2014年10月20日讯 /生物谷BIOON/ --在研发新一类降脂药物——PCSK9抑制剂竞赛中，赛诺菲和合作伙伴Regeneron制药已与竞争对手安进（Amgen）齐头并进。然而，该领域再掀波澜！近日，安进（Amgen）在美国特拉华地方法院起诉赛诺菲（Sanofi）和Regeneron专利侵权，称其PCSK9单抗药物alirocumab侵犯了安进有关PCSK9单抗的3个美国专利（专利号：8563698、8829165、8859741），这些专利描述并声明了对“前蛋白转化酶枯草溶菌素9（PCSK9）单克隆抗体”的权利要求。
通过此次诉讼，安进将寻求禁止令，阻止赛诺菲和Regeneron非法生产、使用、销售PCSK9抑制剂alirocumab。业界认为，安进此举意在阻止竞争对手进入PCSK9药物领域。赛诺菲周五早上未立即置评。
PCSK9抑制剂市场高达100亿美元，而在这场竞赛中，安进早已一马当先，志在率先撬开该市场，并已于2014年8月28日向FDA提交了PCSK9抑制剂evolocumab的生物制品许可申请（BLA）。不过，赛诺菲和Regeneron在今年夏天干了一件有意思的事，耗资6750万美元购买了一张加速审评券，意在将alirocumab的审查时间从常规的10个月缩短至6个月。通过此举，赛诺菲拉平了与安进的差距。
赛诺菲和Regeneron近日宣布，已完成alirocumab的III期临床试验，并计划向FDA提交alirocumab的上市申请。而有了加速审评券，也意味着安进的evolocumab和赛诺菲的alirocumab，这2种药物都将于2015年6月获批。
PCSK9抑制剂，这是一类单抗药物，开发用于高血脂的治疗，该类药物的标靶为PCSK9蛋白，该蛋白会增加低密度脂蛋白胆固醇（LDL-C）的生成率，而LDL-C可阻塞血管，是心脏病的罪魁祸首。PCSK9抑制剂提供了一种全新的治疗模式来对抗低密度脂蛋白胆固醇（LDL-C），该类药物被视为自他汀类药物（如Lipitor和Zocor）之后，在对抗心脏疾病研发领域中所取得的最大进步。
目前，在PCSK9研发狂潮中，安进的evolocumab和赛诺菲和Regeneron的alirocumab处于领先地位，辉瑞bococizumab（RN316）稍微落后，而诺华、罗氏、默沙东则相对落后，正在努力追赶。目前为止，几乎所有公布的III期临床数据都是积极的，疗效也接近，因此，上市次序可能是个决定因素，谁的产品能率先撬开PCSK9市场，就有望夺取最大的市场份额。
英文原文：Amgen sues to block Sanofi and Regeneron at the PCSK9 goal line
Sanofi ($SNY) and Regeneron ($REGN) have cut to the front of the line in the race to develop a new class of cardio drugs, but now rival Amgen ($AMGN) has made a chess move of its own, filing a patent-infringement lawsuit designed to block its rivals from reaching what's expected to be a blockbuster market.
Amgen's lawsuit claims that Sanofi and Regeneron stepped on its intellectual property in crafting an antibody that blocks the protein PCSK9, thereby helping the body clear LDL cholesterol from the blood. The three patents in question apply to antibodies to PCSK9, including Amgen own evolocumab, and the lawsuit seeks to prevent the manufacture, use and sale of Sanofi and Regeneron's similar alirocumab.
Sanofi didn't respond to a request for comment Friday morning.
The lawsuit is the latest development in an increasingly contentious race between the companies, which are angling for first place in a potential $10 billion market for new cholesterol-lowering drugs. Amgen has long led the way, filing evolocumab for approval in August with eyes on a 2015 launch.
But Sanofi and Regeneron made things interesting over the summer when they paid $67.5 million for an FDA voucher that will cut alirocumab's review time down from 10 months to 6 months. The two plan to submit their treatment by year's end, which would put both drugs up for approval next June.
Bringing up the rear in the PCSK9 race is Pfizer ($PFE), which is in the midst of a sweeping Phase III program to demonstrate that its bococizumab can significantly slash rates of bad cholesterol.