{"id":2249,"date":"2026-10-23T15:23:53","date_gmt":"2026-10-23T07:23:53","guid":{"rendered":"https:\/\/www.millibuff.com\/?p=2249"},"modified":"2026-10-23T15:26:40","modified_gmt":"2026-10-23T07:26:40","slug":"%e5%b0%8f%e7%89%9b%e6%b4%9e%e5%af%9f-riptac%ef%bc%9a%e8%af%b1%e5%af%bc%e9%82%bb%e8%bf%91%e6%96%b0%e5%88%86%e5%ad%90%ef%bc%8c%e4%b8%ba%e6%99%9a%e6%9c%9f%e5%89%8d%e5%88%97%e8%85%ba%e7%99%8c%e5%bc%80","status":"publish","type":"post","link":"https:\/\/www.millibuff.com\/?p=2249","title":{"rendered":"\u5c0f\u725b\u6d1e\u5bdf | RIPTAC\uff1a\u8bf1\u5bfc\u90bb\u8fd1\u65b0\u5206\u5b50\uff0c\u4e3a\u665a\u671f\u524d\u5217\u817a\u764c\u5f00\u8f9f\u5168\u65b0\u6740\u4f24\u8def\u5f84"},"content":{"rendered":"\n
\u4e00\u3001RIPTAC\u7684\u8d77\u6e90\u4e0e\u6982\u5ff5\u8bde\u751f<\/strong><\/h5>\n\n\n\n

RIPTAC<\/strong>\u5168\u79f0Regulated Induced Proximity Targeting Chimera\uff0c\u8c03\u63a7\u8bf1\u5bfc\u90bb\u8fd1\u9776\u5411\u5d4c\u5408\u4f53<\/strong>\uff0cRIPTAC\u2122\u662fHalda Therapeutics\u6301\u6709\u7684\u6ce8\u518c\u5546\u6807\u3002\u8fd9\u9879\u6280\u672f\u8bde\u751f\u4e8e\u8036\u9c81\u5927\u5b66Craig Crews\u5b9e\u9a8c\u5ba4\uff0c\u800cCrews\u6559\u6388\u6b63\u662fPROTAC\u9886\u57df\u7684\u5960\u57fa\u4eba\u3002\u6709\u610f\u601d\u7684\u662f\uff0c\u5728PROTAC\u4e0d\u65ad\u8d70\u5411\u4e34\u5e8a\u7684\u540c\u65f6\uff0c\u4ed6\u7684\u56e2\u961f\u5f00\u8f9f\u4e86\u4e00\u6761\u5b8c\u5168\u4e0d\u540c\u7684\u8bf1\u5bfc\u90bb\u8fd1\u6280\u672f\u8def\u7ebf[1]<\/sup>\u3002<\/p>\n\n\n\n

\u4f20\u7edf\u5c0f\u5206\u5b50\u836f\u7269\uff0c\u601d\u8def\u5927\u591a\u662f\u6291\u5236\u9776\u86cb\u767d\u6d3b\u6027\uff1bPROTAC\u5219\u66f4\u8fdb\u4e00\u6b65\uff0c\u62db\u52df\u7ec6\u80de\u5185E3\u6cdb\u7d20\u8fde\u63a5\u9176\uff0c\u628a\u81f4\u75c5\u9776\u86cb\u767d\u76f4\u63a5\u964d\u89e3\u3002\u4f46\u8fd9\u4e24\u79cd\u7b56\u7565\uff0c\u90fd\u9762\u4e34\u65e0\u6cd5\u56de\u907f\u7684\u8010\u836f\u74f6\u9888\u3002\u5728\u524d\u5217\u817a\u764c\u9886\u57df\uff0cNHT\u8010\u836f\u3001AR\u526a\u63a5\u53d8\u5f02\u4f53\u3001AR\u70b9\u7a81\u53d8\uff0c\u751a\u81f3\u90e8\u5206AR-PROTAC\u5bf9\u7f3a\u5931\u914d\u4f53\u7ed3\u5408\u57df\uff08LBD\uff09\u7684AR\u53d8\u4f53\u5931\u6548\uff0c\u90fd\u9650\u5236\u4e86\u7597\u6cd5\u7684\u9002\u7528\u8fb9\u754c\u3002<\/p>\n\n\n\n

RIPTAC\u7684\u8bbe\u8ba1\u521d\u8877\uff0c\u5c31\u662f\u8df3\u51fa\u201c\u6291\u5236\u9776\u86cb\u767d\u201d\u6216\u201c\u964d\u89e3\u9776\u86cb\u767d\u201d\u7684\u56fa\u6709\u601d\u7ef4\u3002\u6838\u5fc3\u60f3\u6cd5\u4e0d\u518d\u662f\u6d88\u706d\u80bf\u7624\u9776\u70b9\u672c\u8eab\uff0c\u800c\u662f\u5229\u7528\u80bf\u7624\u7279\u5f02\u6027\u86cb\u767d\u4f5c\u4e3a\u5206\u5b50\u951a\u5b9a\u652f\u67b6\uff0c\u628a\u7ec6\u80de\u751f\u5b58\u5fc5\u9700\u86cb\u767d\u201c\u631f\u6301\u201d\uff0c\u4ece\u800c\u9009\u62e9\u6027\u6740\u6b7b\u764c\u7ec6\u80de<\/strong>\u3002\u7b80\u5355\u4e00\u53e5\u8bdd\u533a\u5206\uff1aPROTAC\u964d\u89e3\u9776\u86cb\u767d\uff1bRIPTAC\u52ab\u6301\u80bf\u7624\u951a\u5b9a\u86cb\u767d\uff0c\u706d\u6d3b\u764c\u7ec6\u80de\u5fc5\u9700\u86cb\u767d\uff0c\u5168\u7a0b\u4e0d\u964d\u89e3\u951a\u5b9a\u86cb\u767d\u3002<\/p>\n\n\n\n

\u4e8c\u3001RIPTAC\u5206\u5b50\u7ed3\u6784\u4e0e\u6838\u5fc3\u4f5c\u7528\u673a\u5236<\/strong><\/h5>\n\n\n\n

RIPTAC\u5c5e\u4e8e\u5f02\u53cc\u529f\u80fd\u5c0f\u5206\u5b50\uff08heterobifunctional molecules\uff09\uff0c\u5206\u5b50\u9aa8\u67b6\u7531\u4e09\u90e8\u5206\u62fc\u63a5\u800c\u6210\uff1a\u80bf\u7624\u7279\u5f02\u6027\u951a\u5b9a\u86cb\u767d\u914d\u4f53\uff08Target Protein, TP\u914d\u4f53\uff09+ \u8fde\u63a5\u5b50\uff08linker\uff09+ \u7ec6\u80de\u6548\u5e94\u86cb\u767d\u914d\u4f53\uff08Essential Protein, EP\u914d\u4f53\uff09<\/strong>\u3002TP\u5728\u764c\u7ec6\u80de\u4e2d\u7279\u5f02\u6027\u8868\u8fbe\uff0c\u800cEP\u5bf9\u7ec6\u80de\u751f\u5b58\u81f3\u5173\u91cd\u8981\u3002<\/p>\n\n\n\n

\u5b83\u7684\u6838\u5fc3\u5de5\u4f5c\u903b\u8f91\u88ab\u5b9a\u4e49\u4e3aHold and Kill<\/strong>\uff0c\u6293\u4f4f\u5e76\u6740\u6b7b<\/strong>\uff1aRIPTACs\u5728\u8868\u8fbe\u80bf\u7624\u7279\u5f02\u6027TP\u7684\u764c\u7ec6\u80de\u4e2d\u9009\u62e9\u6027\u79ef\u7d2f\uff0c\u5e76\u4e0eTP\u548cEP\u5f62\u6210\u7a33\u5b9a\u7684\u4e09\u5143\u590d\u5408\u7269\uff08TP\uff1aRIPTAC\uff1aEP\uff09\u3002\u8fd9\u79cd\u590d\u5408\u7269\u7684\u5f62\u6210\u589e\u5f3a\u4e86TP\u548cEP\u4e4b\u95f4\u7684\u86cb\u767d\u8d28-\u86cb\u767d\u8d28\u76f8\u4e92\u4f5c\u7528\uff08PPIs\uff09\uff0c\u4ece\u800c\u6291\u5236EP\u7684\u529f\u80fd\uff0c\u5bfc\u81f4\u764c\u7ec6\u80de\u7684\u9009\u62e9\u6027\u6b7b\u4ea1\uff0c\u800c\u5bf9\u975eTP\u8868\u8fbe\u7684\u5065\u5eb7\u7ec6\u80de\u65e0\u5f71\u54cd\u3002\u8fd9\u4e5f\u662fRIPTAC\u5b9e\u73b0\u80bf\u7624\u9009\u62e9\u6027\u7684\u5173\u952e\u3002\u6b63\u5e38\u4eba\u4f53\u7ec6\u80de\u4e0d\u8868\u8fbe\u80bf\u7624\u7279\u5f02\u6027\u951a\u5b9a\u86cb\u767dFL-AR\uff0c\u836f\u7269\u8fdb\u5165\u6b63\u5e38\u7ec6\u80de\u540e\uff0c\u65e0\u6cd5\u7ec4\u88c5\u5f62\u6210\u4e09\u5143\u590d\u5408\u7269\uff0c\u4e0d\u4f1a\u5e72\u6270\u6b63\u5e38\u7ec6\u80de\u5185BRD4\u529f\u80fd\u3002\u7406\u8bba\u4e0a\uff0c\u8fd9\u4e00\u673a\u5236\u53ef\u4ee5\u964d\u4f4eon-target off-tumor\uff08\u9776\u86cb\u767d\u4ecb\u5bfc\u7684\u8131\u7624\u6bd2\u6027\uff09\u98ce\u9669[2]<\/sup>\u3002<\/p>\n\n\n\n

\"\"<\/figure>\n\n\n\n

\u56fe1\uff1aRIPTAC\u4f5c\u7528\u673a\u5236\u539f\u7406\u56fe[2]<\/sup>\u3002<\/p>\n\n\n\n

\u4e09\u3001\u5168\u7403\u4e34\u5e8a\u4e0e\u4e34\u5e8a\u524d\u7ba1\u7ebf\u5168\u666f<\/strong><\/h5>\n\n\n\n

Halda Therapeutics\u662f\u4e00\u5bb6\u7531\u8036\u9c81\u5927\u5b66 Craig Crews \u6559\u6388\u4e8e2019\u5e74\u8054\u5408\u521b\u7acb\u7684\u4e34\u5e8a\u9636\u6bb5\u751f\u7269\u6280\u672f\u516c\u53f8\uff0c\u4e13\u6ce8\u4e8eRIPTAC\u6280\u672f\u7684\u4ea7\u4e1a\u5316\u5e94\u7528\u30022025\u5e7411\u6708\uff0c\u5f3a\u751f\u4ee530.5\u4ebf\u7f8e\u5143\u73b0\u91d1\u6536\u8d2dHalda Therapeutics\uff0c\u521b\u9020\u4e86\u5f53\u5e74\u751f\u7269\u6280\u672f\u9886\u57df\u7684\u91cd\u8981\u5e76\u8d2d\u6848\u4f8b\u3002<\/p>\n\n\n\n

Halda Therapeutics \u5728\u88ab\u5f3a\u751f\u6536\u8d2d\u524d\uff0c\u642d\u5efa\u4e86\u4e00\u5957\u4ee5 RIPTAC \u5e73\u53f0\u4e3a\u6838\u5fc3\u7684\u5206\u5b50\u7ba1\u7ebf\uff0c\u4f9d\u6258 \u201c\u80bf\u7624\u7279\u5f02\u6027\u951a\u5b9a\u86cb\u767d\uff08TP\uff09+ \u7ec6\u80de\u5fc5\u9700\u86cb\u767d\uff08EP\uff09\u201d \u7684\u7ec4\u5408\u601d\u8def\uff0c\u8986\u76d6\u524d\u5217\u817a\u764c\u3001\u4e73\u817a\u764c\u3001\u7a81\u53d8 p53 \u5b9e\u4f53\u7624\u7b49\u591a\u4e2a\u764c\u79cd\u3002\u5176\u4e2d\uff0cHLD-0915 \u662f Halda Therapeutics \u5f00\u53d1\u7684\u53e3\u670d first-in-class RIPTAC \u836f\u7269\uff0c\u7528\u4e8e\u6cbb\u7597\u8f6c\u79fb\u6027\u53bb\u52bf\u62b5\u6297\u6027\u524d\u5217\u817a\u764c\uff08mCRPC\uff09\u3002\u8be5\u5206\u5b50\u5728 RIPTAC \u9886\u57df\u5177\u6709\u91cc\u7a0b\u7891\u5730\u4f4d\u2014\u20142025 \u5e74 HLD-0915 \u5b8c\u6210\u9996\u4f8b\u60a3\u8005\u7ed9\u836f\uff0c\u6807\u5fd7\u7740\u8be5\u6280\u672f\u6b63\u5f0f\u4ece\u5b9e\u9a8c\u5ba4\u8d70\u5411\u4e34\u5e8a\u3002<\/p>\n\n\n\n

\u88681\uff1a\u5168\u7403 RIPTAC \u7ba1\u7ebf\u4e0d\u5b8c\u5168\u7edf\u8ba1\u76d8\u70b9<\/strong><\/h6>\n\n\n\n

\uff08\u6570\u636e\u6765\u6e90\uff1a\u533b\u836f\u9b54\u65b9 NextPharma \u53e3\u5f84\uff0c\u622a\u81f3 2026-09-21\uff09<\/p>\n\n\n\n

\u673a\u6784<\/strong><\/td>\u5206\u5b50 \/ \u516c\u5f00\u6807\u8bc6<\/strong><\/td>\u9776\u86cb\u767d\uff08TP\uff09<\/strong><\/td>\u6548\u5e94\u86cb\u767d\uff08EP\uff09<\/strong><\/td>\u5168\u7403\u6700\u9ad8\u9636\u6bb5<\/strong><\/td>\u6838\u5fc3\u4e13\u5229 \/ \u5907\u6ce8<\/strong><\/td><\/tr>
\u5f3a\u751f \/ Halda<\/td>HLD-0915\uff08JNJ-101556143\uff09<\/td>\u5168\u957f AR<\/td>BRD4<\/td>II \u671f\u4e34\u5e8a<\/td>WO2024054603\/04\u3001WO20205085738 \u7b49<\/td><\/tr>
\u5f3a\u751f \/ Halda<\/td>HLD-0117\uff08JNJ-4362\uff09<\/td>ER<\/td>BRD4<\/td>I \u671f\u4e34\u5e8a<\/td>WO2025189056A1<\/td><\/tr>
\u5f3a\u751f \/ Halda<\/td>\u4e13\u5229\u9879\u76ee<\/td>AR<\/td>PLK1<\/td>\u4e34\u5e8a\u524d<\/td>WO2024054952A1<\/td><\/tr>
\u5f3a\u751f \/ Halda<\/td>\u4e13\u5229\u9879\u76ee<\/td>AR<\/td>CDK9<\/td>\u4e34\u5e8a\u524d<\/td>WO2024054602A1<\/td><\/tr>
\u5f3a\u751f \/ Halda<\/td>\u4e13\u5229\u9879\u76ee<\/td>BCL6<\/td>BRD4<\/td>\u4e34\u5e8a\u524d<\/td>WO2024211684A1<\/td><\/tr>
\u5f3a\u751f \/ Halda<\/td>p53 Y220C \u9879\u76ee<\/td>p53 Y220C<\/td>\u672a\u516c\u5f00<\/td>\u4e34\u5e8a\u524d<\/td>AACR 2025 Poster LB428<\/td><\/tr>
Kolm\uff08\u7f57\u6c0f\u6536\u8d2d\uff09<\/td>\u4e13\u5229\u9879\u76ee<\/td>AR\/ER<\/td>CBP\/EP300<\/td>\u4e34\u5e8a\u524d<\/td>WO2025081091A1\u3001WO2025081082A1 \u7b49<\/td><\/tr>
Flare Therapeutics<\/td>ARON RIPTAC<\/td>\u8f6c\u5f55\u6d3b\u6027\u6784\u8c61 AR<\/td>\u672a\u516c\u5f00<\/td>\u4e34\u5e8a\u524d<\/td>2026 \u5e74 6 \u6708 Series C \u4e13\u9879\u63a8\u8fdb<\/td><\/tr>
Alaw\uff08Eilean\uff09<\/td>AL-060<\/td>\u672a\u516c\u5f00<\/td>\u672a\u516c\u5f00<\/td>\u4e34\u5e8a\u524d<\/td>\u2014<\/td><\/tr>
Alaw\uff08Eilean\uff09<\/td>AL-995<\/td>\u672a\u516c\u5f00<\/td>\u672a\u516c\u5f00<\/td>\u4e34\u5e8a\u524d<\/td>\u2014<\/td><\/tr>
\u827e\u65af\u9686\u533b\u836f<\/td>RIPTAC program<\/td>\u672a\u516c\u5f00<\/td>\u672a\u516c\u5f00<\/td>\u4e34\u5e8a\u524d<\/td>\u524d\u5217\u817a\u764c + \u4e73\u817a\u764c<\/td><\/tr>
\u6052\u745e\u533b\u836f<\/td>WO2026108978A1\uff08\u4e1a\u5185\u63a8\u6d4b\u5bf9\u5e94 SHR-7525\uff09<\/td>AR<\/td>\u672a\u5b98\u65b9\u62ab\u9732<\/td>\u4e34\u5e8a\u524d\uff08\u7ba1\u7ebf\u63a8\u6d4b\u5bf9\u5e94 I \u671f\uff09<\/td>WO2026108978A1\u3001WO2026153393A1<\/td><\/tr>
\u4e1c\u9633\u5149 \/ Accutar<\/td>RIPTAC program<\/td>\u672a\u516c\u5f00\uff08\u9996\u53d1 mCRPC\uff09<\/td>\u672a\u516c\u5f00<\/td>\u4e34\u5e8a\u524d<\/td>2026-06-24 \u8bbe NewCo<\/td><\/tr><\/tbody><\/table><\/figure>\n\n\n\n

Halda\u7684RIPTAC\u5e73\u53f0\u4e0d\u6b62\u805a\u7126\u524d\u5217\u817a\u764c\uff0c\u540c\u6b65\u5e03\u5c40\u4e73\u817a\u764c\u3001\u80ba\u764c\u7b49\u591a\u4e2a\u5b9e\u4f53\u7624\u9776\u70b9\u5019\u9009\u5206\u5b50\uff0c\u76ee\u524d\u5747\u505c\u7559\u5728\u65e9\u671f\u4e34\u5e8a\u524d\u9636\u6bb5\u3002\u5f53\u524d\u8d5b\u9053\u73a9\u5bb6\u683c\u5c40\u975e\u5e38\u96c6\u4e2d\uff1a<\/p>\n\n\n\n

    \n
  • Halda\uff08\u5f3a\u751f\u65d7\u4e0b\uff09\uff1a\u5168\u7403\u552f\u4e00\u62e5\u6709\u8fdb\u5165\u4eba\u4f53\u4e34\u5e8aRIPTAC\u5206\u5b50\u7684\u5e73\u53f0\uff0c\u6838\u5fc3\u8d44\u4ea7HLD-0915\uff1b<\/li>\n\n\n\n
  • Flare Therapeutics\uff1a\u5e03\u5c40ARON RIPTAC\uff0c\u5904\u4e8e\u4e34\u5e8a\u524d\uff1b<\/li>\n\n\n\n
  • \u5b66\u672f\u754c\u4e0e\u5176\u4ed6\u5c0f\u578bBiotech\uff1a\u9488\u5bf9\u5404\u7c7b\u80bf\u7624\u9776\u70b9\u5f00\u5c55\u65e9\u671fRIPTAC\u6982\u5ff5\u9a8c\u8bc1\u3002<\/li>\n<\/ul>\n\n\n\n

    \u6574\u4f53\u8d5b\u9053\u5c1a\u5904\u4e8e\u840c\u82bd\u9636\u6bb5\uff0c\u5168\u7403\u81f3\u4eca\u6ca1\u6709\u4efb\u4f55\u4e00\u6b3eRIPTAC\u836f\u7269\u83b7\u6279\u4e0a\u5e02\uff0cHLD-0915 \u7684\u4e34\u5e8a\u7ed3\u679c\uff0c\u5c06\u5f88\u5927\u7a0b\u5ea6\u5b9a\u4e49 RIPTAC \u8d5b\u9053\u7684\u53d1\u5c55\u524d\u666f\u3002<\/p>\n\n\n\n

    3<\/strong>.1 HLD-0915\uff1a\u9996\u4e2a\u8fdb\u5165\u4e34\u5e8a\u7684 RIPTAC \u5206\u5b50<\/strong><\/h6>\n\n\n\n
    3.1.1 \u5206\u5b50\u8bbe\u8ba1\u7ed3\u6784<\/strong><\/h6>\n\n\n\n
    HLD-0915 \u662f\u4e00\u6b3eAR-BRD4 \u53cc\u529f\u80fd RIPTAC \u5206\u5b50<\/strong>\uff1a\u4e00\u7aef\u914d\u4f53\u9776\u5411\u5168\u957f\u96c4\u6fc0\u7d20\u53d7\u4f53\uff08FL-AR\uff0cTP\uff0c\u951a\u5b9a\u86cb\u767d\uff09\uff0c\u53e6\u4e00\u7aef\u914d\u4f53\u9776\u5411\u6eb4\u7ed3\u6784\u57df\u86cb\u767d4 \uff08BRD4\uff0cEP\uff0c\u7ec6\u80de\u5fc5\u9700\u86cb\u767d\uff09\uff0c\u4e24\u6bb5\u914d\u4f53\u4e4b\u95f4\u7531\u67d4\u6027 linker \u76f8\u8fde[3]<\/sup>\u3002<\/h6>\n\n\n\n
    \"\"<\/figure>\n\n\n\n

    \u56fe2\uff1aHLD-0915 \u4f5c\u7528\u673a\u5236\u3002\u524d\u5217\u817a\u764c\u7ec6\u80de\u6838\u5185\u5b58\u5728 AR \u4e0e BRD4\uff1b\u7ed9\u836f\u540e HLD-0915 \u5165\u6838\uff0c\u6784\u5efa AR-HLD-0915-BRD4 \u4e09\u5143\u590d\u5408\u7269\uff0c\u4f7f BRD4 \u5931\u6d3b\uff0c\u8bf1\u5bfc\u80bf\u7624\u7ec6\u80de\u51cb\u4ea1\uff0c\u9009\u62e9\u6027\u6740\u4f24\u524d\u5217\u817a\u764c\u7ec6\u80de\u3002<\/p>\n\n\n\n

    \u548c\u4f20\u7edf AR \u6291\u5236\u5242\u3001AR-PROTAC \u4e0d\u540c<\/strong>\u4e4b\u5904<\/strong>\uff1a<\/strong><\/h6>\n\n\n\n
    -\u4f20\u7edf NHT \u836f\u7269\uff1a<\/strong>\u5355\u7eaf\u7ed3\u5408 AR\uff0c\u6291\u5236 AR \u8f6c\u5f55\u6d3b\u6027\uff1b<\/h6>\n\n\n\n
    -AR-PROTAC\uff1a<\/strong>\u7ed3\u5408 AR\uff0c\u62db\u52df E3 \u8fde\u63a5\u9176\u964d\u89e3 AR\uff1b<\/h6>\n\n\n\n
    – HLD-0915\uff1a<\/strong>\u4ee5 FL-AR \u4f5c\u4e3a\u5206\u5b50\u652f\u67b6\uff0c\u8fd1\u8ddd\u79bb\u62db\u52df BRD4\uff0c\u5f62\u6210\u4e09\u5143\u590d\u5408\u7269\uff0c\u6270\u52a8 BRD4 \u529f\u80fd\uff0c\u8bf1\u5bfc\u80bf\u7624\u51cb\u4ea1\uff0c\u4e0d\u964d\u89e3 AR<\/strong>\u3002<\/strong>\u8be5\u8bbe\u8ba1\u7684\u4f18\u52bf\u5728\u4e8e\uff1a\u4e0d\u9700\u8981\u4f9d\u8d56 AR \u7684\u8f6c\u5f55\u529f\u80fd\uff0c\u5728\u4fdd\u7559\u5168\u957f AR \u86cb\u767d\u7684 NHT \u8010\u836f\u3001AR \u7a81\u53d8 \/ \u526a\u63a5\u53d8\u4f53\u80bf\u7624\u6a21\u578b\u4e2d\u4f9d\u7136\u6709\u6548\u3002<\/h6>\n\n\n\n
    \uff08\u9700\u6ce8\u610f\uff1a\u5f88\u591a\u6587\u732e\u3001\u4f1a\u8bae\u8d44\u6599\u4e2d\u4f1a\u770b\u5230\u591a\u4e2a\u4ee3\u53f7\uff0c\u5176\u5b9e\u6307\u4ee3\u540c\u4e00\u4e2a\u5206\u5b50\uff1a\u4e34\u5e8a\u524d\u9636\u6bb5\u4ee3\u53f7 H001\uff1b\u63a8\u8fdb\u81f3\u4e34\u5e8a\u9636\u6bb5\u547d\u540d HLD-0915\uff1b\u5f3a\u751f\u6536\u8d2d Halda \u4e4b\u540e\uff0c\u8d4b\u4e88\u65b0\u836f\u5185\u90e8\u7f16\u53f7 JNJ-101556143\u3002\uff09<\/h6>\n\n\n\n
    \"\"<\/figure>\n\n\n\n

    \u56fe3\uff1aHLD-0915 \u63a8\u65ad\u4ee3\u8868\u5316\u5408\u7269\u7ed3\u6784\u62c6\u89e3\uff1aAR \u914d\u4f53\uff08\u82ef\u6c27\u57fa-\u56db\u7532\u57fa\u73af\u4e01\u70f7\uff09\u2014\u8fde\u63a5\u5b50\u2014BRD4 \u914d\u4f53\uff08JQ1 \u9aa8\u67b6 + C6-\u5641\u5511\u51fa\u53e3\uff09\u3002\u56fe\u6e90\uff1a\u533b\u836f\u9b54\u65b9\u300a\u4ece “\u6e05\u9664\u964d\u89e3” \u5230 “\u4e34\u8fd1\u6263\u62bc”\uff1aRIPTAC \u7684\u60ca\u9e3f\u4e00\u77a5\u300b\u3002<\/p>\n\n\n\n

    3.1.2 \u5173\u952e\u4e34\u5e8a\u8bd5\u9a8c NCT06800313<\/strong><\/h6>\n\n\n\n

    HLD-0915 \u7684 I\/II \u671f\u9996\u6b21\u4eba\u4f53\u8bd5\u9a8c\uff08FIH\uff09\u662f\u4e00\u9879\u591a\u4e2d\u5fc3\u3001\u5f00\u653e\u6807\u7b7e\u7814\u7a76\uff0c\u91c7\u7528 BOIN \u8d1d\u53f6\u65af\u5242\u91cf\u722c\u5761\u8bbe\u8ba1\uff0c\u76ee\u6807\u4eba\u7fa4\u4e3a\u8fdb\u5c55\u671f mCRPC \u60a3\u8005\u3002\u5165\u7ec4\u53d7\u8bd5\u8005\u5927\u591a\u5c5e\u4e8e\u96be\u6cbb\u4eba\u7fa4\uff1a\u65e2\u5f80\u63a5\u53d7\u8fc7 ARPI \u65b0\u578b\u5185\u5206\u6ccc\u836f\u7269\u3001\u7d2b\u6749\u7c7b\u5316\u7597\uff0c\u90e8\u5206\u60a3\u8005\u751a\u81f3\u7ecf\u8fc7 PSMA \u653e\u5c04\u6027\u914d\u4f53\u6cbb\u7597\u540e\u75be\u75c5\u8fdb\u5c55\u3002\u8bd5\u9a8c\u8ba1\u5212\u6700\u591a\u5165\u7ec4 190 \u4f8b\u60a3\u8005\u3002<\/p>\n\n\n\n

    2025 \u5e74\u516c\u5e03\u7684 I\/II \u671f\u521d\u6b65\u6570\u636e\uff0c\u662f RIPTAC \u9886\u57df\u91cc\u7a0b\u7891\u5f0f\u7684\u4eba\u4f53\u7ed3\u679c[4]<\/sup>\u3002\u5728\u81f3\u5c11\u5b8c\u6210 2 \u5468\u671f\u6cbb\u7597\u3001\u53ef\u8bc4\u4f30\u7597\u6548\u7684 22 \u4f8b\u60a3\u8005\u4e2d\uff1a<\/p>\n\n\n\n

    – PSA50 \u5e94\u7b54\u7387 59%\uff08PSA \u4e0b\u964d\u226550%\uff09\u3002<\/strong><\/h6>\n\n\n\n
    – PSA90 \u5e94\u7b54\u7387 32%\uff08PSA \u4e0b\u964d\u226590%\uff09\u3002<\/strong><\/h6>\n\n\n\n

    – \u57fa\u7ebf\u5e26\u6709\u53ef\u6d4b\u91cf\u5b9e\u4f53\u75c5\u7076\u7684 5 \u4f8b\u60a3\u8005\uff0c\u5168\u90e8\u8fbe\u5230 RECIST \u6807\u51c6\u7684\u90e8\u5206\u7f13\u89e3 PR\uff0c\u5176\u4e2d 2 \u4f8b\u5df2\u786e\u8ba4\u4e3a\u5b8c\u5168\u7f13\u89e3\uff0c\u53e6\u6709 1 \u4f8b\u6df7\u5408\u75c5\u7076\u60a3\u8005\u7684\u8f6f\u7ec4\u7ec7\u75c5\u7076\u5b8c\u5168\u6d88\u9000[5]<\/sup>\u3002<\/p>\n\n\n\n

    \"\"<\/figure>\n\n\n\n

    \u56fe 4\uff1aHLD-0915 I\/II \u671f\u7597\u6548\u6c47\u603b\uff0c\u6765\u6e90 AACR-NCI-EORTC \u5927\u4f1a\u6d77\u62a5\u3002<\/p>\n\n\n\n

    \u5b89\u5168\u6027\u6570\u636e\u521d\u6b65\u663e\u793a\u8010\u53d7\u6027\u826f\u597d\uff0c\u6ca1\u6709\u89c2\u5bdf\u5230\u9884\u671f\u5916\u7684\u4e25\u91cd\u6bd2\u6027\u3002\u57fa\u4e8e\u8fd9\u9879\u65e9\u671f\u79ef\u6781\u6570\u636e\uff0cFDA \u6388\u4e88 HLD-0915\u5feb\u901f\u901a\u9053\u8d44\u683c\uff0c\u52a0\u901f\u540e\u7eed\u5ba1\u8bc4\u5f00\u53d1\u3002<\/p>\n\n\n\n

    \u76ee\u524d\uff0c\u56fd\u5185CDE \u5e73\u53f0\u767b\u8bb0\u5176 II \u671f\u7814\u7a76\uff08CTR20263367\uff0cJNJ-101556143 \u786c\u80f6\u56ca\uff0c\u8f6c\u79fb\u6027\u524d\u5217\u817a\u764c\uff09\u5c1a\u672a\u62db\u52df\u3002<\/p>\n\n\n\n

    3.2 HLD-0117\uff08ER\u03b1-BRD4\uff09<\/strong><\/h6>\n\n\n\n

    HLD-0117 \u9009\u62e9 ER\u03b1\uff08\u96cc\u6fc0\u7d20\u53d7\u4f53 \u03b1\uff09\u4f5c\u4e3a\u80bf\u7624\u951a\u5b9a\u86cb\u767d\uff0cEP \u540c\u6837\u9009\u62e9 BRD4\uff0c\u9002\u5e94\u75c7\u4e3a ER \u9633\u6027\u8f6c\u79fb\u6027\u4e73\u817a\u764c\u3002\u7814\u53d1\u8fdb\u5c55\u4e3a Ia\/Ib \u671f\uff0c2026 \u5e74 4 \u6708\u6b63\u5f0f\u8fdb\u5165 I \u671f\u4e34\u5e8a\uff08NCT07524855\uff0c\u8ba1\u5212\u62db\u52df\u7ea6 170 \u4f8b\uff0c\u6db5\u76d6\u7f8e\u56fd 6 \u5bb6\u4e2d\u5fc3\uff09\uff0c\u662f\u7ba1\u7ebf\u4e2d\u7b2c\u4e8c\u5feb\u8fdb\u5165\u4eba\u4f53\u8bd5\u9a8c\u7684 RIPTAC\u3002<\/p>\n\n\n\n

    \"\"<\/figure>\n\n\n\n

    \u56fe5\uff1aHLD-0117 \u63a8\u65ad\u7ed3\u6784\u62c6\u89e3\uff1aBRD4 \u914d\u4f53\u2014\u8fde\u63a5\u5b50\u2014ER \u914d\u4f53\uff08\u96f7\u6d1b\u6614\u82ac\u82ef\u5e76\u567b\u5429\u9aa8\u67b6\uff09\u3002\u56fe\u6e90\uff1a\u533b\u836f\u9b54\u65b9\u300a\u4ece “\u6e05\u9664\u964d\u89e3” \u5230 “\u4e34\u8fd1\u6263\u62bc”\uff1aRIPTAC \u7684\u60ca\u9e3f\u4e00\u77a5\u300b\u3002<\/p>\n\n\n\n

    \u539f\u7406\u548c HLD-0915 \u4e00\u81f4\uff1a\u5229\u7528\u80bf\u7624\u7ec6\u80de\u7279\u5f02\u6027\u9ad8\u8868\u8fbe\u7684 ER\u03b1 \u4f5c\u4e3a\u652f\u67b6\uff0c\u8fd1\u8ddd\u79bb\u6270\u52a8 BRD4 \u529f\u80fd\uff0c\u7528\u4e8e ER \u6291\u5236\u5242\u8010\u836f\u7684\u4e73\u817a\u764c\u4eba\u7fa4\u3002<\/p>\n\n\n\n

    3.3  HLD-0221\uff08PR-BRD4\uff09<\/strong><\/h6>\n\n\n\n

    \u951a\u5b9a\u86cb\u767d\u4e3a\u5b55\u6fc0\u7d20\u53d7\u4f53 PR\uff0cEP \u4e3a BRD4\uff0c\u76ee\u6807\u9002\u5e94\u75c7\u5b50\u5bab\u5185\u819c\u764c\uff0c\u76ee\u524d\u5904\u4e8e\u4e34\u5e8a\u524d\u7814\u7a76\u9636\u6bb5\u3002\u5b50\u5bab\u5185\u819c\u764c\u90e8\u5206\u4e9a\u578b\u9ad8\u8868\u8fbe PR\uff0c\u9002\u5408\u4f5c\u4e3a RIPTAC \u7684\u80bf\u7624\u7279\u5f02\u6027\u951a\u70b9\u3002<\/p>\n\n\n\n

    3.4 p53-Y220C \u9776\u5411 RIPTAC<\/strong><\/h6>\n\n\n\n

    \u8fd9\u662f\u7ba1\u7ebf\u4e2d\u8bbe\u8ba1\u601d\u8def\u5dee\u5f02\u5316\u6700\u5927\u7684\u5206\u5b50\u3002TP \u4e3a\u7a81\u53d8\u578b p53\uff08Y220C \u7a81\u53d8\uff09\uff0c\u642d\u914d\u5bf9\u5e94\u7684\u5fc5\u9700\u86cb\u767d EP\uff0c\u7528\u4e8e\u643a\u5e26 p53 Y220C \u7a81\u53d8\u7684\u5b9e\u4f53\u7624\u3002<\/p>\n\n\n\n

    \u91ce\u751f\u578b p53 \u662f\u6291\u764c\u57fa\u56e0\uff0c\u800c Y220C \u7a81\u53d8 p53 \u4f1a\u5728\u80bf\u7624\u7ec6\u80de\u5185\u5927\u91cf\u79ef\u7d2f\uff0c\u8be5\u5206\u5b50\u5229\u7528\u7a81\u53d8 p53 \u4f5c\u4e3a\u951a\u5b9a\u652f\u67b6\uff0c\u6740\u4f24\u643a\u5e26\u8be5\u7a81\u53d8\u7684\u5b9e\u4f53\u7624\uff1b\u8be5\u5206\u5b50\u5f53\u524d\u5904\u4e8e\u4e34\u5e8a\u524d\u9a8c\u8bc1\u9636\u6bb5\u3002<\/p>\n\n\n\n

    \"\"<\/figure>\n\n\n\n

    \u56fe6\uff1aRIPTAC 1 \u5bf9 NUGC3 \u7ec6\u80de\u7684\u589e\u6b96\u6291\u5236\u6d3b\u6027\u3002\u6709 p53\u2011Y220C \u7a81\u53d8\u7684\u80bf\u7624\u7ec6\u80de\u5bf9\u836f\u7269\u654f\u611f\uff0cp53 \u6572\u9664\u540e\u836f\u6548\u57fa\u672c\u6d88\u5931\uff0c\u8bf4\u660e\u836f\u7269\u4f5c\u7528\u4f9d\u8d56\u7a81\u53d8 p53 \u86cb\u767d[6]<\/sup>\u3002<\/p>\n\n\n\n

    \u56db\u3001\u6a2a\u5411\u5bf9\u6bd4\uff1aRIPTAC vs PROTAC<\/strong><\/h5>\n\n\n\n

    \u5f88\u591a\u8bfb\u8005\u770b\u5230\u53cc\u529f\u80fd\u5d4c\u5408\u5c0f\u5206\u5b50\uff0c\u7b2c\u4e00\u53cd\u5e94\u4f1a\u628aRIPTAC\u5f53\u6210PROTAC\u7684\u5347\u7ea7\u7248\uff0c\u8fd9\u662f\u884c\u4e1a\u6700\u5e38\u89c1\u7684\u8bef\u533a\u3002\u4e8c\u8005\u540c\u5c5e\u4e8e\u8bf1\u5bfc\u90bb\u8fd1\u5206\u5b50\u5927\u7c7b\uff0c\u4f46\u5e95\u5c42\u539f\u7406\u5b8c\u5168\u72ec\u7acb\uff0c\u4e0d\u5b58\u5728\u8fed\u4ee3\u5347\u7ea7\u5173\u7cfb\u3002<\/p>\n\n\n\n

    \u88682\uff1aRIPTAC\u4e0ePROTAC\u5bf9\u6bd4<\/p>\n\n\n\n

    \u5bf9\u6bd4\u7ef4\u5ea6<\/strong><\/td>PROTAC<\/strong><\/td>RIPTAC\uff08HLD-0915\uff09<\/strong><\/td><\/tr>
    \u6838\u5fc3\u673a\u5236<\/td>\u62db\u52dfE3\u6cdb\u7d20\u8fde\u63a5\u9176\uff0c\u6cdb\u7d20\u5316\u964d\u89e3\u9776\u86cb\u767dTP<\/strong><\/td>\u4e0d\u964d\u89e3\u4efb\u4f55\u86cb\u767d\uff1b\u4ecb\u5bfc\u951a\u5b9a\u86cb\u767dTP\u4e0eEP\u5f62\u6210\u4e09\u5143\u590d\u5408\u7269\uff0c\u706d\u6d3bEP\u529f\u80fd<\/strong><\/td><\/tr>
    \u8d77\u6548\u5fc5\u8981\u6761\u4ef6<\/td>\u9776\u86cb\u767d\u53ef\u6cdb\u7d20\u5316\u964d\u89e3\u3001\u7ec6\u80de\u5185\u5b58\u5728\u5bf9\u5e94E3\u8fde\u63a5\u9176<\/td>\u80bf\u7624\u7ec6\u80de\u5b58\u5728\u951a\u5b9a\u86cb\u767d\uff08FL-AR\uff09\uff0c\u4e0d\u8981\u6c42\u951a\u5b9a\u86cb\u767d\u5177\u5907\u8f6c\u5f55\u6d3b\u6027<\/td><\/tr>
    \u524d\u5217\u817a\u764c\u8010\u836f\u8986\u76d6<\/td>\u5bf9\u7f3a\u5931LBD\u7684AR\u526a\u63a5\u53d8\u4f53\uff08AR-V7\uff09\u5927\u591a\u5931\u6548<\/td>\u4ee5\u5168\u957f AR\uff08FL-AR\uff09\u4f5c\u4e3a\u951a\u5b9a\u86cb\u767d\uff0c\u5728\u4fdd\u7559 FL-AR \u7684\u80bf\u7624\u6a21\u578b\u4e2d\uff0c\u5bf9\u90e8\u5206 AR \u7a81\u53d8\u3001AR \u526a\u63a5\u53d8\u4f53\u6709\u6548<\/td><\/tr>
    \u9776\u86cb\u767d\u76f8\u5173\u8131\u7624\u6bd2\u6027\u98ce\u9669<\/td>\u6b63\u5e38\u7ec4\u7ec7\u8868\u8fbe\u9776\u86cb\u767d\u65f6\uff0c\u4f1a\u964d\u89e3\u6b63\u5e38\u9776\u86cb\u767d\uff0c\u5b58\u5728on-target off-tumor\u98ce\u9669<\/td>\u6b63\u5e38\u7ec6\u80de\u7f3a\u5c11\u951a\u5b9a\u86cb\u767d\uff0c\u65e0\u6cd5\u5f62\u6210\u4e09\u5143\u590d\u5408\u7269\uff0c\u7406\u8bba\u4e0a\u8be5\u98ce\u9669\u66f4\u4f4e<\/td><\/tr>
    \u524d\u5217\u817a\u764c\u4ee3\u8868\u5206\u5b50<\/td>ARV-766<\/td>HLD-0915<\/td><\/tr><\/tbody><\/table><\/figure>\n\n\n\n

    \u7b80\u5355\u901a\u4fd7\u603b\u7ed3\uff1a PROTAC\u601d\u8def\uff1a\u627e\u5230\u764c\u7ec6\u80de\u7684AR\uff0c\u628aAR\u86cb\u767d\u62c6\u6389\uff1b RIPTAC\u601d\u8def\uff1a\u501f\u7528\u764c\u7ec6\u80de\u81ea\u5e26\u7684\u5168\u957fAR\u4f5c\u4e3a\u624b\u94d0\uff0c\u9501\u4f4f\u764c\u7ec6\u80de\u8d56\u4ee5\u751f\u5b58\u7684BRD4\uff0c\u76f4\u63a5\u8bf1\u5bfc\u764c\u7ec6\u80de\u51cb\u4ea1\u3002<\/p>\n\n\n\n

    \u4e94<\/strong>\u3001RIPTAC\u5f53\u524d\u524d\u6cbf\u6311\u6218\u4e0e\u56fa\u6709\u5c40\u9650\u6027<\/strong><\/h5>\n\n\n\n

    RIPTAC\u867d\u7136\u65e9\u671f\u6570\u636e\u4eae\u773c\uff0c\u4f46\u6280\u672f\u672c\u8eab\u81ea\u5e26\u56fa\u6709\u77ed\u677f\uff0c\u540c\u65f6\u4ecd\u6709\u5927\u91cf\u5f85\u653b\u514b\u7684\u96be\u9898\u3002<\/p>\n\n\n\n

    \u7b2c\u4e00\uff0c\u4e34\u5e8a\u8bc1\u636e\u7b49\u7ea7\u4e0d\u8db3\uff1a\u76ee\u524d\u6240\u6709\u4eba\u4f53\u6570\u636e\u90fd\u6765\u81eaI\/II\u671f\u5c0f\u6837\u672c\u7814\u7a76\u3002\u957f\u671f\u6297\u80bf\u7624\u7597\u6548\u3001\u8fdc\u671f\u8010\u836f\u3001\u957f\u671f\u5b89\u5168\u6027\u3001\u771f\u5b9e\u4e16\u754c\u7684\u5e94\u7b54\u7a33\u5b9a\u6027\uff0c\u90fd\u9700\u8981III\u671f\u5927\u6837\u672c\u8bd5\u9a8c\u6765\u786e\u8ba4\u3002\u65e9\u671f\u5c0f\u6837\u672c\u6570\u636e\u5b58\u5728\u4e50\u89c2\u504f\u501a\uff0c\u4e0d\u80fd\u7b49\u540c\u4e8e\u6700\u7ec8\u4e34\u5e8a\u83b7\u76ca\u3002<\/p>\n\n\n\n

    \u7b2c\u4e8c\uff0c\u5206\u5b50\u5de5\u7a0b\u7684\u6280\u672f\u96be\u70b9\u3002RIPTAC \u7c7b\u5206\u5b50\u7684\u6d3b\u6027\u5e38\u4f9d\u8d56\u4e09\u5143\u590d\u5408\u7269\u7684\u5f62\u6210\u6548\u7387\u4e0e\u6301\u7eed\u65f6\u95f4\u3002Linker\u7684\u957f\u5ea6\u3001\u4eb2\u758f\u6c34\u6027\u3001\u5206\u5b50\u67d4\u6027\u4f1a\u6781\u5927\u5f71\u54cd\u4e09\u5143\u590d\u5408\u7269\u7ec4\u88c5\u3002\u540c\u65f6\uff0c\u8fd8\u8981\u5e73\u8861\u53e3\u670d\u751f\u7269\u5229\u7528\u5ea6\u3001\u4f53\u5185PK\/PD\uff0c\u8fd9\u7c7b\u53cc\u529f\u80fd\u5c0f\u5206\u5b50\u666e\u904d\u5206\u5b50\u91cf\u504f\u5927\uff0c\u6210\u836f\u6027\u4f18\u5316\u96be\u5ea6\u8fdc\u9ad8\u4e8e\u4f20\u7edf\u5c0f\u5206\u5b50\u836f\u7269\u3002<\/p>\n\n\n\n

    \u7b2c\u4e09\uff0c\u6f5c\u5728\u8010\u836f\u673a\u5236\u5c1a\u672a\u5b8c\u5168\u9610\u660e\u3002\u73b0\u6709\u7814\u7a76\u63a8\u6d4b\uff0c\u80bf\u7624\u53ef\u901a\u8fc7AR \u86cb\u767d\u5b8c\u5168\u4e22\u5931\uff08\u542b\u5168\u957f FL-AR \u4e0e AR \u526a\u63a5\u53d8\u4f53\uff09\u3001\u4e09\u5143\u590d\u5408\u7269\u5f62\u6210\u53d7\u963b\u3001BRD4 \u6548\u5e94\u86cb\u767d\u5f02\u5e38\u7b49\u9014\u5f84\u4ea7\u751f\u8010\u836f\uff1bBRD4 \u76f8\u5173\u8010\u836f\u5047\u8bf4\u4ecd\u9700\u66f4\u591a\u4e34\u5e8a\u524d\u4e0e\u4e34\u5e8a\u6837\u672c\u9a8c\u8bc1\u3002<\/p>\n\n\n\n

    \u516d<\/strong>\u3001\u672a\u6765\u53d1\u5c55\u65b9\u5411<\/strong><\/h5>\n\n\n\n
    \u4e34\u5e8a\u65b9\u5411<\/strong><\/h6>\n\n\n\n

    \u77ed\u671f\u91cd\u5fc3\u662f\u63a8\u8fdbHLD-0915\u7684II\u671f\u6269\u5c55\u961f\u5217\u4ee5\u53ca\u540e\u7eedIII\u671f\u786e\u8bc1\u8bd5\u9a8c\u3002\u540c\u65f6\u7814\u7a76\u8005\u6b63\u5728\u601d\u8003\u8054\u5408\u7b56\u7565\uff1a\u63a2\u7d22RIPTAC\u4e0ePSMA\u653e\u5c04\u6027\u914d\u4f53\u3001\u514d\u75ab\u6cbb\u7597\u3001\u5316\u7597\u7b49\u65b9\u6848\u8054\u5408\uff0c\u8fdb\u4e00\u6b65\u6269\u5927\u83b7\u76ca\u4eba\u7fa4\uff0c\u5ef6\u7f13\u8010\u836f\u3002<\/p>\n\n\n\n

    \u5e73\u53f0\u62d3\u5c55<\/strong><\/h6>\n\n\n\n

    RIPTAC\u4e0d\u5c40\u9650\u4e8e\u524d\u5217\u817a\u764cAR\u9776\u70b9\u3002Halda\u7684\u5e73\u53f0\u6b63\u5728\u5c1d\u8bd5\u5c06\u8fd9\u5957\u201c\u52ab\u6301\u80bf\u7624\u7279\u5f02\u6027\u86cb\u767d\u201d\u601d\u8def\u8fc1\u79fb\u5230\u4e73\u817a\u764c\u3001\u80ba\u764c\u7b49\u5176\u4ed6\u5b9e\u4f53\u7624\uff0c\u5bfb\u627e\u66f4\u591a\u5408\u9002\u7684\u80bf\u7624\u951a\u5b9a\u86cb\u767d\uff0c\u62d3\u5c55\u6280\u672f\u9002\u7528\u8fb9\u754c\u3002<\/p>\n\n\n\n

    \u5206\u5b50\u4f18\u5316<\/strong><\/h6>\n\n\n\n

    \u4e0b\u4e00\u4ee3RIPTAC\u5206\u5b50\u7684\u7814\u53d1\u76ee\u6807\uff1a\u4f18\u5316\u4e09\u5143\u590d\u5408\u7269\u4eb2\u548c\u529b\uff0c\u6539\u5584\u836f\u4ee3\u52a8\u529b\u5b66\u7279\u5f81\uff0c\u8fdb\u4e00\u6b65\u62d3\u5bbd\u6cbb\u7597\u7a97\u53e3\uff0c\u964d\u4f4e\u7ed9\u836f\u5242\u91cf\uff0c\u51cf\u5c11\u6f5c\u5728\u8131\u9776\u6548\u5e94\u3002<\/p>\n\n\n\n

    \u7ad9\u5728\u8bf1\u5bfc\u90bb\u8fd1\u6574\u4e2a\u8d5b\u9053\u6765\u770b\uff1aPROTAC\u4e0eRIPTAC\u5e76\u975e\u4e92\u76f8\u66ff\u4ee3\u7684\u7ade\u4e89\u5173\u7cfb\uff0c\u4e8c\u8005\u662f\u4e92\u8865\u3002PROTAC\u9002\u5408\u9700\u8981\u6e05\u9664\u81f4\u75c5\u9776\u86cb\u767d\u7684\u573a\u666f\uff1bRIPTAC\u66f4\u9002\u5408\u5229\u7528\u80bf\u7624\u7279\u5f02\u6027\u86cb\u767d\u4f5c\u4e3a\u951a\u70b9\uff0c\u6740\u4f24\u643a\u5e26\u8be5\u86cb\u767d\u7684\u80bf\u7624\u7ec6\u80de\u3002\u5c0f\u5206\u5b50\u836f\u7269\u7684\u5f00\u53d1\u601d\u8def\uff0c\u6b63\u5728\u4ece\u5355\u7eaf\u6291\u5236\u9776\u70b9\uff0c\u8d70\u5411\u66f4\u52a0\u591a\u5143\u7684\u86cb\u767d\u8c03\u63a7\u6a21\u5f0f\u3002<\/p>\n\n\n\n

    \u4e03\u3001<\/strong>\u7ed3\u5c3e<\/strong><\/h5>\n\n\n\n

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    \u53c2\u8003\u6587\u732e\uff1a<\/strong><\/h5>\n\n\n\n

    [1] Raina K, Forbes CD, Stronk R, Rappi JP Jr, Eastman KJ, Gerritz SW, Yu X, Li H, Bhardwaj A, Forgione M, Hundt A, King MP, Posner ZM, Denny A, McGovern A, Puleo DE, Garvin E, Chenard R, Zaware N, Mousseau JJ, Macaluso J, Martin M, Bassoli K, Jones K, Garcia M, Howard K, Smith LM, Chen JM, De Leon CA, Hines J, Kayser-Bricker KJ, Crews CM. Regulated Induced Proximity Targeting Chimeras (RIPTACs): a Novel Heterobifunctional Small Molecule Therapeutic Strategy for Killing Cancer Cells Selectively. bioRxiv [Preprint]. 2023 Jan 2:2023.01.01.522436. doi: 10.1101\/2023.01.01.522436. Update in: Cell Chem Biol. 2024 Aug 15;31(8):1490-1502.e42. doi: 10.1016\/j.chembiol.2024.07.005. PMID: 36711980; PMCID: PMC9881854.<\/p>\n\n\n\n

    [2] Ma Z, Zhang C, Shen Q, Zhou J. RIPTACs for Precision Cancer Therapy: A Novel Modality with the Inspiration of HLD-0915 as the First Candidate in Clinical Trials. J Med Chem. 2025 Jun 12;68(11):10503-10506. doi: 10.1021\/acs.jmedchem.5c01250. PMID: 40501287; PMCID: PMC12507177.<\/p>\n\n\n\n

    [3] Nypaver, J. R., & Barata, P. C. (2026). HLD-0915: Could it be the breakthrough drug we need for metastatic prostate cancer? Expert Opinion on Investigational Drugs, 35(9), 643\u2013646. https:\/\/doi.org\/10.1080\/13543784.2026.2724869.<\/p>\n\n\n\n

    [4] Halda Therapeutics. Halda Therapeutics Announces First\u2011in\u2011Human Results for HLD\u20110915, an Oral RIPTAC\u2122 Therapeutic Demonstrating Encouraging Safety and Anti\u2011Tumor Activity in Metastatic Castration\u2011Resistant Prostate Cancer (mCRPC)[EB\/OL]. (2025\u201110\u201124).<\/p>\n\n\n\n

    [5] UT MD Anderson Cancer Center. New oral therapy shows early signs of safety and effectiveness in advanced treatment-resistant prostate cancer. 2025-10-24.<\/p>\n\n\n\n

    [6] Lupey\u2011Green L N, Giffin L C, Zaware N, et al. An orally bioavailable RIPTAC\u2122 therapeutic for p53 Y220C mutant tumors[C]\/\/Proceedings of the American Association for Cancer Research Annual Meeting; 2025\u201104\u201125\u201130; Philadelphia, PA. Cancer Research, 2025, 85(8_Supplement_2): LB428. https:\/\/aacrjournals.org\/cancerres\/article\/85\/8_Supplement_2\/LB428\/761504\/Abstract\u2011LB428\u2011An\u2011orally\u2011bioavailable\u2011RIPTACT.<\/p>\n\n\n\n

    <\/p>\n\n\n\n

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