{"id":88,"date":"2023-09-18T15:12:40","date_gmt":"2023-09-18T07:12:40","guid":{"rendered":"http:\/\/www.yaozhiyou.com\/?p=88"},"modified":"2023-09-18T15:12:41","modified_gmt":"2023-09-18T07:12:41","slug":"%e5%8d%a1%e5%8d%9a%e6%9b%bf%e5%b0%bc%e7%8f%a0%e5%b3%b0%e5%88%b6%e8%8d%af-cabozanix","status":"publish","type":"post","link":"http:\/\/www.yaozhiyou.com\/?p=88","title":{"rendered":"\u5361\u535a\u66ff\u5c3c|\u73e0\u5cf0\u5236\u836f-Cabozanix"},"content":{"rendered":"\n
\"\"<\/figure>\n\n\n\n

\u3010\u836f\u7269\u540d\u3011<\/strong>cabozantinib<\/p>\n\n\n\n

\u3010\u5546\u54c1\u540d\u3011<\/strong>Cabometyx<\/p>\n\n\n\n

\u3010\u901a\u7528\u540d\u3011<\/strong>\u5361\u535a\u66ff\u5c3c<\/p>\n\n\n\n

\u3010\u521d\u6b21\u83b7\u6279\u65f6\u95f4\u3011<\/strong>2012\u5e74<\/p>\n\n\n\n

\u3010\u7c7b\u522b\u3011<\/strong>\u5c0f\u5206\u5b50\u6fc0\u9176\u6291\u5236\u5242<\/p>\n\n\n\n

\u3010\u9776\u70b9\u3011<\/strong>VEGFR2,MET,RET<\/p>\n\n\n\n

\u3010\u5206\u5b50\u7ed3\u6784\u3011<\/strong>\u5206\u5b50\u5f0f\uff1aC28H24FN3O5\u00b7C4H6O5\u5206\u5b50\u91cf\u4e3a\uff1a635.6<\/p>\n\n\n\n

\u3010\u751f\u4ea7\u516c\u53f8\u3011<\/strong>Exelixis\u5236\u836f\u516c\u53f8<\/p>\n\n\n\n

\u3010\u9002\u5e94\u75c7\u3011<\/strong><\/p>\n\n\n\n

1\u3001\u6cbb\u7597\u8fdb\u5c55\u7684\u3001\u4e0d\u80fd\u5207\u9664\u7684\u5c40\u90e8\u665a\u671f\u6216\u8f6c\u79fb\u7684\u9ad3\u6027\u7532\u72b6\u817a\u764c\u3002<\/p>\n\n\n\n

2\u3001\u7d22\u5766\u6cbb\u7597\u5931\u8d25\u7684\u665a\u671f\u80be\u764c\u3002<\/p>\n\n\n\n

\u3010\u5242\u91cf\u548c\u836f\u7269\u7ba1\u7406\u3011<\/strong><\/p>\n\n\n\n

1 \u63a8\u8350\u5242\u91cf<\/strong><\/p>\n\n\n\n

\u4e0d\u8981\u7528\u5361\u8d5e\u66ff\u5c3c\u80f6\u56ca\u66ff\u4ee3\u5361\u535a\u66ff\u5c3c\u7247\u3002<\/p>\n\n\n\n

\u5361\u535a\u66ff\u5c3c\u63a8\u8350\u7684\u6bcf\u5929\u5242\u91cf\u662f60 mg\uff0c\u4e0d\u8981\u4e0e\u98df\u7269\u540c\u5403\u5361\u535a\u66ff\u5c3c\u3002<\/p>\n\n\n\n

\u6307\u5bfc\u60a3\u8005\u670d\u7528\u5361\u535a\u66ff\u5c3c\u524d\u548c\u81f3\u5c111\u5c0f\u65f6\u540e\u5171\u81f3\u5c112\u5c0f\u65f6\u4e0d\u8981\u8fdb\u98df\u3002<\/p>\n\n\n\n

\u7ee7\u7eed\u6cbb\u7597\u76f4\u81f3\u60a3\u8005\u518d\u4e5f\u4e0d\u7ecf\u5386\u4e34\u5e8a\u83b7\u76ca\u6216\u7ecf\u53d7\u4e0d\u53ef\u63a5\u53d7\u6bd2\u6027\u3002<\/p>\n\n\n\n

\u6574\u541e\u5361\u535a\u66ff\u5c3c\u7247\uff0c\u4e0d\u8981\u538b\u788e\u5361\u535a\u66ff\u5c3c\u7247\u3002<\/p>\n\n\n\n

\u4e0b\u4e00\u5242\u91cf12\u5c0f\u65f6\u5185\u4e0d\u8981\u670d\u7528\u7f3a\u5931\u5242\u91cf\u3002<\/p>\n\n\n\n

\u5361\u535a\u66ff\u5c3c\u6cbb\u7597\u671f\u95f4\u4e0d\u8981\u6444\u53d6\u98df\u7269(\u5982\uff0c\u67da\u5b50\uff0c\u67da\u5b50\u6c41)\u6216\u8425\u517b\u8865\u5145\u7269\u5df2\u77e5\u6291\u5236\u7ec6\u80de\u8272\u7d20P450\u3002<\/p>\n\n\n\n

2 \u5242\u91cf\u8c03\u6574<\/strong><\/p>\n\n\n\n

\u5bf9\u6b63\u5728\u8fdb\u884c\u624b\u672f\u60a3\u8005\u8ba1\u5212\u5b89\u6392\u7684\u624b\u672f\u524d\u81f3\u5c1128\u5929\u505c\u6b62\u6cbb\u7597\u7528\u5361\u535a\u66ff\u5c3c\uff0c\u5305\u62ec\u7259\u79d1\u624b\u672f\u3002<\/p>\n\n\n\n

\u5bf9\u4e0d\u826f\u53cd\u5e94\u5bf9<\/strong><\/p>\n\n\n\n

\u7f8e\u56fd\u56fd\u5bb6\u764c\u75c7\u7814\u7a76\u6240\u4e0d\u826f\u4e8b\u4ef6\u5e38\u7528\u540d\u8bcd[NCI CTCAE] 4\u7ea7\u4e0d\u826f\u53cd\u5e94\uff0c\u548c\u5bf93\u7ea7\u6216\u4e0d\u80fd\u8010\u53d7\u76842\u7ea7\u4e0d\u826f\u53cd\u5e94\uff0c\u5f53\u4e0d\u80fd\u7528\u4e00\u4e2a\u5242\u91cf\u51cf\u4f4e\u6216\u652f\u6301\u533b\u62a4\u5904\u7406\u65f6\u4e0d\u7ed9\u5361\u535a\u66ff\u5c3c\u3002<\/p>\n\n\n\n

\u5728\u4e00\u4e2a\u4e0d\u826f\u53cd\u5e94\u89e3\u51b3\/\u6539\u5584\u65f6(\u5373\uff0c\u8fd4\u56de\u81f3\u57fa\u7ebf\u6216\u89e3\u51b3\u81f31\u7ea7)\uff0c\u51cf\u4f4e\u5242\u91cf\u5982\u4e0b:<\/p>\n\n\n\n

\u5982\u4ee5\u524d\u5730\u63a5\u53d760 mg\u6bcf\u5929\u5242\u91cf\uff0c\u572840 mg\u6bcf\u5929\u6062\u590d\u6cbb\u7597\u3002<\/p>\n\n\n\n

\u5982\u4ee5\u524d\u5730\u63a5\u53d740 mg\u6bcf\u5929\u5242\u91cf\uff0c\u572820 mg\u6bcf\u5929\u6062\u590d\u6cbb\u7597\u3002<\/p>\n\n\n\n

\u5982\u4ee5\u524d\u5730\u63a5\u53d720 mg\u6bcf\u5929\u5242\u91cf\uff0c\u5982\u8010\u53d7\u572820 mg\u6062\u590d\uff0c\u5426\u5219\uff0c\u7ec8\u6b62\u670d\u7528\u5361\u535a\u66ff\u5c3c\u3002<\/p>\n\n\n\n

\u56e0\u4ee5\u4e0b\u4efb\u4f55\u60c5\u51b5\u6c38\u4e45\u5730\u7ec8\u6b62\u5361\u535a\u66ff\u5c3c\uff1a<\/p>\n\n\n\n

\u53d1\u751f\u4e0d\u80fd\u5904\u7406\u7684\u7618\u7ba1\u6216GI\u7a7f\u5b54\u4e25\u91cd\u51fa\u8840<\/p>\n\n\n\n

\u52a8\u8109\u8840\u6813\u6813\u585e\u4e8b\u4ef6(\u5982\uff0c\u5fc3\u808c\u6897\u6b7b\uff0c\u8111\u6897\u585e)<\/p>\n\n\n\n

\u9ad8\u8840\u538b\u5371\u8c61\u6216\u4e25\u91cd\u9ad8\u8840\u538b<\/p>\n\n\n\n

\u5728\u5f53\u524d\u5730\u670d\u7528\u4e00\u4e2a\u5f3aCYP3A4\u6291\u5236\u5242\u60a3\u8005\uff0c\u51cf\u4f4e\u6bcf\u5929\u5361\u535a\u66ff\u5c3c\u5242\u91cf20 mg(\u4f8b\u5982\uff0c\u4ece60 mg\u81f340 mg\u6bcf\u5929\u6216\u4ece40 mg\u81f320 mg\u6bcf\u5929)\u3002<\/p>\n\n\n\n

\u7ec8\u6b62\u5f3a\u6291\u5236\u5242\u540e2\u81f33\u5929\uff0c\u6062\u590dCYP3A4\u6291\u5236\u5242\u5f00\u59cb\u524d\u4f7f\u7528\u5242\u91cf\u3002<\/p>\n\n\n\n

\u5728\u5f53\u524d\u5730\u670d\u7528\u4e00\u4e2a\u5f3aCYP3A4\u8bf1\u5bfc\u5242\u60a3\u8005\u5982\u8010\u53d7\u65f6\uff0c\u589e\u52a0\u6bcf\u5929\u5361\u535a\u66ff\u5c3c\u5242\u91cf20 mg(\u4f8b\u5982\uff0c\u4ece60 mg\u81f380 mg\u6bcf\u5929\u6216\u4ece40 mg\u81f360 mg\u6bcf\u5929)\u3002<\/p>\n\n\n\n

\u5f3a\u8bf1\u5bfc\u5242\u7ec8\u6b622\u81f33\u5929\u6062\u590dCYP3A4\u8bf1\u5bfc\u5242\u5f00\u59cb\u524d\u4f7f\u7528\u5242\u91cf\u3002\u5361\u535a\u66ff\u5c3c\u7684\u6bcf\u5929\u5242\u91cf\u4e0d\u5e94\u8d85\u8fc780 mg\u3002<\/p>\n\n\n\n

\u5728\u6709\u809d\u53d7\u635f\u60a3\u8005 \u5728\u6709\u8f7b\u5ea6\u6216\u4e2d\u5ea6\u809d\u53d7\u635f\u60a3\u8005\u4e2d\u51cf\u4f4e\u5361\u535a\u66ff\u5c3c\u7684\u5f00\u59cb\u5242\u91cf\u81f340 mg\u6bcf\u59291\u6b21\u3002<\/p>\n\n\n\n

\u5efa\u8bae\u5728\u6709\u4e25\u91cd\u809d\u53d7\u635f\u60a3\u8005\u4e0d\u4f7f\u7528\u5361\u535a\u66ff\u5c3c\u3002<\/p>\n\n\n\n

\u3010\u5242\u578b\u548c\u89c4\u683c\u3011<\/strong><\/p>\n\n\n\n

60 mg \u5361\u535a\u66ff\u5c3c\u7247\u4e3a\u9ec4\u8272\u8584\u819c\u5305\u8863\uff0c\u692d\u5706\u5f62\u65e0\u5212\u7ebf\uff0c\u548c\u5728\u4e00\u4fa7\u51f9\u6709\u201cXL\u201d\u548c\u53e6\u4e00\u4fa7\u201c60\u201d\u3002<\/p>\n\n\n\n

40 mg \u5361\u535a\u66ff\u5c3c\u7247\u662f\u9ec4\u8272\u8584\u819c\u5305\u8863\uff0c\u4e09\u89d2\u5f62\u65e0\u5212\u7ebf\uff0c\u548c\u5728\u4e00\u4fa7\u51f9\u6709\u201cXL\u201d\u548c\u53e6\u4e00\u4fa7\u201c40\u201d\u3002<\/p>\n\n\n\n

20 mg \u5361\u535a\u66ff\u5c3c\u7247\u662f\u9ec4\u8272\u8584\u819c\u5305\u8863\uff0c\u5706\u65e0\u5212\u7ebf\uff0c\u548c\u5728\u4e00\u4fa7\u51f9\u6709\u201cXL\u201d\u548c\u53e6\u4e00\u4fa7\u201c20\u201d\u3002<\/p>\n\n\n\n

\u3010\u7981\u5fcc\u75c7\u3011\u65e0\u3002<\/strong><\/p>\n\n\n\n

\u3010\u8b66\u544a\u548c\u6ce8\u610f\u4e8b\u9879\u3011<\/strong><\/p>\n\n\n\n

1 \u51fa\u8840\u7528\u5361\u535a\u66ff\u5c3c\u53d1\u751f\u4e25\u91cd\u51fa\u8840\u3002<\/p>\n\n\n\n

\u5728\u5361\u535a\u66ff\u5c3c-\u6cbb\u7597\u60a3\u8005\u2265 3\u7ea7\u51fa\u8840\u4e8b\u4ef6\u53d1\u751f\u7387\u4e3a2.1%<\/p>\n\n\n\n

\u800c\u5728\u4f9d\u7ef4\u83ab\u53f8[everolimus]-\u6cbb\u7597\u60a3\u80051.6%\u3002<\/p>\n\n\n\n

\u5728\u5361\u8d5e\u66ff\u5c3c\u4e34\u5e8a\u8ba1\u5212\u8fd8\u53d1\u751f\u81f4\u547d\u6027\u51fa\u8840\u3002\u4e0d\u8981\u7ed9\u4e88\u5361\u535a\u66ff\u5c3c\u6709\u4e25\u91cd\u51fa\u8840\u6216\u5904\u4e8e\u4e25\u91cd\u51fa\u8840\u98ce\u9669\u60a3\u8005\u3002<\/p>\n\n\n\n

2 GI\u7a7f\u5b54\u548c\u7618\u7ba1\u5728\u4e00\u9879\u968f\u673a\u5316\u80be\u7ec6\u80de\u764c\u7814\u7a76\u4e2d\uff0c<\/strong><\/p>\n\n\n\n

\u5361\u535a\u66ff\u5c3c-\u6cbb\u7597\u60a3\u8005\u62a5\u9053\u7618\u7ba11.2%(\u5305\u62ec0.6%\u809b\u95e8\u7618\u7ba1) \u800c\u4f9d\u7ef4\u83ab\u53f8-\u6cbb\u7597\u60a3\u8005\u4e3a0%\u3002<\/p>\n\n\n\n

\u5361\u535a\u66ff\u5c3c-\u6cbb\u7597\u60a3\u8005\u62a5\u9053\u80c3\u80a0\u9053(GI)\u7a7f\u5b540.9%\u800c\u4f9d\u7ef4\u83ab\u53f8-\u6cbb\u7597\u60a3\u80050.6%\u3002\u5361\u8d5e\u66ff\u5c3c\u4e34\u5e8a\u8ba1\u5212\u4e2d\u53d1\u751f\u81f4\u547d\u6027\u7a7f\u5b54\u3002\u76d1\u89c6\u60a3\u8005\u7618\u7ba1\u548c\u7a7f\u5b54\u75c7\u72b6\u3002\u7ecf\u53d7\u4e00\u4e2a\u7618\u7ba1\u4e0d\u80fd\u9002\u5f53\u5730\u5904\u7406\u6216GI\u7a7f\u5b54\u60a3\u8005\u7ec8\u6b62\u5361\u535a\u66ff\u5c3c\u3002<\/p>\n\n\n\n

3 \u8840\u6813\u6027\u4e8b\u4ef6<\/strong><\/p>\n\n\n\n

\u5361\u535a\u66ff\u5c3c\u6cbb\u7597\u5bfc\u81f4\u8840\u6813\u6027\u4e8b\u4ef6\u53d1\u751f\u7387\u589e\u52a0\u3002<\/p>\n\n\n\n

\u5361\u535a\u66ff\u5c3c-\u6cbb\u7597\u60a3\u8005\u62a5\u9053\u9759\u8109\u8840\u6813\u6813\u585e7.3%\u800c\u4f9d\u7ef4\u83ab\u53f8-\u6cbb\u7597\u60a3\u8005\u4e3a2.5%\u3002<\/p>\n\n\n\n

\u5361\u535a\u66ff\u5c3c-\u6cbb\u7597\u60a3\u8005\u53d1\u751f\u80ba\u6813\u585e3.9%\u800c\u4f9d\u7ef4\u83ab\u53f8-\u6cbb\u7597\u60a3\u8005\u4e3a0.3%\u3002<\/p>\n\n\n\n

\u5361\u535a\u66ff\u5c3c-\u6cbb\u7597\u60a3\u8005\u62a5\u9053\u52a8\u8109\u8840\u6813\u6813\u585e\u4e8b\u4ef60.9%\u800c\u4f9d\u7ef4\u83ab\u53f8-\u6cbb\u7597\u60a3\u8005\u4e3a 0.3%\u3002<\/p>\n\n\n\n

\u5728\u5361\u8d5e\u66ff\u5c3c\u4e34\u5e8a\u8ba1\u5212\u4e2d\u53d1\u751f\u81f4\u547d\u6027\u8840\u6813\u6027\u4e8b\u4ef6\u3002\u5728\u53d1\u751f\u4e00\u4e2a\u6025\u6027\u5fc3\u808c\u6897\u6b7b\u6216\u4efb\u4f55\u5176\u4ed6\u52a8\u8109\u8840\u6813\u6813\u585e\u5408\u5e76\u75c7\u60a3\u8005\u7ec8\u6b62\u5361\u535a\u66ff\u5c3c\u3002<\/p>\n\n\n\n

4 \u9ad8\u8840\u538b\u548c\u9ad8\u8840\u538b\u5371\u8c61<\/strong><\/p>\n\n\n\n

\u5361\u535a\u66ff\u5c3c\u6cbb\u7597\u5bfc\u81f4\u6cbb\u7597-\u51fa\u73b0\u9ad8\u8840\u538b\u7684\u53d1\u751f\u7387\u589e\u52a0\u3002<\/p>\n\n\n\n

\u5361\u535a\u66ff\u5c3c-\u6cbb\u7597\u60a3\u8005\u62a5\u9053\u9ad8\u8840\u538b\u4e3a37%(15%\u22653\u7ea7)\u800c\u4f9d\u7ef4\u83ab\u53f8-\u6cbb\u7597\u60a3\u8005\u4e3a7.1%(3.1%\u22653\u7ea7)\u3002<\/p>\n\n\n\n

\u5361\u535a\u66ff\u5c3c\u524d\u81f3\u5f00\u59cb\u548c\u6cbb\u7597\u671f\u95f4\u5b9a\u671f\u5730\u76d1\u89c6\u8840\u538b\uff0c\u5bf9\u7528\u533b\u836f\u5904\u7406\u4e0d\u80fd\u9002\u5f53\u63a7\u5236\u7684\u9ad8\u8840\u538b\u4e0d\u7ed9\u5361\u535a\u66ff\u5c3c\uff1b<\/p>\n\n\n\n

\u5f53\u88ab\u63a7\u5236\uff0c\u5728\u51cf\u4f4e\u5242\u91cf\u6062\u590d\u5361\u535a\u66ff\u5c3c\u3002<\/p>\n\n\n\n

\u5bf9\u7528\u6297-\u9ad8\u8840\u538b\u6cbb\u7597\u4e0d\u80fd\u63a7\u5236\u7684\u4e25\u91cd\u9ad8\u8840\u538b\u7ec8\u6b62\u5361\u535a\u66ff\u5c3c\u3002<\/p>\n\n\n\n

\u5982\u533b\u5b66\u5904\u7406\u6709\u9ad8\u8840\u538b\u5371\u8c61\u6216\u4e25\u91cd\u9ad8\u8840\u538b\u8bc1\u636e\u7ec8\u6b62\u5361\u535a\u66ff\u5c3c\u3002<\/p>\n\n\n\n

5 \u8179\u6cfb\u7528\u5361\u535a\u66ff\u5c3c\u6cbb\u7597\u60a3\u800574%\u53d1\u751f\u8179\u6cfb\u548c\u7528\u4f9d\u7ef4\u83ab\u53f8\u6cbb\u7597\u60a3\u8005\u4e2d28%\u3002<\/p>\n\n\n\n

\u5361\u535a\u66ff\u5c3c-\u6cbb\u7597\u60a3\u800511%\u53d1\u751f3\u7ea7\u8179\u6cfb\u800c\u4f9d\u7ef4\u83ab\u53f8-\u6cbb\u7597\u60a3\u8005\u4e3a2%\u3002<\/p>\n\n\n\n

\u5728\u53d1\u751f\u4e0d\u80fd\u8010\u53d72\u7ea7\u8179\u6cfb\u62163-4\u7ea7\u8179\u6cfb\u7528\u6807\u51c6\u6297\u8179\u6cfb\u6cbb\u7597\u4e0d\u80fd\u5904\u7406\u76f4\u81f3\u6539\u5584\u81f31\u7ea7\u60a3\u8005\u4e0d\u7ed9\u5361\u535a\u66ff\u5c3c\uff1b<\/p>\n\n\n\n

\u5728\u51cf\u4f4e\u5242\u91cf\u6062\u590d\u5361\u535a\u66ff\u5c3c\u300226%\u60a3\u8005\u7531\u4e8e\u53d1\u751f\u8179\u6cfb\u5242\u91cf\u4fee\u9970\u3002<\/p>\n\n\n\n

6 \u638c\u8dd6\u7ea2\u611f\u89c9\u8fdf\u949d\u7efc\u5408\u75c7<\/strong><\/p>\n\n\n\n

\u5361\u535a\u66ff\u5c3c\u6cbb\u7597\u60a3\u800542%\u53d1\u751f\u638c\u8dd6\u7ea2\u611f\u89c9\u8fdf\u949d\u7efc\u5408\u75c7(PPES)\u548c\u7528\u4f9d\u7ef4\u83ab\u53f8\u6cbb\u7597\u60a3\u8005\u4e2d6%\u3002<\/p>\n\n\n\n

\u5361\u535a\u66ff\u5c3c-\u6cbb\u7597\u60a3\u80058.2%\u53d1\u751f3\u7ea7PPES\u800c\u4f9d\u7ef4\u83ab\u53f8-\u6cbb\u7597\u60a3\u8005\u4e2d<1%\u3002<\/p>\n\n\n\n

\u53d1\u751f\u4e0d\u80fd\u8010\u53d72\u7ea7PPES\u62163\u7ea7PPES\u60a3\u8005\u4e0d\u7ed9\u5361\u535a\u66ff\u5c3c\u76f4\u81f3\u6539\u5584\u81f31\u7ea7\uff1b<\/p>\n\n\n\n

\u5728\u51cf\u4f4e\u5242\u91cf\u6062\u590d\u5361\u535a\u66ff\u5c3c\u300216%\u60a3\u8005\u7531\u4e8e\u53d1\u751fPPES\u5242\u91cf\u4fee\u9970\u3002<\/p>\n\n\n\n

7 \u53ef\u9006\u6027\u540e\u90e8\u767d\u8d28\u8111\u75c5\u7efc\u5408\u75c7<\/strong><\/p>\n\n\n\n

\u5728\u5361\u8d5e\u66ff\u5c3c\u4e34\u5e8a\u8ba1\u5212\u4e2d\u53d1\u751f\u53ef\u9006\u6027\u540e\u90e8\u767d\u8d28\u8111\u75c5\u7efc\u5408\u5f81(RPLS)\uff0c\u4e00\u79cd\u901a\u8fc7MRI\u4e0a\u7279\u5f81\u6027\u53d1\u73b0\u8bca\u65ad\u7684\u76ae\u5c42\u4e0b\u8840\u7ba1\u6027\u6c34\u80bf\u7684\u7efc\u5408\u75c7\u3002\u4efb\u4f55\u5b58\u5728\u766b\u75eb\uff0c\u5934\u75db\uff0c\u89c6\u529b\u969c\u788d\uff0c\u6df7\u4e71\u6216\u7cbe\u795e\u529f\u80fd\u6539\u53d8\u60a3\u8005\u8fdb\u884c\u5bf9RPLS\u8bc4\u4ef7\u3002\u53d1\u751fRPLS\u60a3\u8005\u7ec8\u6b62\u5361\u535a\u66ff\u5c3c\u3002<\/p>\n\n\n\n

8 \u80da\u80ce-\u80ce\u513f\u6bd2\u6027<\/strong><\/p>\n\n\n\n

\u6839\u636e\u6765\u81ea\u52a8\u7269\u7814\u7a76\u6570\u636e\u548c\u5176\u4f5c\u7528\u673a\u5236\uff0c\u5f53\u7ed9\u4e88\u598a\u5a20\u5987\u5973\u5361\u535a\u66ff\u5c3c\u53ef\u80fd\u81f4\u80ce\u513f\u5371\u5bb3\u3002\u5361\u8d5e\u66ff\u5c3c\u5728\u5668\u5b98\u5f62\u6210\u671f\u7ed9\u4e88\u81f3\u598a\u5a20\u52a8\u7269\u5728\u66b4\u9732\u4f4e\u4e8e\u4e34\u5e8a\u4e0a\u63a8\u8350\u5242\u91cf\u65f6\u66b4\u9732\u65f6\u5bfc\u81f4\u80da\u80ce\u80ce\u513f\u81f4\u6b7b\uff0c\u548c\u5728\u5927\u9f20\u589e\u52a0\u9aa8\u9abc\u53d8\u5f02\u53d1\u751f\u7387\u548c\u5728\u5154\u4e2d\u5185\u810f\u53d8\u5f02\u548c\u7578\u5f62\u3002\u5fe0\u544a\u598a\u5a20\u5987\u5973\u5bf9\u80ce\u513f\u6f5c\u5728\u98ce\u9669\u3002\u5fe0\u544a\u751f\u6b96\u6f5c\u80fd\u5973\u6027\u7528\u5361\u535a\u66ff\u5c3c\u6cbb\u7597\u671f\u95f4\u548c\u672b\u6b21\u5242\u91cf\u540e\u51714\u4e2a\u6708\u4f7f\u7528\u6709\u6548\u907f\u5b55\u3002<\/p>\n\n\n\n

\u3010\u4e0d\u826f\u53cd\u5e94\u3011<\/strong><\/p>\n\n\n\n

\u6700\u5e38\u62a5\u9053\u7684(\u226525%)\u4e0d\u826f\u53cd\u5e94\u4e3a\uff1a\u8179\u6cfb\uff0c\u75b2\u4e4f\uff0c\u6076\u5fc3\uff0c\u98df\u6b32\u51cf\u9000\uff0c\u638c\u8dd6\u7ea2\u611f\u89c9\u8fdf\u949d\u7efc\u5408\u5f81(PPES)\uff0c\u9ad8\u8840\u538b\uff0c\u5455\u5410\uff0c\u4f53\u91cd\u51cf\u4f4e\u548c\u4fbf\u79d8\u3002<\/p>\n\n\n\n

\u3010\u836f\u7269\u76f8\u4e92\u4f5c\u7528\u3011<\/strong><\/p>\n\n\n\n

\u3010\u5728\u7279\u6b8a\u4eba\u7fa4\u4e2d\u7684\u4f7f\u7528\u3011<\/strong><\/p>\n\n\n\n

1 \u598a\u5a20\u98ce\u9669<\/strong><\/p>\n\n\n\n

\u603b\u7ed3\u6839\u636e\u6765\u81ea\u52a8\u7269\u7814\u7a76\u53d1\u73b0\u548c\u5176\u4f5c\u7528\u673a\u5236\uff0c\u5361\u535a\u66ff\u5c3c\u53ef\u81f4\u80ce\u513f\u5371\u5bb3\u5f53\u7ed9\u4e88\u4e00\u4f4d\u598a\u5a20\u5987\u5973\u3002\u5728\u598a\u5a20\u5987\u5973\u4e2d\u6ca1\u6709\u53ef\u5f97\u5230\u6570\u636e\u544a\u77e5\u836f\u7269-\u5173\u8054\u98ce\u9669\u3002\u5728\u52a8\u7269\u53d1\u80b2\u548c\u751f\u6b96\u6bd2\u7406\u5b66\u7814\u7a76\u7ed9\u4e88\u5361\u8d5e\u66ff\u5c3c\u81f3\u598a\u5a20\u5927\u9f20\u548c\u5154\u5668\u5b98\u5f62\u6210\u671f\u95f4\u5bfc\u81f4\u80da\u80ce\u80ce\u513f\u81f4\u6b7b\u6027\u548c\u7ed3\u6784\u5f02\u5e38\u5728\u66b4\u9732\u4f4e\u4e8e\u5728\u63a8\u8350\u5242\u91cf\u4e34\u5e8a\u4e0a\u53d1\u751f\u3002\u5fe0\u544a\u598a\u5a20\u5987\u5973\u6216\u80b2\u9f84\u5987\u5973\u5bf9\u80ce\u513f\u6f5c\u5728\u98ce\u9669\u7684\u6f5c\u80fd\u3002\u4e0d\u77e5\u9053\u5bf9\u9002\u5e94\u75c7\u4eba\u7fa4\u4e3b\u8981\u51fa\u751f\u7f3a\u9677\u548c\u6d41\u4ea7\u7684\u4f30\u7b97\u80cc\u666f\u98ce\u9669\u3002\u5728\u7f8e\u56fd\u4e00\u822c\u4eba\u7fa4\uff0c\u4e3b\u8981\u51fa\u751f\u7f3a\u9677\u548c\u4e34\u5e8a\u4e0a\u8ba4\u53ef\u598a\u5a20\u4e2d\u6d41\u4ea7\u7684\u4f30\u7b97\u80cc\u666f\u98ce\u9669\u5206\u522b\u662f2-4%\u548c15-20%\u3002\u6570\u636e\u52a8\u7269\u6570\u636e\u5728\u4e00\u9879\u598a\u5a20\u5927\u9f20\u80da\u80ce\u80ce\u513f\u53d1\u80b2\u7814\u7a76\uff0c\u5668\u5b98\u5f62\u6210\u671f\u81ea\u59cb\u81f3\u7ec8\u6bcf\u5929\u53e3\u670d\u7ed9\u4e88\u5361\u8d5e\u66ff\u5c3c\u4e0e\u5bf9\u7167\u6bd4\u8f83\u81f4\u80da\u80ce\u80ce\u513f\u81f4\u6b7b\u7387\u589e\u52a0\u5728\u4e00\u4e2a\u5242\u91cf0.03 mg\/kg(\u5728\u63a8\u8350\u5242\u91cf\u4ebaAUC\u7ea60.12-\u500d)\u3002\u53d1\u73b0\u5305\u62ec\u5ef6\u8fdf\u9aa8\u5316\u548c\u9aa8\u9abc\u53d8\u5f02\u5728\u4e00\u4e2a\u5242\u91cf0.1 mg\/kg\/day(\u5728\u63a8\u8350\u5242\u91cf\u4ebaAUC\u7ea60.04-\u500d)\u3002\u5728\u598a\u5a20\u5154\uff0c\u5668\u5b98\u5f62\u6210\u671f\u81ea\u59cb\u81f3\u7ec8\u6bcf\u5929\u7ed9\u4e88\u5361\u8d5e\u66ff\u5c3c\u5bfc\u81f4\u5185\u810f\u7578\u5f62\u7684\u53d1\u73b0\u548c\u53d8\u5f02\u5305\u62ec\u51cf\u4f4e\u813e\u810f\u5927\u5c0f\u548c\u7f3a\u5931\u80ba\u53f6\u57283 mg\/kg(\u5728\u63a8\u8350\u5242\u91cf\u4ebaAUC\u7ea61.1-\u500d)\u3002\u5728\u4e00\u9879\u5927\u9f20\u4e2d\u56f4\u4ea7\u671f\u7814\u7a76\u4e2d\uff0c\u5361\u8d5e\u66ff\u5c3c\u88ab\u7ed9\u4e88\u53e3\u670d\u4ece\u6000\u5b55\u7b2c10\u5929\u81f3\u4ea7\u540e\u7b2c20\u5929\u3002\u5728\u5242\u91cf\u81f30.3 mg\/kg\/day(\u6700\u5927\u63a8\u8350\u4e34\u5e8a\u5242\u91cf0.05-\u500d)\u5361\u8d5e\u66ff\u5c3c\u4e0d\u4ea7\u751f\u4e0d\u826f\u6bcd\u4f53\u6bd2\u6027\u6216\u5f71\u54cd\u96cc\u6027\u5927\u9f20\u598a\u5a20\uff0c\u5206\u5a29\u6216\u54fa\u4e73\uff0c\u548c\u4e0d\u5f71\u54cd\u5b50\u4ee3\u7684\u751f\u5b58\uff0c\u751f\u957f\u6216\u4ea7\u540e\u53d1\u80b2\u3002<\/p>\n\n\n\n

2 \u54fa\u4e73\u98ce\u9669<\/strong><\/p>\n\n\n\n

\u603b\u7ed3\u6ca1\u6709\u5173\u4e8e\u5361\u8d5e\u66ff\u5c3c\u6216\u5176\u4ee3\u8c22\u7269\u5728\u4eba\u4e73\u6c41\u7684\u5b58\u5728\uff0c\u6216\u5b83\u4eec\u5f71\u54cd\u54fa\u4e73\u5582\u517b\u5a74\u513f\uff0c\u6216\u4e73\u6c41\u751f\u4ea7\u7684\u8d44\u6599\u3002\u56e0\u4e3a\u4e00\u4e2a\u54fa\u4e73\u5582\u517b\u5a74\u513f\u6765\u81ea\u5361\u535a\u66ff\u5c3c\u4e25\u91cd\u4e0d\u826f\u53cd\u5e94\u7684\u6f5c\u80fd\uff0c\u5fe0\u544a\u4e00\u4f4d\u54fa\u4e73\u5987\u5973\u5728\u7528\u5361\u535a\u66ff\u5c3c\u6cbb\u7597\u671f\u95f4\u548c\u6700\u540e\u5242\u91cf\u540e\u51714\u4e2a\u6708\u4e0d\u8981\u54fa\u4e73\u5582\u517b\u3002<\/p>\n\n\n\n

3 \u751f\u6b96\u6f5c\u80fd<\/strong><\/p>\n\n\n\n

\u7684\u5973\u6027\u548c\u7537\u6027\u907f\u5b55\u5973\u6027\u5f53\u7ed9\u4e88\u4e00\u4f4d\u598a\u5a20\u5987\u5973\u5361\u535a\u66ff\u5c3c\u53ef\u80fd\u81f4\u80ce\u513f\u5371\u5bb3\u3002\u5fe0\u544a\u751f\u6b96\u6f5c\u80fd\u5973\u6027\u7528\u5361\u535a\u66ff\u5c3c\u6cbb\u7597\u671f\u95f4\u548c\u6700\u540e\u5242\u91cf\u540e\u51714\u4e2a\u6708\u4f7f\u7528\u6709\u6548\u907f\u5b55\u3002\u4e0d\u5b55\u4e0d\u80b2\u5973\u6027\u548c\u7537\u6027\u6839\u636e\u5728\u52a8\u7269\u4e2d\u53d1\u73b0\uff0c\u751f\u6b96\u6f5c\u80fd \u5973\u6027\u548c\u7537\u6027\u4e2d\u5361\u535a\u66ff\u5c3c\u53ef\u80fd\u635f\u5bb3\u751f\u80b2\u529b\u3002<\/p>\n\n\n\n

4 \u513f\u7ae5\u4f7f\u7528<\/strong><\/p>\n\n\n\n

\u5c1a\u672a\u5728\u513f\u7ae5\u60a3\u8005\u4e2d\u7814\u7a76\u5361\u535a\u66ff\u5c3c\u7684\u5b89\u5168\u6027\u548c\u6709\u6548\u6027\u3002\u5e7c\u5e74\u52a8\u7269\u6570\u636e\u5e7c\u5e74\u5927\u9f20\u88ab\u7ed9\u4e88\u5361\u8d5e\u66ff\u5c3c\u6bcf\u5929\u5728\u5242\u91cf1\u62162 mg\/kg\/day\u4ece\u4ea7\u540e\u7b2c12\u5929(\u4e0e\u5728\u4eba\u4f4e\u4e8e2\u5c81\u6709\u53ef\u6bd4\u6027)\u81f3\u4ea7\u540e\u7b2c35\u621670\u5929\u3002\u5728\u5242\u91cf\u7b49\u4e8e\u6216\u5927\u4e8e1 mg\/kg\/day(\u6839\u636e\u4f53\u8868\u9762\u79ef\u7ea6\u4e34\u5e8a\u5242\u91cf60 mg\/day\u76840.16\u500d)\u3002\u5728\u4ea7\u540e\u7b2c22\u5929\u4e24\u4e2a\u6d4b\u8bd5\u5242\u91cf\u90fd\u89c2\u5bdf\u5230\u4f4e\u6d3b\u52a8\u5ea6\u3002\u9776\u70b9\u4e00\u822c\u5730\u4e0e\u6210\u5e74\u52a8\u7269\u6240\u89c1\u76f8\u4f3c\uff0c\u53d1\u751f\u5728\u4e24\u4e2a\u5242\u91cf\uff0c\u548c\u5305\u62ec\u80be(\u80be\u75c5\uff0c\u80be\u5c0f\u7403\u80be\u708e)\uff0c\u751f\u6b96\u5668\u5b98\uff0c\u80c3\u80a0\u9053(\u5e03\u4f26\u7eb3\u817a\u4f53\u56ca\u72b6\u6269\u5f20\u548c\u589e\u751f\u548c\u5341\u4e8c\u6307\u80a0\u708e\u75c7\uff1b\u548c\u7ed3\u80a0\u548c\u76f2\u80a0\u7684\u4e0a\u76ae\u589e\u751f)\uff0c\u9aa8\u9ad3(\u7ec6\u80de\u8fc7\u5c11\u548c\u6dcb\u5df4\u8017\u7aed)\uff0c\u548c\u809d\u3002\u5728\u6240\u6709\u5242\u91cf\u6c34\u5e73\u7259\u5f02\u5e38\u548c\u53d8\u767d\u4ee5\u53ca\u5f71\u54cd\u5bf9\u9aa8\u5305\u62ec\u77ff\u7269\u8d28\u542b\u91cf\u548c\u5bc6\u5ea6\u51cf\u4f4e\uff0c\u9aa8\u9aba\u80a5\u539a\uff0c\u548c\u9aa8\u76ae\u8d28\u51cf\u5c11\u3002\u7531\u4e8e\u6b7b\u4ea1\u7387\u7684\u9ad8\u6c34\u5e73\u57282 mg\/kg\u5242\u91cf\u6c34\u5e73\u6ca1\u6709\u8bc4\u4f30\u6062\u590d(\u6839\u636e\u4f53\u8868\u9762\u79ef\u4e34\u5e8a\u5242\u91cf60 mg\u7ea60.32\u500d)\u3002\u5728\u4f4e\u5242\u91cf\u6c34\u5e73\uff0c\u5bf9\u9aa8\u53c2\u6570\u5f71\u54cd\u662f\u90e8\u5206\u5730\u89e3\u51b3\u4f46\u5bf9\u80be\u548c\u9644\u777e\/\u777e\u4e38\u5f71\u54cd\u6cbb\u7597\u505c\u6b62\u540e\u6301\u7eed\u3002<\/p>\n\n\n\n

5 \u8001\u5e74\u4eba\u4f7f\u7528<\/strong><\/p>\n\n\n\n

\u57283\u671f\u7814\u7a76\u4e2d\uff0c41%\u7528\u5361\u535a\u66ff\u5c3c\u7684\u6cbb\u7597\u60a3\u8005\u4e3a\u5e74\u9f8465\u5c81\u548c\u4ee5\u4e0a\uff0c\u548c8%\u4e3a\u5e74\u9f8475\u548c\u4ee5\u4e0a\u3002\u8001\u5e74\u4eba\u548c\u5e74\u8f7b\u60a3\u8005\u95f4\u672a\u89c2\u5bdf\u5230\u5b89\u5168\u6027\u548c\u7597\u6548\u5dee\u522b\u3002<\/p>\n\n\n\n

6 \u809d\u53d7\u635f<\/strong><\/p>\n\n\n\n

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7 \u80be\u53d7\u635f\u5728\u6709\u8f7b\u5ea6\u6216\u4e2d\u5ea6\u80be\u53d7\u635f\u60a3\u8005\u4e2d\u65e0\u9700\u5242\u91cf\u8c03\u6574\uff0c\u6ca1\u6709\u5728\u6709\u4e25\u91cd\u80be\u53d7\u635f\u60a3\u8005\u7528CABOMETYX\u7684\u7ecf\u9a8c \u3002<\/p>\n\n\n\n

\u3010\u836f\u7269\u8fc7\u91cf\u3011<\/strong><\/p>\n\n\n\n

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\u3010\u836f\u7269\u6210\u5206\u3011<\/strong><\/p>\n\n\n\n

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\u5361\u8d5e\u66ff\u5c3c(S)-\u82f9\u679c\u9178\u76d0\u662f\u767d\u8272\u81f3\u7c73\u767d\u8272\u56fa\u4f53\u5b9e\u9645\u4e0a\u4e0d\u6eb6\u4e8e\u6c34\u6027\u4ecb\u8d28\u3002<\/p>\n\n\n\n

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