弃了！百时美施贵宝终止KRAS G12D项目

新浪财经2025-03-07

2025年3月5日，据外媒消息，百时美施贵宝（BMS）已放弃了此前收购的KRAS G12D抑制剂MRTX1133项目。在肿瘤治疗领域，KRAS G12D抑制剂一直是研究的热点。KRAS G12D是一种在多种癌症中常见的突变类型，尤其在胰腺癌中，约80%的患者存在KRAS突变，且大部分为G12D突变。这使得KRAS G12D成为胰腺癌治疗中一个十分有前景的治疗靶点。寄予厚望的KRAS项目此前被...

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Bristol-Myers Squibb terminates KRAS G12D project","themeId":null,"isJumpTheme":false,"ttsUrl":null,"symbols_score_info":{"BMY":1},"content_text":"2025年3月5日，据外媒消息， 百时美施贵宝 （BMS）已放弃了此前收购的KRAS G12D抑制剂MRTX1133项目。在肿瘤治疗领域，KRAS G12D抑制剂一直是研究的热点。KRAS G12D是一种在多种癌症中常见的突变类型，尤其在胰腺癌中，约80%的患者存在KRAS突变，且大部分为G12D突变。这使得KRAS G12D成为胰腺癌治疗中一个十分有前景的治疗靶点。寄予厚望的KRAS项目此前被百时美施贵宝看中的MRTX1133，就是一种有效的、选择性的和非共价的KRAS G12D抑制剂，目前处于I期临床阶段。2023年10月8日，BMS与Mirati Therapeutics宣布达成合并协议。BMS以每股58.00美元现金收购Mirati，股权价值高达48亿美元。此外，Mirati 股东还能获得一份或有价值权（CVR），每股有望额外获得12.00美元现金，总价值约10亿美元。此次收购Mirati公司，BMS意图强化自身肿瘤学产品组合，布局晚期KRAS项目。而Mirati正好是KRAS领域的明星公司，其研发的KRAS G12C抑制剂阿达格拉西（adagrasib，商品名 Krazati）备受关注。同时，Mirati还拥有处于早期临床阶段的KRAS G12D小分子抑制剂 MRTX1133、选择性SOS1抑制剂MRTX0902、首创MTA协同PRMT5抑制剂MRTX1719等资产。BMS此次收购，无疑是想借助Mirati的研发成果，在竞争激烈的肿瘤药物市场中抢占先机，尤其是在KRAS这个极具潜力的靶点赛道上，分得一杯羹。试验数据“泼冷水”此次，放弃KRAS G12D抑制剂MRTX1133研发项目。据BMS发言人透露，一个重要原因是其药代动力学数据“高度可变且不理想”。以MRTX1133为例，其口服生物利用度极低，尽管通过制剂手段实现了口服给药，但生物利用度提升效果不佳，仍有很大的优化空间。这就好比一辆汽车，动力系统不稳定，行驶过程中时快时慢，无法保证稳定、高效的运行。药物在体内的吸收、分布、代谢和排泄过程受到严重影响，进而极大地削弱了药效，使得该项目在研发道路上举步维艰。并且临床研究结果也泼了一盆“冷水”。原本预计在2024年上半年公布的G12D项目数据并未如期而至。MRTX1133的1/2期研究在2025年1月完成1期后，便悄然终止。这一情况充分表明，该项目在临床研究过程中遭遇了重大阻碍，未达到预期的效果。在竞争激烈的医药研发领域，时间就是生命，每一次延误都可能让竞争对手抢占先机。而且，临床研究结果不理想，也让BMS对该项目的未来发展前景失去了信心，最终选择放弃。值得关注的是，BMS收购Mirati时，重点关注的其实是KRAS G12C抑制剂Krazati，MRTX1133更多是作为附加收获纳入麾下。然而，Krazati在市场上的表现却不尽如人意，2024年销售额仅为1.18亿美元，远未达到预期。这一结果让BMS重新审视在KRAS相关项目上的资源分配策略，决定将资源集中投入到更具潜力或战略核心的产品研发中。KRAS G12D项目在这样的背景下，成为了被舍弃的对象，资源被重新调配，用于支持更有希望的研发方向。同时，KRAS G12C抑制剂赛道的整体表现，给KRAS相关靶点的研发前景蒙上了一层阴影。已上市的两款KRAS G12C抑制剂， 安进 的Lumakras销售额未达华尔街分析师预期，且在FDA的ODAC会议上未通过评估；Mirati的Adgrasib单药临床试验数据不够惊艳，联合疗法进展也不顺利，还被欧盟拒绝上市申请。这些负面消息让BMS对同为KRAS靶点的G12D项目未来的市场竞争力和商业前景深感担忧。在市场竞争日益激烈、研发风险不断攀升的情况下，BMS选择及时止损，放弃KRAS G12D项目来降低潜在风险，也十分可以理解。BMS放弃KRAS G12D项目，是多种因素 综合 作用的结果。这一决策不仅反映了医药研发的复杂性和高风险性，也为整个行业敲响了警钟。在追求 创新药 物的道路上，药企需要不断权衡利弊，做出艰难的抉择。","kind":"news","is_publish_news":true,"is_publish_highlight":false,"is_publish_live":false,"is_publish_wemedia":null,"editions":null,"column":"","sentiment":"-1","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 AppleWebKit/537.36 (KHTML, like Gecko; compatible; ClaudeBot/1.0; +claudebot@anthropic.com)","isDev":false,"isTTM":false,"tenantId":"TBCN","deviceId":"web-server-community-laohu8-v3","version":"4.36.2","shortVersion":"4.36.2","platform":"web","vendor":"web","appName":"laohu8","isIOS":false,"isAndroid":false,"isTiger":false,"isTHS":false,"isWeiXin":false,"isWeiXinMini":false,"isWeiBo":false,"isQQ":false,"isBaiduSwan":false,"isBaiduBox":false,"isDingTalk":false,"isToutiao":false,"isOnePlus":false,"isHuaWei":false,"isXiaomi":false,"isXiaomiWebView":false,"isOppo":false,"isVivo":false,"isSamsung":false,"isMobile":false},"href":"/m/news/2517124356","isCrawlerRequest":true}