patients who met the primary endpoint of CR in the delayed phase was significantly higher in the AKYNZEO group compared to the oral palonosetron group (76.9% versus 69.5%; P = 0.001), which was also seen in the overall (74.3% versus 66.6%; P = 0.001) and acute (88.4% versus 85.0%; P = 0.047) phases post chemotherapy. In this study, AKYNZEO was generally well tolerated with a safety profile similar to that of palonosetron. In a separate study, 309 patients undergoing initial and repeat cycles of chemotherapy (including carboplatin, cisplatin, oxaliplatin, and doxorubicin regimens) received AKYNZEO; efficacy was maintained throughout all cycles. About AKYNZEO® (netupitant/palonosetron) AKYNZEO is an oral, fixed combination of an NK1 receptor antagonist, netupitant, and a 5-HT3 receptor antagonist, palonosetron, that targets two critical signaling pathways associated with chemotherapy-induced nausea and vomiting (CINV). Additional regulatory submissions for netupitant/palonosetron fixed combination are underway worldwide. On January 22, 2014, the European Medicines Agency (EMA) started to review the submission of Helsinn's Marketing Authorization Application for netupitant/palonosetron fixed combination for the prevention of acute and delayed CINV. AKYNZEO Important Safety Information Warning and Precautions •Hypersensitivity reactions, including anaphylaxis, have been reported with or without known hypersensitivity to other 5-HT3 receptor antagonists •Serotonin syndrome has been reported with 5-HT3 receptor antagonists alone but particularly with the use of serotonergic drugs. Symptoms associated with serotonin syndrome may include the following combination of signs and symptoms: mental status changes, autonomic instability, neuromuscular symptoms, seizures, and gastrointestinal symptoms. Patients should be monitored for the emergence of serotonin syndrome, and if symptoms occur, discontinue AKYNZEO and initiate supportive treatment Adverse Reactions •Most common adverse reactions (greater than or equal to 3% and greater than palonosetron): headache, asthenia, dyspepsia, fatigue, constipation and erythema Drug Interactions •Use with caution in patients receiving concomitant medications primarily metabolized by CYP3A4. The inhibitory effect on CYP3A4 can last for multiple days ◦Dexamethasone doses should be reduced when given with AKYNZEO ◦Consider the potential effects of increased plasma concentrations of midazolam or other benzodiazepines metabolized via CYP3A4 (alprazolam, triazolam) when administering with AKYNZEO ◦Caution and monitoring for chemotherapy-related adverse events are advised in patients receiving chemotherapy agents metabolized primarily by CYP3A4 including docetaxel, paclitaxel, etoposide, irinotecan, cyclophosphamide, ifosfamide, imatinib, vinorelbine, vinblastine, and vincristine ◦Avoid concomitant use of AKYNZEO in patients on chronic use of a strong CYP3A4 inducer such as rifampin as this may decrease the efficacy of AKYNZEO Use in Specific Populations •Avoid use of AKYNZEO in patients with severe hepatic impairment, severe renal impairment, or end stage renal disease AKYNZEO is available by prescription only. For more information about AKYNZEO, click here for the full Product Information or visit www.AKYNZEO.com. About Helsinn and Eisai Helsinn signed a licensing agreement with Eisai Inc. granting Eisai commercial rights for AKYNZEO in the United States.  Under the terms of the agreement, Helsinn is responsible for conducting all development activities (Chemistry and Manufacturing Controls [CMC], preclinical and clinical), obtaining regulatory approvals and holding the New Drug Application (NDA). AKYNZEO will be co-promoted in the United States by Eisai Inc. and Helsinn Therapeutics U.S. Inc., the U.S. subsidiary of Helsinn. About the Helsinn Group Helsinn is a family run, privately owned pharmaceutical group focused on building quality cancer care with a large portfolio of products. Founded in 1976 with headquarters in Lugano, Switzerland, Helsinn also has operating subsidiaries in Ireland, the U.S. and a representative office in China. Helsinn's business model is focused on the licensing of pharmaceuticals, medical devices and nutritional supplement products in the therapeutic area of cancer care. Helsinn Group in-licenses early-to-late stage new chemical entities, completing their development by performing preclinical and clinical studies and associated manufacturing activities. Helsinn then prepares necessary regulatory filings in order to achieve marketing approvals worldwide. Helsinn's products are out-licensed to its global network of marketing and commercial partners that have been selected for their local market knowledge. Helsinn supports these partners by providing a full range of product and scientific management services, including commercial, regulatory, and medical marketing advice. In March 2013, Helsinn established a new commercial organization within its subsidiary, Helsinn Therapeutics (U.S.), Inc., in order to conduct direct sales and marketing activities within the U.S. market. Helsinn's products are manufactured according to the highest quality, safety, and environmental standards at Helsinn's GMP facilities in Switzerland and Ireland from where they are then supplied worldwide to customers. Further information on Helsinn Group is available at www.helsinn.com. About Eisai Inc. At Eisai Inc., human health care is our goal. We give our first thoughts to patients and their families, and helping to increase the benefits health care provides. As the U.S. pharmaceutical subsidiary of Tokyo-based Eisai Co., Ltd., we have a passionate commitment to patient care that is the driving force behind our efforts to help address unmet medical needs. We are a fully integrated pharmaceutical business with discovery, clinical, manufacturing and marketing capabilities. Our key areas of commercial focus include oncology and specialty care (Alzheimer's disease, epilepsy and metabolic disorders). To learn more about Eisai Inc., please visit us at www.eisai.com/US.  Eisai Inc. has affiliates that are part of a global product creation organization that includes R&D facilities in Massachusetts, New Jersey, North Carolina and Pennsylvania, as well as a global demand chain organization that includes manufacturing facilities in Maryland and North Carolina. Eisai's global areas of R&D focus include neuroscience; oncology; metabolic disorders; vascular, inflammatory and immunological reaction; and antibody-based programs.