Drugs R D. 2003;4(4):254-7. doi: 10.2165/00126839-200304040-00008.
NXY 059 [CPI 22, NXY 059G], a nitrone with free radical trapping properties, has potential in the treatment of ischaemic stroke.This profile has been selected from R&D Insight, a pharmaceutical intelligence database produced by Adis International Ltd. NXY 059 is based on Centaur Pharmaceuticals' proprietary Nitrone-Related Therapeutics (NRT) technology. A generic form of NXY 059, NXY 059G, has been synthesised. On 12 December 2002, Centaur Pharmaceuticals was acquired by, and integrated into, Renovis. AstraZeneca has exclusive worldwide rights to NXY 059, under a licence from Centaur Pharmaceuticals; the licensing agreement is continuing with Renovis. Renovis will receive a significant milestone payment and retains a co-promotion option for NXY 059 in the US. In addition, Renovis is entitled to royalties on profits from worldwide sales of the drug once commercialised. Centaur received a cash payment of $US1.25 million, and up to 30% of Renovis stock in exchange for these assets. In May 2003, AstraZeneca announced the initiation of two major phase III pivotal clinical trials to determine the effect of NXY 059 on disability and neurological recovery in acute ischemic stroke patients. The trials, known as the SAINT (Stroke-Acute-Ischaemic-NXY-Treatment) trials, will compare the efficacy and safety of a 72-hour intravenous infusion of NXY 059 given within 6 hours of the onset of symptoms vs placebo. The studies will enrol >3000 patients. The SAINT I trial will involve 200 centres across 24 countries in Europe, Asia, Australia and South Africa. The SAINT II trial will involve patients from approximately 150 sites in the US, Canada and South America. AstraZeneca is evaluating NXY 059 in a phase I clinical study in the US. Phase III trials of NXY 059 have begun in the UK and Sweden for the treatment of stroke. In November 2000, Centaur Pharmaceuticals announced that the Japanese regulatory authorities approved AstraZeneca's regulatory filings for phase I clinical studies of NXY 059 in Japan. The purpose of these studies is to investigate the safety and tolerability of 8h and 24h IV infusions of NXY 059 in 56 healthy Japanese male subjects. A secondary objective will be to evaluate the pharmacokinetics of NXY 059 in these volunteers.
NXY 059 [CPI 22, NXY 059G]是一种具有自由基捕获特性的硝酮，在缺血性中风治疗方面具有潜力。此简介摘自研发洞察，这是阿迪斯国际有限公司制作的一个制药情报数据库。NXY 059基于半人马制药公司的专有硝酮相关治疗（NRT）技术。已合成了NXY 059的通用形式NXY 059G。2002年12月12日，半人马制药公司被雷诺维斯收购并并入其中。阿斯利康根据与半人马制药公司的许可协议，在全球范围内拥有NXY 059的独家权利；许可协议继续与雷诺维斯生效。雷诺维斯将获得一笔重要的里程碑付款，并保留在美国对NXY 059的联合推广选择权。此外，一旦该药物商业化，雷诺维斯有权从其全球销售利润中获得版税。半人马公司获得了125万美元的现金付款以及雷诺维斯高达30%的股票，以换取这些资产。2003年5月，阿斯利康宣布启动两项主要的III期关键临床试验，以确定NXY 059对急性缺血性中风患者残疾和神经恢复的影响。这些试验被称为SAINT（中风 - 急性 - 缺血性 - NXY - 治疗）试验，将比较在症状发作6小时内静脉输注72小时的NXY 059与安慰剂的疗效和安全性。这些研究将招募超过3000名患者。SAINT I试验将涉及欧洲、亚洲、澳大利亚和南非24个国家的200个中心。SAINT II试验将涉及来自美国、加拿大和南美洲约150个地点的患者。阿斯利康正在美国进行一项I期临床研究以评估NXY 059。NXY 059的III期试验已在英国和瑞典启动用于中风治疗。2000年11月，半人马制药公司宣布日本监管当局批准了阿斯利康在日本进行NXY 059 I期临床研究的监管申报。这些研究的目的是调查在56名健康日本男性受试者中静脉输注8小时和24小时NXY 059的安全性和耐受性。次要目标将是评估这些志愿者中NXY 059的药代动力学。
