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默沙东4亿3千万美元加盟Arvinas抢占蛋白药物开发新制高点

  1. Arvinas
  2. PROTAC
  3. 蛋白水解途径
  4. 默沙东

来源:生物谷 2015-04-08 16:52

随着生物技术的发展,人类的药物开发早已不仅局限于化学药物。人体内成千上万种蛋白为科学家开发新药物提供了丰富的靶点库。不过,迄今为止研究人员在开发蛋白类药物时的思路仍主要是通过抗体和化学小分子阻断或是刺激相应的蛋白质靶点。有研究人员指出,在目前常用的20000种蛋白药物靶点中,只有不到四分之一能够使用这一策略。因此,开发新的蛋白质药物技术已经成为生物医药巨头竞相参与的一个热点。

2015年4月8日讯 /生物谷BIOON/ --随着生物技术的发展,人类的药物开发早已不仅局限于化学药物。人体内成千上万种蛋白为科学家开发新药物提供了丰富的靶点库。不过,迄今为止研究人员在开发蛋白类药物时的思路仍主要是通过抗体和化学小分子阻断或是刺激相应的蛋白质靶点。有研究人员指出,在目前常用的20000种蛋白药物靶点中,只有不到四分之一能够使用这一策略。因此,开发新的蛋白质药物技术已经成为生物医药巨头竞相参与的一个热点。

最近,默沙东公司宣布和著名药物生产商Arvinas公司签订了一项价值4亿3千4百万美元的合作研发协议,旨在抢占这一领域的制高点。Arvinas公司独有的蛋白水解靶向嵌合体技术(PROTAC)可以通过激活细胞内部的蛋白降解途径定向降解某些”不“受欢迎”的蛋白质,从而将一个个细胞转变为药物单位。这一思路将有望在未来的蛋白质药物研发中大显身手。

根据合约规定,默沙东公司将向Arvinas公司支付包括预付款、研究经费以及相应的里程碑资金在内的共计4亿3千4百万美元的经费,作为回报,默沙东公司将获得PROTAC这一极具前景的新技术。不过合约双方并未透露此次研究涉及的靶点。

成立于2013年的Arvinas公司由于其PROTAC技术而迅速为业内所熟知,公司的这项技术来源于耶鲁大学Craig Crews教授的实验室。公司CEO Manny Litchman称此次合作为Arvinas公司进一步明确自己未来定位起到了重要作用,而他也相信公司的PROTAC技术将成为未来默沙东药物开发系统中的一个重要卖点。目前公司正在利用这一技术开发相应的肿瘤治疗方案,公司希望于明年年中向FDA申报这一治疗方案。(生物谷Bioon.com)

详细英文报道:

Merck ($MRK) has partnered up with fast-moving upstart Arvinas to get its hands on technology that promises to give drug developers a crack at some previously untouchable targets, using the body's natural garbage system to dump troublesome proteins.

Under the deal, Merck will hand the New Haven, CT, biotech an up-front payment and research funding, promising more cash tied to development milestones and setting Arvinas' maximum haul at $434 million if everything works out over the multiyear agreement. In exchange, Merck will get a chance to use the company's proteolysis-targeting chimera, or PROTAC, technology, which creates small-molecule treatments that mark proteins for degradation.

Based on work out of Craig Crews' Yale University labs, PROTAC treatments are designed to get rid of unwanted proteins by triggering a cell's natural clean-up system, marking targets for removal and letting the body's degradation mechanisms do the rest. Arvinas, launched in 2013, has largely focused its internal efforts on oncology, but the Merck deal spans multiple disease targets in an undisclosed array of therapeutic areas, the company said.

The majority of protein-targeting therapeutics in the market or in development work by either inhibiting or boosting their targets, whether via antibodies or small-molecule chemicals. But only about a quarter of the body's roughly 20,000 proteins can be effectively drugged that way, Arvinas CEO Manny Litchman said. By attacking proteins from within their home cells, however, Arvinas' technology can potentially open up new avenues of therapeutic development, he said, exposing some long-untouchable targets to guided degradation.

That potential was a major selling point for Merck, Litchman said, and now it's on Arvinas to demonstrate that its technology can come through in the proof-of-concept stage, rolling into what the CEO expects to be "a true collaboration." Merck has the option to expand the deal to include more disease targets, triggering an undisclosed payment, and Litchman believes the agreement could create a model for Arvinas' future partnerships.

The company has held onto a host of internal programs also based on PROTAC, including a lead oncology asset Arvinas expects to get into the clinic in the middle of next year. The biotech will likely look to ink one or two more deals along the way, Litchman said, at once cautious not to spread itself too thin and optimistic that Merck's big co-sign will help it bring would-be partners to the table.

"I think when a company like Merck has done deep due diligence, surveyed the competitive landscape and selected Arvinas as the best platform out there for protein degradation, that's a signal for others we've talked to that perhaps a deeper dive may be warranted," Litchman said.

Arvinas got rolling with a $15 million A round from Canaan Partners and 5AM Ventures, licensing Crews' technology and assembling a team of investigators to push it forward. The biotech quickly moved to establish preclinical proof of concept for PROTAC, recruiting Litchman, an 18-year Novartis ($NVS) veteran, in time to start showing off the platform at January's JP Morgan Healthcare conference.

 

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