20亿美元，石药AI设计的Lp(a)分子长啥样？

Ofweek光电信息网2025-07-04

前情回顾2024年10月7日，阿斯利康与石药集团达成总额20.2亿美元的独家授权协议：阿斯利康获得石药临床前口服Lp(a)抑制剂YS2302018的全球开发权（石药宣称该药通过AI驱动平台发现），临床前数据显示该药物可有效阻断Lp(a)形成；未来拟与阿斯利康口服PCSK9抑制剂AZD0780联用。石药集团保留中国权益，并收取1亿美元首付款及最高19.2亿美元里程碑款项。言归正传时隔半年之久，石药...

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like?","themeId":null,"isJumpTheme":false,"ttsUrl":null,"symbols_score_info":{"01093":1},"content_text":"前情回顾2024年10月7日，阿斯利康与石药集团达成总额20.2亿美元的独家授权协议：阿斯利康获得石药临床前口服Lp(a)抑制剂YS2302018的全球开发权（石药宣称该药通过AI驱动平台发现），临床前数据显示该药物可有效阻断Lp(a)形成；未来拟与阿斯利康口服PCSK9抑制剂AZD0780联用。石药集团保留中国权益，并收取1亿美元首付款及最高19.2亿美元里程碑款项。言归正传时隔半年之久，石药专利终于于5月22日公开。今天我们来看看，这个AI发现的Lp(a)分子究竟长啥样？专利说明书公开了系列取代的2-(吡咯烷-3-基)乙酸的衍生物及相关活性数据，根通过数据，我们很容易就可以将目标锁定到各方面均具有突出表现的Cpd.96（极有可能是石药的PCC分子）。值得注意的是，专利权利要求书中排除了拓界（Ex.6，WO2023078333）和京新（Ex.5，WO2024199070）的化合物，具体分析可见【20.2亿美元交易加持！Lp(a)小分子新玩家有哪些？】。仔细对比，不难发现，Cpd.96比拓界的化合物仅多了个羰基，其余化合物也是大差不差，无外乎是多个甲基、羰基、酰胺或在苯环上做了些文章，但均不免让人产生莞莞类卿之感。石药的这一操作仿佛是为其官方宣称的“AI驱动平台发现”做了最生动的注脚——AI平台，果然深谙“针对性优化”之道！它精准地“分析目标蛋白与现有化合物分子的结合模式”，并高效地“筛选”出了在已知有效骨架上进行最小修饰便能提升活性的关键位点。如此“优化”出的分子，自然能在临床前数据中展现出“优异”的PK/PD和“更佳”疗效。从法律角度看，专利排他条款确保了其新颖性；从化学角度看，这波操作堪称“高效”利用AI进行分子“微整形”的典范。只是，“发现”二字的光芒，在竞品分子清晰投下的影子中，似乎带上了一丝“优化性借鉴”的赛博滤镜。这颗由AI“发现”并“优化”的果实，也最终以20.2亿美元的价格找到了它的“优良开发性”归宿，实乃AI赋能药物研发的“高效”明证——毕竟，能在巨人的肩膀上如此精准地“点石成金”，怎么不算是一种“发现”呢？最后，关于礼来Lp(a)分子设计思路可见【Nature:多价策略制胜!礼来全球首个Lp(a)小分子设计思路深度剖析】","kind":"news","is_publish_news":true,"is_publish_highlight":false,"is_publish_live":false,"is_publish_wemedia":null,"editions":null,"column":"","sentiment":"0","news_tag":"","news_rank":0,"symbols":[],"gpt_button":1,"need_auth":false,"code":"91000000","status":"200"},"commentList":[],"isCommentEnd":true,"newsSizeData":{"likeSize":0,"commentSize":0,"repostSize":0,"favoriteSize":0,"likeStatus":false,"favoriteStatus":false},"APP":{"userAgent":"Mozilla/5.0 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