{"id":2219,"date":"2026-10-13T15:29:28","date_gmt":"2026-10-13T07:29:28","guid":{"rendered":"https:\/\/www.millibuff.com\/?p=2219"},"modified":"2026-10-13T15:29:28","modified_gmt":"2026-10-13T07:29:28","slug":"%e5%b0%8f%e7%89%9b%e6%b4%9e%e5%af%9f-%e5%8f%88%e4%b8%80%e6%ac%be-ar-ntd-%e6%8a%91%e5%88%b6%e5%89%82%e8%8e%b7%e6%89%b9%e4%b8%b4%e5%ba%8a%ef%bc%9ajmn-2205-%e8%83%bd%e5%90%a6%e7%bb%95%e5%bc%80-lbd","status":"publish","type":"post","link":"https:\/\/www.millibuff.com\/?p=2219","title":{"rendered":"\u5c0f\u725b\u6d1e\u5bdf | \u53c8\u4e00\u6b3e AR-NTD \u6291\u5236\u5242\u83b7\u6279\u4e34\u5e8a\uff1aJMN-2205 \u80fd\u5426\u7ed5\u5f00 LBD \u8010\u836f\uff1f"},"content":{"rendered":"\n<p class=\"wp-block-paragraph\">\u7b2c\u4e8c\u4ee3 AR \u901a\u8def\u6291\u5236\u5242\u662f\u524d\u5217\u817a\u764c\u6cbb\u7597\u7684\u57fa\u77f3\uff0c\u4f46\u8010\u836f\u51e0\u4e4e\u4e0d\u53ef\u907f\u514d\u3002\u8010\u836f\u7684\u6838\u5fc3\u673a\u5236\u4e4b\u4e00\uff0c\u662f AR \u914d\u4f53\u7ed3\u5408\u57df\uff08LBD\uff09\u7684\u7a81\u53d8\u6216 AR \u526a\u63a5\u53d8\u5f02\u4f53\uff08\u5982 AR-V7\uff09\u7684\u51fa\u73b0\u3002\u771f\u5b9e\u4e16\u754c\u6570\u636e\u663e\u793a\uff0cAR-LBD \u7a81\u53d8\u5728\u672a\u63a5\u53d7\u8fc7\u7b2c\u4e8c\u4ee3 ARPI \u6cbb\u7597\u8005\u4e2d\u60a3\u75c5\u7387\u4e3a 15%\uff0c\u63a5\u53d7\u4e00\u7ebf\u6cbb\u7597\u540e\u5347\u81f3 22%\uff0c\u4e24\u7ebf\u6cbb\u7597\u540e\u8fbe 24%<sup><strong>[1]<\/strong><\/sup>\u3002\u800c AR-V7 \u7b49 LBD \u622a\u77ed\u7684\u526a\u63a5\u53d8\u5f02\u4f53\u5b8c\u5168\u7ed5\u5f00\u4e86 LBD\u2014\u2014\u6240\u6709\u9776\u5411 LBD \u7684\u836f\u7269\u5bf9\u5b83\u90fd\u65e0\u6548\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u4e00\u4e2a\u6839\u672c\u6027\u95ee\u9898\u6d6e\u73b0\u51fa\u6765\uff1aLBD \u8fd9\u6761\u8def\u88ab\u6253\u7a7f\u4e4b\u540e\uff0cAR \u8fd8\u6709\u6ca1\u6709\u522b\u7684\u53ef\u6210\u836f\u4f4d\u70b9\uff1f<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u7b54\u6848\u662f AR&nbsp;\u7684 N \u7aef\u7ed3\u6784\u57df\uff08NTD\uff09\u3002AR-V7 \u7b49\u526a\u63a5\u53d8\u5f02\u4f53\u867d\u7136\u4e22\u5931 LBD\uff0c\u4f46 NTD \u5b8c\u6574\u4fdd\u7559\uff0c\u4e14 NTD \u4e2d\u7684\u6fc0\u6d3b\u529f\u80fd\u57df AF-1 \u662f AR \u8f6c\u5f55\u6d3b\u6027\u7684\u6838\u5fc3\u533a\u57df\u3002\u7406\u8bba\u4e0a\uff0c\u9776\u5411 NTD \u53ef\u4ee5\u540c\u65f6\u8986\u76d6\u5168\u957f AR \u548c AR-V7\uff0c\u7ed5\u5f00 LBD \u4ecb\u5bfc\u7684\u5168\u90e8\u8010\u836f\u673a\u5236\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">2026 \u5e74 10 \u6708 10 \u65e5\uff0c\u6d4e\u715c\u533b\u836f\u65d7\u4e0b\u5b50\u516c\u53f8\u676d\u715c\u5236\u836f\u7533\u62a5\u7684 1 \u7c7b\u65b0\u836f JMN-2205 \u7247\u83b7 CDE \u6279\u51c6\u5f00\u5c55\u4e34\u5e8a\u8bd5\u9a8c\uff0c\u7528\u4e8e\u6cbb\u7597\u8f6c\u79fb\u6027\u53bb\u52bf\u62b5\u6297\u6027\u524d\u5217\u817a\u764c\uff08mCRPC\uff09\u3002\u8fd9\u662f\u4e00\u6b3e\u65b0\u578b AR-NTD \u6291\u5236\u5242<sup><strong>[2]<\/strong><\/sup>\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u4f46 AR-NTD \u771f\u7684\u662f\u4e00\u4e2a\u53ef\u6210\u836f\u7684\u9776\u70b9\u5417\uff1f\u540c\u9776\u70b9\u836f\u7269\u6b64\u524d\u7684\u4e34\u5e8a\u6570\u636e\uff0c\u63d0\u4f9b\u4e86\u51b7\u9759\u7684\u53c2\u8003\u3002<\/p>\n\n\n\n<h5 class=\"wp-block-heading\"><strong>\u4e00\u3001<\/strong><strong>AR-NTD<\/strong><strong>\uff1a\u673a\u5236\u4e0a\u6210\u7acb\uff0c\u6210\u836f\u4e0a<\/strong><strong>\u6709<\/strong><strong>\u56f0\u96be<\/strong><\/h5>\n\n\n\n<p class=\"wp-block-paragraph\">NTD \u7684\u6210\u836f\u96be\u5ea6\u8fdc\u9ad8\u4e8e LBD\u3002LBD \u6709\u660e\u786e\u7684\u4e09\u7ef4\u53e3\u888b\uff0c\u5c0f\u5206\u5b50\u53ef\u4ee5\u7cbe\u786e\u5b9a\u4f4d\u7ed3\u5408\uff1bNTD \u5219\u662f\u4e00\u4e2a\u5185\u5728\u65e0\u5e8f\u533a\u57df\uff0c\u7f3a\u4e4f\u7a33\u5b9a\u7684\u6676\u4f53\u7ed3\u6784\uff0c\u4f20\u7edf\u57fa\u4e8e\u7ed3\u6784\u7684\u836f\u7269\u8bbe\u8ba1\u5728\u8fd9\u91cc\u51e0\u4e4e\u5931\u6548\u3002\u6b63\u56e0\u5982\u6b64\uff0cAR-NTD \u66fe\u88ab\u957f\u671f\u89c6\u4e3a\u300c\u4e0d\u53ef\u6210\u836f\u300d\u9776\u70b9\u3002\u76f4\u5230 2010 \u5e74\u4ee3\u521d EPI-001 \u7c7b\u5316\u5408\u7269\u51fa\u73b0\u3001\u5e76\u901a\u8fc7\u5176\u524d\u836f EPI-506\uff08ralaniten acetate\uff09\u4e8e 2016 \u5e74\u6210\u4e3a\u9996\u4e2a\u8fdb\u5165\u4e34\u5e8a\u7684 AR-NTD \u6291\u5236\u5242\uff0cAR-NTD \u624d\u771f\u6b63\u8fdb\u5165\u836f\u7269\u5f00\u53d1\u89c6\u91ce\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">JMN-2205 \u7684\u83b7\u6279\u4e34\u5e8a\uff0c\u610f\u5473\u7740\u4e2d\u56fd\u5728\u8fd9\u4e00\u8d5b\u9053\u6709\u4e86\u65b0\u7684\u4e34\u5e8a\u5019\u9009\u836f\u7269\u3002\u4f46\u4ece\u540c\u9776\u70b9\u836f\u7269\u7684\u4e34\u5e8a\u7ecf\u9a8c\u770b\uff0c\u8fd9\u4e00\u65b9\u5411\u7684\u6210\u836f\u6027\u4ecd\u9762\u4e34\u663e\u8457\u6311\u6218\u3002<\/p>\n\n\n\n<h5 class=\"wp-block-heading\"><strong>\u4e8c\u3001\u540c\u9776\u70b9\u836f\u7269\u7684\u4e34\u5e8a\u7ecf\u9a8c\uff1a\u6709\u4fe1\u53f7\uff0c\u4f46<\/strong><strong>\u79bb<\/strong><strong>\u8fc7\u5173<\/strong><strong>\u5c1a\u8fdc<\/strong><\/h5>\n\n\n\n<p class=\"wp-block-paragraph\">Masofaniten\uff08EPI-7386\uff09\uff1a\u4ece&nbsp;mHSPC&nbsp;\u7684\u79ef\u6781\u4fe1\u53f7\u5230&nbsp;mCRPC&nbsp;\u7684\u5931\u8d25<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">Masofaniten&nbsp;\u662f ESSA Pharma \u5f00\u53d1\u7684 AR-NTD \u6291\u5236\u5242\uff0c\u4e5f\u662f\u8be5\u8d5b\u9053\u4e34\u5e8a\u63a8\u8fdb\u6700\u8fdc\u7684\u5206\u5b50\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u5728 I \u671f\u5242\u91cf\u6269\u5c55\u7814\u7a76\u4e2d\uff0cMasofaniten&nbsp;\u5355\u836f\u5728\u91cd\u5ea6\u7ecf\u6cbb\u7684&nbsp;mCRPC&nbsp;\u60a3\u8005\u4e2d\u786e\u8ba4\u4e86\u826f\u597d\u7684\u5b89\u5168\u6027\u548c\u4e34\u5e8a\u76f8\u5173\u66b4\u9732\uff0c\u7ea6 1\/3 \u7684\u60a3\u8005\u89c2\u5bdf\u5230\u6297\u80bf\u7624\u6d3b\u6027\u8bc1\u636e<sup><strong>[3]<\/strong><\/sup>\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u5728&nbsp;mHSPC&nbsp;\u9636\u6bb5\uff0cMasofaniten&nbsp;\u8054\u5408\u6069\u624e\u5362\u80fa\u548c ADT \u7684 II \u671f\uff08EXTRA-PC\uff0cNCT06312670\uff09\u6570\u636e\u663e\u793a\uff0c13 \u4f8b\u60a3\u8005\u4e2d 10 \u4f8b\uff0877%\uff09\u5728 6 \u4e2a\u6708\u5185\u5b9e\u73b0 PSA&lt;0.2 ng\/mL\uff0c\u8fbe\u5230\u4e86 Simon \u4e24\u9636\u6bb5\u8bbe\u8ba1\u7684\u7597\u6548\u9608\u503c<sup><strong>[3]<\/strong><\/sup>\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u4f46\u771f\u6b63\u503c\u5f97\u5173\u6ce8\u7684\u662f&nbsp;mCRPC&nbsp;\u9636\u6bb5\u7684\u7ed3\u679c\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">2024 \u5e74 10 \u6708 31 \u65e5\uff0cESSA Pharma \u5ba3\u5e03\u7ec8\u6b62&nbsp;Masofaniten&nbsp;\u8054\u5408\u6069\u624e\u5362\u80fa\u6cbb\u7597&nbsp;mCRPC&nbsp;\u7684 II \u671f\u8bd5\u9a8c\uff08NCT05075577\uff09&nbsp;<sup><strong>[4]<\/strong><\/sup>\u3002\u4e2d\u671f\u5206\u6790\u663e\u793a\uff0c\u8054\u5408\u7ec4 PSA90 \u5e94\u7b54\u7387\u4e3a 64%\uff0c\u6069\u624e\u5362\u80fa\u5355\u836f\u7ec4\u4e3a 73%\u2014\u2014\u8054\u5408\u7ec4\u5e76\u672a\u4f18\u4e8e\u5355\u836f\u3002\u8be5\u7814\u7a76\u539f\u8ba1\u5212\u5165\u7ec4\u7ea6 120 \u4f8b\u60a3\u8005\uff0c\u4e2d\u671f\u5206\u6790\u7eb3\u5165\u4e86 52 \u4f8b\uff0c\u56e0\u4e0d\u592a\u53ef\u80fd\u8fbe\u5230\u4e3b\u8981\u7ec8\u70b9\u800c\u63d0\u524d\u7ec8\u6b62\u3002\u6b64\u540e\uff0cESSA \u51b3\u5b9a\u7ec8\u6b62\u6240\u6709&nbsp;Masofaniten&nbsp;\u4e34\u5e8a\u8bd5\u9a8c\u5e76\u64a4\u56de\u76f8\u5173 IND \u548c CTA\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u8fd9\u662f\u4e00\u4e2a\u6765\u81ea\u540c\u9776\u70b9\u836f\u7269\u7684\u5173\u952e\u4fe1\u53f7\uff1aAR-NTD \u6291\u5236\u5242\u5728\u6fc0\u7d20\u654f\u611f\u9636\u6bb5\u53ef\u80fd\u6709\u6d3b\u6027\uff0c\u4f46\u5728\u53bb\u52bf\u62b5\u6297\u9636\u6bb5\u2014\u2014\u6070\u6070\u662f JMN-2205 \u7684\u76ee\u6807\u9002\u5e94\u75c7\u2014\u2014\u9762\u4e34\u66f4\u5927\u7684\u6311\u6218\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">ONCT-534\uff1a\u751f\u7269\u5b66\u6d3b\u6027\u9a8c\u8bc1\uff0c\u4f46\u4e34\u5e8a\u5e94\u7b54\u6709\u9650<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">ONCT-534 \u662f\u4e00\u6b3e\u901a\u8fc7 NTD \u7ed3\u5408\u540c\u65f6\u5b9e\u73b0 AR \u62ee\u6297\u548c\u964d\u89e3\u7684\u53cc\u91cd\u4f5c\u7528 AR \u6291\u5236\u5242\uff08DAARI\uff09\uff0c\u540c\u65f6\u9776\u5411 AR \u526a\u63a5\u53d8\u5f02\u4f53\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u5176 I \u671f\u7814\u7a76\u5165\u7ec4 21 \u4f8b&nbsp;mCRPC&nbsp;\u60a3\u8005\uff0c\u5242\u91cf\u8303\u56f4 40-1200 mg \u6bcf\u65e5\u4e00\u6b21\u3002\u672a\u5728 28 \u5929\u5185\u89c2\u5bdf\u5230 DLT\uff0c\u6700\u5e38\u89c1\u7684 AE \u4e3a\u8d2b\u8840\u3001\u80cc\u75db\u548c\u75b2\u4e4f\u3002\u4f46\u672a\u89c2\u5bdf\u5230\u5f71\u50cf\u5b66\u6216 PSA \u5e94\u7b54\uff0c\u4ec5 3 \u4f8b\u60a3\u8005\u5728 4 \u5468\u65f6\u51fa\u73b0 PSA \u4e0b\u964d\uff0c\u5176\u4e2d 1 \u4f8b\u5728\u7814\u7a76\u5173\u95ed\u65f6\u8fbe\u5230 PSA50<sup><strong>[5]<\/strong><\/sup>\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u5173\u952e\u7684\u751f\u7269\u5b66\u8bc1\u636e\u6765\u81ea\u836f\u6548\u5b66\u6807\u5fd7\u7269\uff1a10 \u4f8b\u6709\u57fa\u7ebf AR \u86cb\u767d\u6570\u636e\u7684\u60a3\u8005\u4e2d\uff0c\u7b2c 4 \u5468 AR \u86cb\u767d\u6c34\u5e73\u4e2d\u4f4d\u53d8\u5316\u4e3a \u221240.59%\uff0c\u5176\u4e2d 7 \u4f8b\u60a3\u8005 AR \u86cb\u767d\u6c34\u5e73\u4e0b\u964d\u8d85\u8fc7 30%\u3002\u5728 300 mg \u961f\u5217\u4e2d\uff0c3 \u4f8b\u60a3\u8005\u663e\u793a AR \u86cb\u767d\u4e0e AR \u57fa\u56e0\u8868\u8fbe\u4e00\u81f4\u4e0b\u964d\uff0c\u4e14 PSA \u6c34\u5e73\u4e0e AR \u9776\u57fa\u56e0\u548c AR \u57fa\u56e0\u8868\u8fbe\u5448\u6b63\u76f8\u5173<sup><strong>[5]<\/strong><\/sup>\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u751f\u7269\u5b66\u6d3b\u6027\u786e\u5b9e\u4ea7\u751f\u4e86\uff0c\u4f46\u6ca1\u6709\u8f6c\u5316\u4e3a\u4e34\u5e8a\u5e94\u7b54\u3002\u8bba\u6587\u7ed3\u8bba\u660e\u786e\uff1a\u300cAlthough clinical responses weren&#8217;t observed, these findings provide proof-of-concept for examining AR protein changes in patients receiving DAARIs.\u300d<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">ITRI-148\uff1a\u4e34\u5e8a\u524d\u6570\u636e\u79ef\u6781\uff0c\u5c1a\u672a\u8fdb\u5165\u4e34\u5e8a<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">ITRI-148 \u662f\u4e00\u6b3e\u53e3\u670d AR-NTD PROTAC\uff0c\u901a\u8fc7\u521a\u6027\u54cc\u5576-\u7094\u70c3\u8fde\u63a5\u5668\u4f18\u5316\u53e3\u670d\u751f\u7269\u5229\u7528\u5ea6\uff0c\u53ef\u540c\u65f6\u964d\u89e3\u5168\u957f AR\u3001AR-V7 \u53ca\u4e34\u5e8a\u76f8\u5173\u7a81\u53d8\u4f53\uff08L702H\u3001H875Y\uff09<sup><strong>[6]<\/strong><\/sup>\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u4e34\u5e8a\u524d\u6570\u636e\u663e\u793a\uff1a\u5728\u6069\u624e\u5362\u80fa\u8010\u836f\u7684 CRPC \u7ec6\u80de\u4e2d\uff0cITRI-148 \u7684\u6297\u589e\u6b96\u6d3b\u6027\u4f18\u4e8e\u6069\u624e\u5362\u80fa\u548c LBD \u9776\u5411\u964d\u89e3\u5242 ARV-110\uff1b\u957f\u671f\u6cbb\u7597\u7ef4\u6301\u4e86\u6301\u7eed\u7684 AR \u4fe1\u53f7\u6291\u5236\uff0c\u672a\u89e6\u53d1\u4ee3\u507f\u6027 AR-V7 \u4e0a\u8c03\u6216 PSA \u518d\u8868\u8fbe\uff1b\u5728\u4f53\u5185\uff0c\u53e3\u670d ITRI-148 \u5728\u53bb\u52bf&nbsp;VCaP&nbsp;\u5f02\u79cd\u79fb\u690d\u6a21\u578b\u4e2d\u8bf1\u5bfc\u663e\u8457\u80bf\u7624\u6d88\u9000\uff0c\u5728\u6fc0\u7d20\u5b8c\u6574 CWR22Rv1 \u6a21\u578b\u4e2d\u6291\u5236\u80bf\u7624\u751f\u957f\uff0c\u5e76\u5c55\u73b0\u51fa\u826f\u597d\u7684\u836f\u4ee3\u52a8\u529b\u5b66\u7279\u6027\u548c\u5b89\u5168\u6027<sup><strong>[6]<\/strong><\/sup>\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">ITRI-148 \u76ee\u524d\u4ecd\u5904\u4e8e\u4e34\u5e8a\u524d\u9636\u6bb5\uff0c\u5c1a\u672a\u8fdb\u5165\u4e34\u5e8a\u3002<\/p>\n\n\n\n<h5 class=\"wp-block-heading\"><strong>\u4e09\u3001\u7406\u6027\u5224\u65ad\uff1a<\/strong><strong>JMN-2205 <\/strong><strong>\u7684\u5b9a\u4f4d\u4e0e\u6311\u6218<\/strong><\/h5>\n\n\n\n<p class=\"wp-block-paragraph\">JMN-2205 \u7684\u83b7\u6279\u4e34\u5e8a\u662f\u4e00\u4e2a\u79ef\u6781\u4fe1\u53f7\u2014\u2014AR-NTD \u9776\u5411\u7b56\u7565\u5728\u4e2d\u56fd\u6709\u4e86\u65b0\u7684\u4e34\u5e8a\u5019\u9009\u836f\u7269\u3002\u4f46\u4ece\u540c\u9776\u70b9\u836f\u7269\u7684\u4e34\u5e8a\u7ecf\u9a8c\u770b\uff0c\u8fd9\u4e00\u65b9\u5411\u9762\u4e34\u51e0\u4e2a\u5173\u952e\u6311\u6218\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u7b2c\u4e00\uff0cmCRPC&nbsp;\u9636\u6bb5\u7684\u7597\u6548\u5c1a\u672a\u88ab\u9a8c\u8bc1\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">Masofaniten&nbsp;\u5728&nbsp;mHSPC&nbsp;\u4e2d\u6709\u79ef\u6781\u4fe1\u53f7\uff0c\u4f46\u5728&nbsp;mCRPC&nbsp;\u4e2d\u8054\u5408\u7ec4\u5e76\u672a\u4f18\u4e8e\u6069\u624e\u5362\u80fa\u5355\u836f\uff0c\u4e14\u516c\u53f8\u5df2\u7ec8\u6b62\u5168\u90e8\u4e34\u5e8a\u5f00\u53d1\u3002ONCT-534 \u5728&nbsp;mCRPC&nbsp;\u4e2d\u5c55\u73b0\u4e86\u660e\u786e\u7684 AR \u86cb\u767d\u964d\u89e3\uff08\u4e2d\u4f4d \u221240.59%\uff09\uff0c\u4f46\u672a\u8f6c\u5316\u4e3a PSA \u6216\u5f71\u50cf\u5b66\u5e94\u7b54\u3002AR-NTD \u6291\u5236\u5728&nbsp;mCRPC&nbsp;\u4e2d\u662f\u5426\u771f\u7684\u80fd\u4ea7\u751f\u6709\u4e34\u5e8a\u610f\u4e49\u7684\u6297\u80bf\u7624\u6d3b\u6027\uff0c\u76ee\u524d\u5c1a\u65e0\u5b9a\u8bba<sup><strong>[3-5]<\/strong><\/sup>\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u7b2c\u4e8c\uff0cNTD \u7684\u6210\u836f\u96be\u5ea6\u51b3\u5b9a\u4e86\u4f18\u5316\u7684\u4e0d\u786e\u5b9a\u6027\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">NTD \u7f3a\u4e4f\u7a33\u5b9a\u4e09\u7ef4\u7ed3\u6784\uff0c\u5c0f\u5206\u5b50\u4e0e NTD \u7684\u7ed3\u5408\u6a21\u5f0f\u96be\u4ee5\u901a\u8fc7\u4f20\u7edf\u7ed3\u6784\u751f\u7269\u5b66\u624b\u6bb5\u4f18\u5316\u3002JMN-2205 \u7684\u5177\u4f53\u5206\u5b50\u7ed3\u6784\u3001\u7ed3\u5408\u673a\u5236\u3001\u9009\u62e9\u6027\u3001\u53e3\u670d\u66b4\u9732\u548c\u9776\u7ec4\u7ec7\u5206\u5e03\u5747\u672a\u516c\u5f00\uff0c\u65e0\u6cd5\u4e0e&nbsp;Masofaniten\u3001ONCT-534 \u6216 ITRI-148 \u8fdb\u884c\u76f4\u63a5\u6bd4\u8f83\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u7b2c\u4e09\uff0c\u4e34\u5e8a\u524d\u6570\u636e\u5c1a\u672a\u62ab\u9732\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u76ee\u524d\u516c\u5f00\u4fe1\u606f\u4ec5\u63d0\u53ca JMN-2205\u300c\u5728\u4e34\u5e8a\u524d\u7814\u7a76\u4e2d\u5c55\u73b0\u51fa\u663e\u8457\u7684\u6cbb\u7597\u6f5c\u529b\u300d\uff0c\u4f46\u5177\u4f53\u7684\u4f53\u5916\u6d3b\u6027\u3001\u52a8\u7269\u6a21\u578b\u7597\u6548\u548c\u6bd2\u7406\u5b66\u6570\u636e\u5747\u672a\u77e5\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u7b2c\u56db\uff0c\u8d5b\u9053\u7ade\u4e89\u683c\u5c40\u503c\u5f97\u5173\u6ce8\u3002<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">AR-NTD \u6291\u5236\u5242\u3001AR PROTAC \u548c AR \u4e8c\u805a\u5316\u754c\u9762\uff08DIP\uff09\u9776\u5411\u7b56\u7565\uff0c\u90fd\u65e8\u5728\u7ed5\u5f00 LBD \u8010\u836f\u673a\u5236\u3002PROTAC \u5df2\u6709\u591a\u4e2a\u5206\u5b50\u8fdb\u5165\u4e34\u5e8a\uff08QLH12016\u3001HP518\u3001GLR2037 \u7b49\uff09\uff0cDIP \u9776\u5411\u7684 DIP-1018 \u4e5f\u4e8e 2026 \u5e74 7 \u6708\u83b7 CDE \u627f\u529e\u3002JMN-2205 \u5728\u8fd9\u4e00\u7ade\u4e89\u683c\u5c40\u4e2d\u7684\u5dee\u5f02\u5316\u4ef7\u503c\uff0c\u53d6\u51b3\u4e8e\u5176 I \u671f\u6570\u636e\u80fd\u5426\u8bc1\u660e NTD \u9776\u5411\u5728&nbsp;mCRPC&nbsp;\u4e2d\u7684\u72ec\u7279\u4f18\u52bf\u3002<\/p>\n\n\n\n<h5 class=\"wp-block-heading\"><strong>\u4e00\u53e5\u8bdd\u603b\u7ed3<\/strong><\/h5>\n\n\n\n<p class=\"wp-block-paragraph\">AR-NTD \u7684\u751f\u7269\u5b66\u903b\u8f91\u6210\u7acb\uff0c\u4f46\u6982\u5ff5\u9a8c\u8bc1\u6216\u4e34\u5e8a\u9a8c\u8bc1\u5c1a\u672a\u8fc7\u5173\u3002Masofaniten&nbsp;\u5728&nbsp;mCRPC&nbsp;\u4e2d\u7684\u5931\u8d25\u548c ONCT-534\u300c\u6709\u751f\u7269\u5b66\u6d3b\u6027\u3001\u65e0\u4e34\u5e8a\u5e94\u7b54\u300d\u7684\u7ed3\u679c\uff0c\u662f\u8fd9\u6761\u8def\u5f84\u4e0a\u4e24\u4e2a\u91cd\u8981\u7684\u8d1f\u9762\u4fe1\u53f7\u3002JMN-2205 \u7684\u83b7\u6279\u4e34\u5e8a\u662f\u4e00\u4e2a\u8d77\u70b9\uff0c\u4f46\u771f\u6b63\u7684\u8003\u9a8c\u662f I \u671f\u6570\u636e\u80fd\u5426\u8bc1\u660e NTD \u9776\u5411\u5728&nbsp;mCRPC&nbsp;\u4e2d\u8d70\u5f97\u901a\u2014\u2014\u8fd9\u4e0d\u4ec5\u5173\u4e4e\u4e00\u4e2a\u5206\u5b50\u7684\u6210\u8d25\uff0c\u4e5f\u5173\u4e4e\u300c\u7ed5\u5f00 LBD\u300d\u8fd9\u4e00\u7b56\u7565\u80fd\u5426\u771f\u6b63\u5151\u73b0\u3002<\/p>\n\n\n\n<h5 class=\"wp-block-heading\"><strong>\u53c2\u8003\u6587\u732e<\/strong><\/h5>\n\n\n\n<p class=\"wp-block-paragraph\">[1] Antonarakis ES, Zhang N, Saha J, et al. Prevalence and Spectrum of AR Ligand-Binding Domain Mutations Detected in Circulating-Tumor DNA Across Disease States in Men With Metastatic Castration-Resistant Prostate Cancer. <em>JCO Precis <\/em><em>Oncol<\/em>. 2024;8:e2300330.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">[2] \u6d4e\u715c\u533b\u836f\u65d7\u4e0b\u676d\u715c\u5236\u836f AR-NTD \u6291\u5236\u5242 JMN-2205 \u7247\u4e34\u5e8a\u8bd5\u9a8c\u7533\u8bf7\u83b7\u6279\u51c6. \u533b\u836f\u9b54\u65b9&nbsp;ByDrug \/ \u65b0\u6d6a\u8d22\u7ecf. 2026-10-10 \/ 2026-10-11.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">[3] Laccetti AL, Iannotti N, Pachynski RK, et al. A Phase 1b Trial of Masofaniten (EPI-7386) in Patients With Metastatic Castration-Resistant Prostate Cancer (mCRPC). <em>Clin<\/em><em>Genitourin<\/em><em> Cancer<\/em>. 2025;23(1). \u53c2\u89c1 EXTRA-PC II \u671f\u6570\u636e\uff1aJang A, et al. <em>Oncologist<\/em>. 2026;31(2):oyaf434.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">[4] ESSA Pharma. PR Newswire: ESSA Pharma Announces Termination of Phase 2 Study Evaluating Masofaniten Combined with Enzalutamide in Patients with mCRPC. 2024-10-31\uff08OncLive 2024-11-01 \u540c\u6b65\u62a5\u9053\uff09.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">[5] Zhao S, Lang JM, Chrostek M, et al. Phase I multi-center clinical and biomarker study of the dual-action androgen receptor inhibitor ONCT-534. <em>Investigational New Drugs<\/em>. 2026;44:103-112.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">[6] Hung CL, Hsu WN, Wang TC, et al. Oral bioavailable ITRI-148 degrades androgen receptor variants and overcomes antiandrogen resistance in advanced prostate cancer. <em>Neoplasia<\/em>. 2026;71:101253.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">[7] Small-molecule modulators of the androgen receptor N-terminal domain: Advances in medicinal chemistry for prostate cancer. Eur J Med Chem. 2026;305:118580.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">[8] ESSA Pharma Provides Corporate Update and Reports Financial Results for Fiscal Fourth Quarter and Year Ended September 30, 2024. ESSA Pharma Investors. 2024-12-17.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\"><\/p>\n\n\n\n<p class=\"wp-block-paragraph\">\u64b0\u6587\uff1a\u90d1\u53f6\u654f<\/p>\n","protected":false},"excerpt":{"rendered":"<p>LBD \u88ab\u6253\u7a7f\u4e4b\u540e\uff0cAR \u8fd8\u6709\u522b\u7684\u53ef\u6253\u5417\uff1f<\/p>\n","protected":false},"author":1,"featured_media":2220,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[147],"tags":[35,86,15,32,34,29],"class_list":["post-2219","post","type-post","status-publish","format-standard","has-post-thumbnail","hentry","category-147","tag-35","tag-86","tag-15","tag-32","tag-34","tag-29"],"_links":{"self":[{"href":"https:\/\/www.millibuff.com\/index.php?rest_route=\/wp\/v2\/posts\/2219","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/www.millibuff.com\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/www.millibuff.com\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/www.millibuff.com\/index.php?rest_route=\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/www.millibuff.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=2219"}],"version-history":[{"count":1,"href":"https:\/\/www.millibuff.com\/index.php?rest_route=\/wp\/v2\/posts\/2219\/revisions"}],"predecessor-version":[{"id":2221,"href":"https:\/\/www.millibuff.com\/index.php?rest_route=\/wp\/v2\/posts\/2219\/revisions\/2221"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/www.millibuff.com\/index.php?rest_route=\/wp\/v2\/media\/2220"}],"wp:attachment":[{"href":"https:\/\/www.millibuff.com\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=2219"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.millibuff.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=2219"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.millibuff.com\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=2219"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}