{"id":53717,"date":"2018-09-27T01:00:00","date_gmt":"2018-09-30T01:48:20","guid":{"rendered":"http:\/\/www.05921.net\/index.php\/2018\/09\/30\/%e7%bd%97%e6%b0%8f%e5%8f%91%e5%b8%83alk%e6%8a%91%e5%88%b6%e5%89%82entrectinib%e7%9a%84%e4%b8%b4%e5%ba%8a%e6%95%b0%e6%8d%ae\/"},"modified":"2018-09-30T09:48:20","modified_gmt":"2018-09-30T01:48:20","slug":"%e7%bd%97%e6%b0%8f%e5%8f%91%e5%b8%83alk%e6%8a%91%e5%88%b6%e5%89%82entrectinib%e7%9a%84%e4%b8%b4%e5%ba%8a%e6%95%b0%e6%8d%ae","status":"publish","type":"post","link":"https:\/\/www.05921.net\/index.php\/53717\/","title":{"rendered":"\u7f57\u6c0f\u53d1\u5e03ALK\u6291\u5236\u5242Entrectinib\u7684\u4e34\u5e8a\u6570\u636e"},"content":{"rendered":"
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\u8fd1\u65e5\uff0c\u7f57\u6c0f\u516c\u5e03\u4e86<\/span> Entrectinib \u5728\u6cbb\u7597<\/span>ROS1\u7a81\u53d8\u7684\u975e\u5c0f\u7ec6\u80de\u80ba\u764c\u7684\u60a3\u8005\u7684\u4e34\u5e8a\u7814\u7a76\u7684\u6700\u65b0\u5206\u6790\u7ed3\u679c\u3002\u7814\u7a76\u8868\u660e\uff0c\u5728\u643a\u5e26<\/span> ROS1\u9633\u6027\u7684\u665a\u671f\u8f6c\u79fb\u6027\u975e\u5c0f\u7ec6\u80de\u80ba\u764c\uff08<\/span>NSCLC\uff09\u60a3\u8005\u4e2d\uff0c\u65e0\u8bba\u6709\u65e0\u8111\u8f6c\u79fb\uff0c\u5728\u63a5\u53d7 <\/span>Entrectinib <\/span>\u6cbb\u7597\u540e\u60a3\u8005\u7684\u4e2d\u4f4d\u65e0\u8fdb\u5c55\u751f\u5b58\u671f\uff08<\/span>PFS\uff09\u53ef\u8fbe\u5230<\/span>1\u5e74\u5230\u4e24\u5e74\u4ee5\u4e0a\u4e0d\u7b49\u3002<\/span><\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n


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Entrectinib\u662f\u4e00\u79cd\u65b0\u578b\u3001\u53ef\u53e3\u670d\u7684\u3001\u5177\u6709\u4e2d\u67a2\u795e\u7ecf\u7cfb\u7edf\u6d3b\u6027\u7684\u916a\u6c28\u9178\u6fc0\u9176\u6291\u5236\u5242\uff08<\/span>TKI<\/span>\uff09\uff0c\u9776\u5411\u6cbb\u7597\u643a\u5e26<\/span>NTRK1\/2\/3<\/span>\uff08\u7f16\u7801<\/span>TRKA\/TRKB\/TRKC<\/span>\uff09\u3001<\/span>ROS1<\/span>\u548c<\/span>ALK<\/span>\u57fa\u56e0\u878d\u5408\u7a81\u53d8\u7684\u5b9e\u4f53\u80bf\u7624\u3002<\/span><\/strong><\/span>Entrectinib<\/span>\u53ef\u901a\u8fc7\u8840\u8111\u5c4f\u969c\uff0c\u5e76\u4e14\u6ca1\u6709\u4e0d\u826f\u7684\u8131\u9776\u6d3b\u6027\uff08<\/span>off-target activity<\/span>\uff09\u3002<\/span><\/span><\/p>\n

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\u79d1\u7f57\u62c9\u591a\u5927\u5b66\u5965\u7f57\u62c9\u5206\u6821\u7684<\/span>Robert C. Doebele\u535a\u58eb\u62a5\u544a\u4e86\u5bf9\u4e09\u9879\u4e34\u5e8a\u8bd5\u9a8c\u548c\u7528<\/span>entrectinib<\/span>\u6cbb\u7597\u7684<\/span>355<\/span>\u540d\u5404\u79cd\u7c7b\u578b\u7684\u80bf\u7624\u60a3\u8005\u548c\u57fa\u56e0\u91cd\u6392\u7684\u60a3\u8005\u7684\u7efc\u5408\u5206\u6790\u7ed3\u679c\u3002<\/span><\/span><\/p>\n

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\u4e34\u5e8a\u8bd5\u9a8c\u4e2d\u7684\u4e2d\u4f4d\u968f\u8bbf\u65f6\u95f4\u4e3a<\/span>15.5\u4e2a\u6708\uff0c\u5305\u62ec\u4e86<\/span>53\u540d\u4e4b\u524d\u6ca1\u6709\u4f7f\u7528<\/span>ROS1<\/span>\u6291\u5236\u5242\u6cbb\u7597\u8fc7<\/span>ROS1<\/span>\u9633\u6027\u7684<\/span>NSCLC<\/span>\u60a3\u8005\u3002\u8fd9<\/span>53\u540d\u60a3\u8005\u7684\u5e73\u5747\u5e74\u9f84\u4e3a<\/span>53<\/span>\u5c81\uff0c\u5973\u6027\u5360\u8be5\u7ec4\u60a3\u8005\u4eba\u6570\u7684\u4e09\u5206\u4e4b\u4e8c\uff0c\u4e14<\/span>59\uff05\u7684\u60a3\u8005\u65e0\u5438\u70df\u53f2\u3002\u53e6\u5916\uff0c\u8fd9<\/span>53\u540d\u60a3\u8005\u4e2d\u6709<\/span>13\uff05\u7684\u60a3\u8005\u4e4b\u524d\u6ca1\u6709\u8fdb\u884c\u8fc7\u5168\u8eab\u6cbb\u7597\uff0c<\/span>47.1<\/span>\uff05\u7684\u60a3\u8005\u63a5\u53d7\u8fc7\u4e09\u6b21\u6216\u66f4\u591a\u6b21\u7684\u5168\u8eab\u6cbb\u7597\uff0c<\/span> 23\u4f8b\uff08<\/span>43.4<\/span>\uff05\uff09\u60a3\u8005\u5b58\u5728\u8111\u8f6c\u79fb\u3002<\/span><\/span><\/p>\n

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\u7814\u7a76\u8005\u8bc4\u4f30<\/span>Entrectinib\u7684\u5ba2\u89c2\u7f13\u89e3\u7387\u4e3a<\/span> 77.4%<\/span>\uff08<\/span>ORR<\/span>\uff09\uff0c\u5305\u62ec<\/span>17<\/span>\u540d\uff08<\/span>73.9<\/span>\uff05\uff09<\/span>CNS<\/span>\u8f6c\u79fb\u60a3\u8005\u548c<\/span>24<\/span>\u540d\uff08<\/span>80<\/span>\uff05\uff09\u6ca1\u6709\u8f6c\u79fb\u7684\u60a3\u8005\u3002\u4e2d\u4f4d\u7f13\u89e3\u6301\u7eed\u65f6\u95f4\uff08<\/span>median DOR\uff09<\/span>24.6 <\/span>\u4e2a\u6708\uff0c\u8fd9\u4e00\u7ed3\u679c\u4e0e<\/span>12<\/span>\u4e2a\u6708\u65f6\u65e0\u8fdb\u5c55\u751f\u5b58\u7387\u7684\u6982\u7387\u4e3a<\/span>65\uff05\u76f8\u5173\u3002<\/span><\/span><\/p>\n

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\u603b\u4f53\u800c\u8a00\uff0c\u60a3\u8005\u7684\u4e2d\u4f4d\u65e0\u8fdb\u5c55\u751f\u5b58\u671f\uff08<\/span>PFS\uff09\u4e3a<\/span>19.0\u4e2a\u6708\uff0c\u5176\u4e2d\u57fa\u7ebf\u8111\u8f6c\u79fb\u7684\u60a3\u8005\u7684\u4e2d\u4f4d\u65e0\u8fdb\u5c55\u751f\u5b58\u671f\uff08<\/span>PFS\uff09\u4e3a<\/span>13.6\u4e2a\u6708\uff0c\u65e0\u8111\u8f6c\u79fb\u7684\u4e3a<\/span>26.3<\/span>\u4e2a\u6708\u3002 \u5bf9\u4e8e\u4f34\u6709\u8111\u8f6c\u79fb\u7684\u60a3\u8005\uff0c\u72ec\u7acb\u76f2\u6cd5\u4e2d\u5fc3\u8bc4\u4ef7\u7684\u9885\u5185\u7f13\u89e3\u7387\u8fbe\u5230\u4e86<\/span> 55%<\/span>\uff0c\u9885\u5185\u4e2d\u4f4d\u6301\u7eed\u5e94\u7b54\uff08<\/span>median DOR<\/span>\uff09<\/span>12.9 <\/span>\u4e2a\u6708\u3002<\/span><\/span><\/p>\n

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\u5bf9<\/span>355\u540d\u60a3\u8005\u8fdb\u884c\u7684\u5b89\u5168\u5206\u6790\u663e\u793a\uff0c\u5927\u591a\u6570\u4e0d\u826f\u4e8b\u4ef6\u7684\u4e25\u91cd\u7a0b\u5ea6\u4e3a<\/span>1-2<\/span>\u7ea7\u4e14\u53ef\u9006\u3002 \u6700\u5e38\u89c1\u7684\u4e0d\u826f\u4e8b\u4ef6\uff08\u6240\u6709\u7b49\u7ea7\uff09\u662f\u5473\u89c9\u969c\u788d\uff08<\/span>41.4<\/span>\uff05\uff09\uff0c\u75b2\u52b3\uff08<\/span>27.9<\/span>\uff05\uff09\uff0c\u5934\u6655\uff08<\/span>25.4<\/span>\uff05\uff09\uff0c\u4fbf\u79d8\uff08<\/span>23.7<\/span>\uff05\uff09\uff0c\u8179\u6cfb\uff08<\/span>22.8<\/span>\uff05\uff09\u548c\u6076\u5fc3\uff08<\/span>20.8<\/span>\uff05\uff09\u3002 \u6700\u5e38\u89c1\u7684<\/span>\u22653<\/span>\u7ea7\u4e0d\u826f\u4e8b\u4ef6\u662f\u4f53\u91cd\u589e\u52a0\uff08<\/span>5.1<\/span>\uff05\uff09\uff0c\u8d2b\u8840\uff08<\/span>4.5<\/span>\uff05\uff09\u548c\u75b2\u52b3\uff08<\/span>2.8<\/span>\uff05\uff09\u3002 \u672a\u53d1\u751f<\/span>5<\/span>\u7ea7\uff08\u81f4\u547d\uff09\u4e0d\u826f\u4e8b\u4ef6\u3002\u4e25\u91cd\u4e0d\u826f\u4e8b\u4ef6\u53d1\u751f\u7387\u4e3a<\/span>8.5<\/span>\uff05\uff0c\u56e0\u4e0d\u826f\u4e8b\u4ef6\u5bfc\u81f4\u7684\u505c\u836f\u7387\u4e3a<\/span>3.9<\/span>\uff05\u3002<\/span><\/span><\/p>\n

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ROS1\u878d\u5408\u57fa\u56e0\u5728\u975e\u5c0f\u7ec6\u80de\u80ba\u764c\uff08<\/span>NSCLC<\/span>\uff09\u4e2d\u53d1\u751f\u7387\u4ec5\u4e3a<\/span>1%-2%,<\/span>\u514b\u5511\u66ff\u5c3c\u4f5c\u4e3a<\/span>ROS1\u9633\u6027\u7684\u8f6c\u79fb\u6027\u975e\u5c0f\u7ec6\u80de\u80ba\u764c\u7684\u4e00\u7ebf\u6807\u51c6\u7597\u6cd5\uff0c\u5728\u4e00\u9879<\/span>50\u4eba\u7684\u4e34\u5e8a\u8bd5\u9a8c\u4e2d\u663e\u793a\uff0c\u514b\u5511\u66ff\u5c3c\u7684\u7f13\u89e3\u7387\u4e3a<\/span>72%\uff0c\u4e2d\u4f4d\u7f13\u89e3\u6301\u7eed\u65f6\u95f4\u4e3a<\/span>17.6\u4e2a\u6708\u3002\u60a3\u8005\u4f7f\u7528\u514b\u5511\u66ff\u5c3c\u540e\u4f1a\u4e0d\u53ef\u907f\u514d\u7684\u51fa\u73b0\u8010\u836f\uff0c\u4f46\u4e34\u5e8a\u6570\u636e\u79ef\u7d2f\u8868\u660e<\/span>Entretinib\u53ef\u4ee5\u514b\u670d\u514b\u5511\u66ff\u5c3c\u7684\u8010\u836f\u6027\uff0c\u56e0\u6b64\uff0c\u4e0e\u514b\u5511\u66ff\u5c3c\u76f8\u6bd4\uff0c<\/span>Entretinib\u53ef\u80fd\u662f\u66f4\u597d\u7684\u4e00\u7ebf\u6cbb\u7597\u9009\u62e9\u3002<\/span><\/span><\/p>\n


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\u53c2\u8003\u6587\u732e\uff1a<\/span><\/p>\n

\u3010<\/span>1\u3011<\/span>Novel Agent Active in ROS1-Mutant NSCLC\u2014Frequent, durable responses with entrectinib, including CNS mets<\/span><\/p>\n

https:\/\/www.medpagetoday.com\/meetingcoverage\/iaslc\/75302<\/span><\/p>\n


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\u6392\u7248\uff1a\u9621\u4e0a\u964c\u964c<\/span><\/p>\n


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\u57f9\u8bad\u548c\u4f1a\u8bae\uff1a<\/p>\n