{"id":84652,"date":"2019-04-17T00:00:50","date_gmt":"2019-04-17T03:14:51","guid":{"rendered":"http:\/\/www.05921.net\/index.php\/84652\/"},"modified":"2019-04-17T11:14:54","modified_gmt":"2019-04-17T03:14:54","slug":"178a97bc0c","status":"publish","type":"post","link":"https:\/\/www.05921.net\/index.php\/84652\/","title":{"rendered":"DS-8201 \u4e3a\u4ec0\u4e48\u503c10\u4ebf\u4ee5\u4e0a\u9996\u4ed8\u6b3e"},"content":{"rendered":"
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\u4f5c\u8005 l \u697c\u670d\u5c0f\u9c81\u73ed<\/span><\/strong><\/span><\/strong><\/p>\n

\u7f16\u8f91 l<\/strong> \u7ec6\u80de\u623f\u95f4<\/strong><\/span><\/strong><\/p>\n


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\u8fd1\u671f\u6709\u5173\u963f\u65af\u5229\u5eb7\u4e0e\u7b2c\u4e00\u4e09\u5171\u5ba3\u5e03\u7684\u5408\u4f5c\u4e2d\uff0c\u9996\u4ed8\u6b3e\u5c31\u5e26\u5230Billion Dollar\u7684\u7ea7\u522b\uff0c\u4f7f\u5c0f\u7f16\u975e\u5e38\u597d\u5947DS-8201\u662f\u4ec0\u4e48\u6837\u7684ADC\uff0c\u7a76\u7adf\u4e34\u5e8a\u8bd5\u9a8c\u597d\u5230\u4ec0\u4e48\u7a0b\u5ea6\u53ef\u4ee5\u8ba9\u963f\u65af\u5229\u5eb7\u4e0b\u8fd9\u4e48\u91cd\u7684\u6ce8\u3002<\/span><\/span>
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\"DS-8201<\/p>\n

\u5de6\u56fe\u4e3aDS-8201\uff0c\u53f3\u56fe\u4e3aT-MD1<\/span><\/strong><\/span><\/span><\/p>\n


<\/p>\n

\u8fc5\u901f\u7f15\u4e0bADC\u5e02\u573a\u73b0\u72b6\u3002\u622a\u6b62\u76ee\u524d\uff0cFDA\u6279\u51c6\u4e0a\u5e02\u7684ADC\u4e00\u5171\u6709\u56db\u6b3e\u836f\uff0c\u4e09\u6b3e\u8840\u6db2\u80bf\u7624ADC\u836f\u7269\uff1a\u6700\u65e9\u662fPfizer\u7684Mylotarg\uff0c\u4ee5CD33\u4e3a\u9776\u70b9\u6cbb\u7597\u6025\u6027\u9aa8\u9ad3\u6027\u767d\u8840\u75c5\uff0c2010\u5e74\u56e0\u5b89\u5168\u6027\u95ee\u9898\u9000\u5e02\uff1b\u63a5\u4e0b\u6765\u662fSeattle Genetics\u7684Adcetris\uff0c\u4ee5CD30\u4e3a\u9776\u70b9,\u9002\u5e94\u75c7\u4e3a\u970d\u5947\u91d1\u6dcb\u5df4\u7624\uff1bPifzer\u7684Besponsa\u4ee5CD22\u4e3a\u9776\u70b9\u6cbb\u7597\u6025\u6027\u6dcb\u5df4\u7ec6\u80de\u767d\u8840\u75c5\u3002\u552f\u4e00\u4e00\u6b3e\u4ee5\u5b9e\u4f53\u7624\u4e3a\u9002\u5e94\u75c7\u7684\u662fKadcyla (TDM1) \uff0c\u9002\u5e94\u75c7\u4e3a\u665a\u671f\u5df2\u6269\u6563\u4e73\u817a\u764c\uff0c\u9776\u70b9HER2\u91c7\u7528Roch\u7684\u6297\u4f53\uff0cpayloa\u3001linker\u548c\u5076\u8054\u6280\u672f\u6765\u81ealimmunoGen\u3002\u5176\u4ed6\u4ee5\u5b9e\u4f53\u7624\u4e3a\u9002\u5e94\u75c7\u7684\u9776\u70b9\u90fd\u5728\u4e34\u5e8a\u7814\u7a76\u9636\u6bb5\uff0c\u5982Mesothelin\uff0cPSMA\uff0cEGFR\uff0cNectin-4\uff0cENNP3\uff0cTROP2\u548cp-cadherin\uff1b\u524d\u4e24\u4e2a\u4e5f\u6709\u76f8\u5bf9\u5e94\u7684TCR-T\u4ea7\u54c1\u3002<\/span><\/p>\n

\"DS-8201<\/p>\n


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Her2\u65e0\u7591\u662f\u7ade\u4e89\u6700\u6fc0\u70c8\u7684\u9776\u70b9\uff0cHer2\u9776\u70b9\u5df2\u7ecf\u4e0a\u5e02\u7684\u6297\u4f53\u4e3a\u66f2\u59a5\u73e0\u5355\u6297\u548c\u5e15\u6258\u73e0\u5355\u6297\uff0c\u6297\u4f53\u90e8\u5206\u4e0d\u662f\u96be\u70b9\uff0c\u5173\u6ce8\u70b9\u5728payload\u7684potency\uff0c\u534a\u8870\u671f\uff0clinker-payloadd\u7684\u7a33\u5b9a\u6027\u548c\u7ec6\u80de\u5185\u526a\u5207\u96be\u5ea6\uff1b\u6b64\u5916\u8fd8\u6709\u53d7\u5de5\u827a\u5f71\u54cd\u7684drug\/antibody ratio\u3002\u6709\u4e2a\u7cbe\u7b80\u7684\u6846\u67b6\u540e\u770b\u4e0bDS-8201\u7684\u8bd5\u9a8c\u6570\u636e\u3002<\/span><\/p>\n

\"DS-8201<\/p>\n


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\"DS-8201<\/p>\n


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2016\u5e74\u7684\u5c0f\u9f20\u8bd5\u9a8c\u5c31\u5df2\u7ecf\u663e\u793a\u51fa\u663e\u8457\u7684\u4f18\u8d8a\u6027\uff0c\u4e14\u7ed9\u836f\u540e14\u5929\u7684\u5c0f\u9f20\u80bf\u7624\u5207\u7247\u7ed3\u679c\u6e05\u6670\u3002\u5728\u63a5\u7740\u7b2c\u4e00\u4e09\u5171\u505a\u4e86\u624e\u5b9e\u7684\u5927I\u671f\u4e34\u5e8a\u8bd5\u9a8c\uff0c\u8ba1\u91cf\u722c\u5761\u4ece0.8mg\/kg\u5f00\u59cb\uff0c\u53ef\u89c1\u975e\u5e38\u4fdd\u5b88\u4e86\uff0c\u540e\u4e24\u500d\u9012\u589e1.6mg\/kg\uff0c3.2mg\/kg\uff0c3.2mg\/kg\uff0c6.4mg\/kg\u7ec4\u4e3a6\u4f8b\u60a3\u8005\u8fbe\u5230pharmacologically active level\u540e\uff0c\u518d\u505a\u4e865.4mg\/kg\u548c8.0mg\/kg\u5206\u522b\u6d4b\u8bd56\u4f8b\u60a3\u8005\uff0c\u5728\u540e\u7eeddose expansion\u8bd5\u9a8c\u4e2d\u9009\u62e95.4mg\/kg\u548c6.4mg\/kg\uff0c\u52065\u7ec4\uff0c\u5171\u5165\u7ec4240\u4eba\uff1a(a) T-DM1-treated HER2 positive breast cancer(IHC3+,or ISH+<\/span>)(b) Trastuzumab-treated HER2-positve gastric cancer\uff08IHC3+<\/span>\uff09(c) HER2-low breast cancer\uff08IHC2+\/ISH-<\/span>\uff09(d) HER2-expressionor HER2-mutated solid tumor\uff08IHC1+\uff0cIHC2+\uff0cIHC3+\uff09(e) HER2-positive or HER2-low breast cancer\uff08IHC1+\uff0cIHC2+\uff0cIHC3+\uff09\u3002\u4e34\u5e8a\u8bd5\u9a8c\u5df2\u89c1\u91ce\u5fc3\uff0c\u5448\u66ff\u4ee3\u4e4b\u52bf\uff0cT-MD1\u53bb\u5e74\u7684\u9500\u552e\u989d\u4e3a9.79\u4ebf\u745e\u58eb\u6cd5\u90ce\uff08\u4e0e\u7f8e\u5143\u6c47\u7387\u63a5\u8fd11\uff09\uff0cTrastuzumab\u53bb\u5e74\u9500\u552e\u989d69.82\u4ebf\u745e\u58eb\u6cd5\u90ce\u3002\u60f3\u5230\u963f\u65af\u5229\u5eb7\u5728\u4e2d\u56fd\u5c31\u67099000\u540d\u9500\u552e\uff0c\u5403\u74dc\u5fc3\u6001\u66f4\u5feb\u901f\u7684\u5f00\u59cb\u641c\u7d22\u4e34\u5e8a\u6570\u636e\uff0c\u4ee5\u4e0b\u3002<\/span><\/p>\n

\"DS-8201<\/p>\n


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\u57282018\u5e74ASCO\u4e0a\u5e76\u6ca1\u6709\u5bf9\u8fd95\u7ec4\u6570\u636e\u8fdb\u884c\u5206\u6790\uff0c\u800c\u662f\u7ed9\u4e86HER2\u9633\u6027\u4e73\u817a\u764c\uff0cHER2\u4f4e\u8868\u8fbe\u4e73\u817a\u764c\uff0cHER2\u9633\u6027\u80c3\u764c\u548c\u5176\u4ed6\u5b9e\u4f53\u7624\u7684\u6570\u636e\u3002\u5728\u4e73\u817a\u764cHER2\u4f4e\u8868\u8fbe\u7ec4\u670950%\u7684ORR\u3002\u5728\u4e73\u817a\u764cHER2-positve\u7ec4\uff0cDS-8201\u7684ORR\u4e3a54.6% v.s. T-DM1\u768443.6%\uff0c\u4e25\u91cd\u4e0d\u826f\u53cd\u5e94\u5c0f\u4e2a\u4f4d\u6570\u7684\u63d0\u9ad8\uff0c\u56e0\u4e3aHER2\u9633\u6027\u6570\u636e\u5e76\u6ca1\u6709\u7ed9\u51faT-DM1 treated HER2-positive\u60a3\u8005\u7684\u6bd4\u4f8b\uff0c\u5c0f\u7f16\u975e\u5e38\u671f\u5f85\u540e\u7eed\u7684\u4e34\u5e8a\u5206\u6790\u7ed3\u679c\u3002<\/span><\/p>\n

\"DS-8201<\/p>\n


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\"DS-8201<\/p>\n


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\"DS-8201<\/p>\n

\u56fe\u4e3aT-MD1<\/span><\/strong><\/span><\/span><\/p>\n


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\u6cbb\u7597\u671f\u95f4\u53d1\u751f\u7684\u4e0d\u826f\u4e8b\u4ef6<\/span><\/p>\n

\"DS-8201<\/p>\n


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\"DS-8201<\/p>\n

\u5de6\u56fe\u4e3aDS-8201\uff0c\u53f3\u56fe\u4e3aT-MD1<\/span><\/strong><\/span><\/p>\n


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\u53c2\u8003\u6587\u732e
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[1] Ogitani Y., Hagihara K., Oitate M. et al. Bystander killing effect of DS\u20108201a, a novel anti\u2010human epidermal growth factor receptor 2 antibody\u2013drug conjugate, in tumors with human epidermal growth factor receptor 2 heterogeneity[J]. 2016,107(7): 1039-1046.<\/span><\/span><\/p>\n

[2] 2018, ASCO, report.
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[3] T-MD1, FDA, report<\/span><\/p>\n

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\u6b22\u8fce\u52a0\u5165\u5c0f\u7f16\u56e2\u961f\u6210\u4e3a\u5c0f\u7f16\u4e00\u5458<\/strong><\/span>
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\u8bf7\u52a0\u5c0f\u7f16\u5fae\u4fe1\u53f7\uff1awuwenjun7237<\/span><\/strong><\/span><\/p>\n

\u5982\u6709\u6280\u672f\u89e3\u8bfb\u3001\u884c\u4e1a\u6d1e\u89c1\u613f\u610f\u5206\u4eab<\/span><\/strong><\/span><\/p>\n

\u6b22\u8fce\u6295\u7a3f\u5230\u5c0f\u7f16\u90ae\u7bb1\uff1awuwj06@163.com<\/strong><\/span><\/strong><\/span><\/p>\n

\"DS-8201
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\u575a\u6301\u539f\u521b\u3001\u575a\u6301\u4e13\u4e1a<\/strong><\/span><\/p>\n

\u6b22\u8fce\u5173\u6ce8<\/strong><\/span><\/strong><\/span><\/span><\/p>\n

\u6295\u7a3f\u4fe1\u7bb1\uff1awuwj06@163.com<\/span><\/p>\n

\u5c0f\u7f16\u56e2\u961f\u73b0\u670921\u4f4d\u6210\u5458\uff1a<\/strong><\/span><\/p>\n

Armstrong\u3001\u533b\u836f\u5c40\u5916\u4eba\u3001Fairy\u3001Jone\u3001<\/span>\u4e1c\u80dc\u897f\u725b\u3001Alpharesearcher\u3001MT\u3001\u767e\u8349\u3001Irene\u3001<\/span>Self Renew\u3001\u86cb\u767d\u5de5\u4eba\u3001At.Zhou\u3001Julia\u3001\u6e38\u65b9\u548c\u5c1a\u3001Grand\u3001\u5915\u9633\u6b66\u58eb\u3001\u5403\u74dc\u7fa4\u4f17\u3001Nathan\u3001\u795e\u7ecf\u5143\u3001Clear\u516e\u3001\u5357\u5c71\u5357<\/span><\/span><\/p>\n

\u6b22\u8fce\u6709\u5171\u540c\u5174\u8da3\u7684\u670b\u53cb\u52a0\u5165<\/strong><\/span><\/p>\n<\/section>\n<\/section>\n

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