{"id":73433,"date":"2018-11-27T01:00:00","date_gmt":"2018-12-07T05:16:18","guid":{"rendered":"http:\/\/www.05921.net\/index.php\/2018\/12\/07\/e8c0691e80\/"},"modified":"2018-12-07T13:16:26","modified_gmt":"2018-12-07T05:16:26","slug":"e8c0691e80","status":"publish","type":"post","link":"https:\/\/www.05921.net\/index.php\/73433\/","title":{"rendered":"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def"},"content":{"rendered":"
\n

\u70b9\u51fb\u4e0a\u65b9\u7684  \u25b2 \u6dfb\u52a0\u5173\u6ce8<\/span><\/p>\n


<\/p>\n

\u6297\u4f53\u5076\u8054\u836f\u7269\uff08Antibody\u2013drug conjugates (ADCs)\uff09\u53ef\u4ee5\u5b9a\u4e49\u4e3a\u836f\u7269\u524d\u4f53\uff0c\u6297\u4f53\u80fd\u591f\u8bc6\u522b\u8868\u8fbe\u80bf\u7624\u6297\u539f\u7684\u9776\u70b9\uff0c\u5e76\u901a\u8fc7\u8fde\u63a5\u5b50\u4e0e\u7ec6\u80de\u6bd2\u7d20\u7684\u201c\u5f39\u5934\u201d\u5076\u8054\u5f62\u6210\u9488\u5bf9\u80bf\u7624\u7ec6\u80de\u7684\u9776\u5411\u9012\u9001\u7cfb\u7edf\u3002\u5728\u7406\u60f3\u72b6\u6001\u4e0b\uff0c\u8be5\u836f\u7269\u524d\u4f53\u5728\u7cfb\u7edf\u7ed9\u836f\u65f6\u4e0d\u5177\u6709\u6bd2\u6027\uff0c\u800c\u5f53ADC\u836f\u7269\u4e2d\u7684\u6297\u4f53\u4e0e\u8868\u8fbe\u80bf\u7624\u6297\u539f\u7684\u9776\u7ec6\u80de\u7ed3\u5408\u3001\u6574\u4e2aADC\u836f\u7269\u88ab\u80bf\u7624\u7ec6\u80de\u5185\u541e\u540e\uff0c\u5c0f\u5206\u5b50\u7ec6\u80de\u6bd2\u7d20\u7ec4\u5206\u5c06\u4ee5\u9ad8\u6548\u6d3b\u6027\u5f62\u5f0f\u88ab\u8db3\u91cf\u91ca\u653e\uff0c\u4ece\u800c\u5b8c\u6210\u5bf9\u80bf\u7624\u7ec6\u80de\u7684\u6740\u4f24\u3002<\/span>
<\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"<\/p>\n

\u56fe1. \u6297\u4f53\u5076\u8054\u836f\u7269\u7ed3\u6784\u6a21\u5f0f<\/span><\/strong><\/span><\/p>\n


<\/p>\n

\u90a3\u4e48\u5176\u5b9e\u53ef\u60f3\u800c\u77e5\uff0c\u4e00\u4e2a\u7406\u60f3\u7684ADC\u836f\u7269\u9700\u8981\u56db\u4e2a\u90e8\u5206\u7684\u5b8c\u7f8e\u7ed3\u5408\uff1a<\/span><\/p>\n


<\/p>\n

\u00b7\u6297\u4f53\uff08\u9776\u70b9\uff09\u7684\u9009\u62e9\uff1a\u9488\u5bf9\u80bf\u7624\u7279\u5f02\uff08\u76f8\u5173\uff09\u6027\u6297\u539f\uff0c\u8f83\u9ad8\u7684\u8868\u8fbe\u6c34\u5e73\uff0c\u826f\u597d\u7684\u5185\u541e\u6548\u7387\u3001\u826f\u597d\u7684\u6297\u539f\u4eb2\u548c\u529b\u3001\u65e0\u514d\u75ab\u539f\u6027\u3001\u836f\u7269\u53ef\u53ca\u6027\uff1b<\/span><\/p>\n

\u00b7\u8fde\u63a5\u81c2\u7684\u9009\u62e9\uff1a\u8840\u6db2\u5faa\u73af\u4e2d\u4fdd\u6301\u7a33\u5b9a\uff0c\u5728\u7ec6\u80de\u5185\u5feb\u901f\u89e3\u4f53\uff0c\u9ad8\u6548\u91ca\u653e\u6bd2\u7269\uff1b<\/span><\/p>\n

\u00b7\u8fde\u63a5\u65b9\u5f0f\uff1a\u5b9a\u70b9\u5076\u8054\uff0c\u4ea7\u751f\u5747\u4e00\u7684\u6297\u4f53\u5076\u8054\u7269\uff1b<\/span><\/p>\n

\u00b7\u6bd2\u7d20\u5206\u5b50\uff1a\u4e00\u822c\u8981\u6c42\u6bd2\u7d20\u6bd2\u6027\u8db3\u591f\u5f3a\uff0c\u8fbe\u5230\u5355\u4f7f\u7528\u4f7fIC50<1nmol\uff1b\u8db3\u591f\u7684\u6c34\u6eb6\u6027\u53ca\u8840\u6e05\u4e2d\u7684\u7a33\u5b9a\u6027\uff1b\u6bd2\u7269\u7684\u4f5c\u7528\u9776\u70b9\u4f4d\u4e8e\u7ec6\u80de\u5185\u3002<\/span><\/p>\n


<\/p>\n

\u5176\u5b9eADC\u836f\u7269\u8fd9\u4e00\u6784\u60f3\u65e9\u5df2\u7ecf\u4e0d\u662f\u4ec0\u4e48\u65b0\u9c9c\u7684\u4e8b\u7269\u3002\u65e9\u57281960s\uff0c\u6587\u732e\u4e2d\u5c31\u62a5\u9053\u4e86\u52a8\u7269\u6a21\u578b\u4e2dADC\u836f\u7269\u7684\u4f7f\u7528\uff1b1980s\uff0c\u5c31\u5f00\u59cb\u8fdb\u884c\u4e86\u57fa\u4e8e\u5c0f\u9f20\u514d\u75ab\u7403\u86cb\u767dG\uff08IgG\uff09\u5206\u5b50\u7684ADC\u7684\u4e34\u5e8a\u8bd5\u9a8c\u3002\u7ec8\u4e8e\u57282000\u5e74\uff0cFDA\u6279\u51c6\u4e86\u7684\u7b2c\u4e00\u4e2aADC\u836f\u7269\u2014\u2014Mylotarg\uff08Gemtuzumab ozogamicin\uff0c\u4e00\u79cd\u4e0e\u5361\u5947\u9709\u7d20\u7ed3\u5408\u7684\u6297CD33\u4eba\u6e90\u5316\u5355\u514b\u9686\u6297\u4f53\uff09\uff0c\u7528\u4e8e\u6cbb\u7597\u6025\u6027\u9ad3\u6027\u767d\u8840\u75c5\u60a3\u8005\u3002<\/span><\/p>\n


<\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"
<\/p>\n

\u7b2c\u4e00\u4ee3\u6297\u4f53\u5076\u8054\u836f\u7269\u2014Mylotarg<\/strong><\/span><\/p>\n


<\/p>\n

\u50cf\u6240\u6709\u65b0\u6280\u672f\u53d1\u5c55\u7684\u8def\u5f84\u4e00\u6837\uff0c\u5927\u591a\u6570\u7684\u7b2c\u4e00\u4ee3\u7684\u4ea7\u54c1\u56e0\u4e3a\u6709\u5f88\u591a\u7f3a\u9677\u6210\u4e86\u70ae\u7070\u3002\u5728\u6279\u51c6\u540e\u4e00\u9879\u7814\u7a76\u4e2d\uff0cMylotarg\uff08\u5982\u4e0b\u56fe1\uff09\u4e0e\u5316\u7597\u76f8\u7ed3\u5408\u5e76\u672a\u8868\u73b0\u51fa\u6bd4\u5355\u72ec\u5316\u7597\u66f4\u9ad8\u7684\u751f\u5b58\u7387\u548c\u66f4\u9ad8\u7684\u81f4\u6b7b\u6bd2\u6027\u7387\uff0c\u8fd9\u5bfc\u81f4\u8f89\u745e\u516c\u53f82010\u5e74\u81ea\u613f\u5c06\u6b64\u8be5\u836f\u7269\u4ece\u5e02\u573a\u4e0a\u64a4\u51fa\u3002\u80cc\u540e\u7684\u539f\u56e0\u53ef\u80fd\u6709\u4ee5\u4e0b\u51e0\u4e2a\uff1a<\/span><\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"<\/p>\n

\u56fe<\/span>2. Mylotarg\uff08<\/span>Gemtuzumab ozogamicin\uff09\u7ed3\u6784\u5f0f<\/span><\/span><\/strong><\/span><\/p>\n


<\/p>\n

\u00b7\u7b2c\u4e00\u4ee3ADC\u836f\u7269Mylotarg\u91c7\u7528\u7684\u662f\u5229\u7528\u6297\u4f53\u4e0a\u7684\u8d56\u6c28\u9178\u548c\u6d3b\u5316\u7684\u7fa7\u9178\u916f\u8fde\u63a5\u5b50\u901a\u8fc7\u9170\u80fa\u952e\u8fde\u63a5\u3002\u4f46\u4e00\u4e2a\u4eba\u6e90\u5316\u6297\u4f53\u5305\u62ec\u4e8680\uff5e90\u4e2a\u8d56\u6c28\u9178\uff0c\u5076\u8054\u7684\u4f4d\u7f6e\u53ef\u80fd\u4f1a\u53d1\u751f\u5728\u6297\u4f53\u8f7b\u94fe\u548c\u91cd\u94fe\u4e0a\u8fd140\u4e2a\u4e0d\u540c\u8d56\u6c28\u9178\u6b8b\u57fa\u4e0a\uff0c\u800c\u4e14\u901a\u8fc7\u8d56\u6c28\u9178\u5076\u8054\u6bcf\u4e2a\u6297\u4f53\u4f1a\u5076\u8054\u4e0a0\uff5e8\u4e2a\u5c0f\u5206\u5b50\u836f\u7269, \u56e0\u6b64\u8fd9\u79cd\u65b9\u6cd5\u751f\u4ea7\u51fa\u6765\u7684ADC\u836f\u7269\u5176\u5b9e\u662f\u4e00\u7ec4\u9ad8\u5ea6\u5f02\u8d28\u6df7\u5408\u7269\uff0c\u8fd9\u4e25\u91cd\u5f71\u54cd\u836f\u7269\u7684PK\/PD\u548c\u6cbb\u7597\u7a97\u53e3\u3002<\/span><\/p>\n


<\/p>\n

\u00b7\u53e6\u5916Mylotarg\u7684\u8fde\u63a5\u5b50\u548c\u6bd2\u7d20\u5206\u5b50\u5229\u7528\u8159\u952e\u76f8\u8fde\uff0c\u8159\u952e\u662f\u4e00\u79cd\u5bf9\u9178\u4e0d\u7a33\u5b9a\u7684\u57fa\u56e2\uff0c\u662f\u4e00\u79cd\u53ef\u65ad\u5f00\u7684\u8fde\u63a5\u952e\uff0c\u4e00\u65e6ADC\u8f6c\u8fd0\u5230\u9178\u6027\u5185\u4f53\uff08pH 5.0-6.0\uff09\u548c\u6eb6\u9176\u4f53\uff08pH\u7ea64.8\uff09\uff0c\u5c31\u4f1a\u901a\u8fc7\u6c34\u89e3\u91ca\u653e\u6e38\u79bb\u836f\u7269\u3002\u4f46\u5b9e\u9645\u4e0a\u5728\u4f53\u5faa\u73af\u4e2d\uff08pH 7.4, 37\u00b0C\uff09\u4e0b\u4e5f\u4f1a\u7f13\u6162\u6c34\u89e3\uff0c\u5bfc\u81f4\u6709\u6bd2\u6709\u6548\u8d1f\u8f7d\u7684\u7f13\u6162\u91ca\u653e\uff0c\u4ea7\u751f\u672a\u9884\u671f\u7684off-target\u6bd2\u6027\u3002<\/span><\/p>\n


<\/p>\n

\u56e0\u6b64\u65e0\u8bba\u662f\u4ece\u8fde\u63a5\u5b50\u3001\u8fde\u63a5\u65b9\u5f0f\u6765\u770b\uff0c\u4ee5Mylotarg\u4e3a\u4ee3\u8868\u7684\u7b2c\u4e00\u4ee3ADC\u836f\u7269\u90fd\u8fd8\u5b58\u5728\u7740\u5f88\u591a\u9700\u8981\u6539\u8fdb\u7684\u5730\u65b9\u3002<\/span><\/p>\n


<\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"
<\/p>\n

\u7b2c\u4e8c\u4ee3\u6297\u4f53\u5076\u8054\u836f\u7269\u2014Kadcyla<\/strong><\/span><\/p>\n


<\/p>\n

\u7f57\u6c0f\u7684Trastuzumab emtansine\uff08Kadcyla\uff09\u4e8e2013\u5e742\u6708\u83b7\u5f97FDA\u6279\u51c6\uff0c\u7528\u4e8e\u6cbb\u7597\u4e4b\u524d\u63a5\u53d7\u8fc7\u66f2\u59a5\u73e0\u5355\u6297\u548c\u7d2b\u6749\u7c7b\u5316\u7597\u5931\u8d25\u7684HER2\u9633\u6027\u4e73\u817a\u764c\u60a3\u8005\u3002Kadcyla\uff0c\u662f\u4e00\u4e2a\u9776\u5411HER2 \u6297\u4f53\u836f\u7269\u5076\u8054\u7269 (ADC)\uff0c\u542b\u4eba\u6e90\u5316\u6297HER2 IgG1\u66f2\u59a5\u73e0\u5355\u6297(Trastuzumab)\u548c\u5fae\u7ba1\u6291\u5236\u5242DM1(\u7f8e\u767b\u7d20maytansine\u884d\u751f\u7269)\uff0c\u4e24\u8005\u901a\u8fc7\u7a33\u5b9a\u786b\u919a\u8fde\u63a5\u7269(MCC)\u5171\u4ef7\u8fde\u63a5\uff0c\u5176\u7ed3\u6784\u5982\u4e0b\u56fe3\u6240\u793a\uff1a<\/span><\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"<\/p>\n

\u56fe<\/span>3. Trastuzumab emtansine\uff08<\/span>Kadcyla\uff09\u7ed3\u6784\u5f0f<\/span><\/span><\/strong><\/span><\/p>\n


<\/p>\n

\u76f8\u8f83\u4e8e\u7b2c\u4e00\u4ee3ADC\u836f\u7269\uff0cKadcyla\u6709\u4e86\u4ee5\u4e0b\u65b9\u9762\u7684\u63d0\u9ad8\uff1a<\/span><\/p>\n


<\/p>\n

\u00b7Kadcyla\u91c7\u7528\u4e86\u4e0d\u53ef\u65ad\u88c2\u7684\u786b\u919a\u8fde\u63a5\u7269(MCC)\u5171\u4ef7\u5c06\u6297\u4f53\u548c\u6bd2\u7d20\u8fde\u63a5\u3002\u7814\u7a76\u8868\u660e\uff0c\u4e0e\u4e8c\u786b\u5316\u7269\uff08\u53ef\u65ad\u5f00\uff09\u8fde\u63a5\u7684\u7f8e\u767b\u7d20\u6784\u5efa\u4f53\u76f8\u6bd4\uff0c\u5728\u8840\u6db2\u5faa\u73af\u4e2d\u7a33\u5b9a\u6027\u8f83\u597d\uff0c\u56e0\u6b64\u8010\u53d7\u6027\u8f83\u597d\uff0c\u660e\u663e\u7684\u6539\u5584\u4e86\u7ec6\u80de\u6bd2\u6027\u836f\u7269\u7684\u6cbb\u7597\u6307\u6570\u3002<\/span><\/p>\n


<\/p>\n

\u00b7Kadcyla\u5728\u9776\u7ec6\u80de\u5185\u541e\u540e\uff0c\u6297\u4f53\u88ab\u6c34\u89e3\u4e3a\u6c28\u57fa\u9178\uff0cADC\u836f\u7269\u7684\u6d3b\u6027\u4ee3\u8c22\u4ea7\u7269\u4e3a\u8d56\u6c28\u9178-MCC-DM1\uff0c\u56e0\u4e3a\u5176\u5e26\u7535\u4eb2\u6c34\u6027\u3001\u9776\u7ec6\u80de\u88c2\u89e3\u540e\uff0c\u4e0d\u4f1a\u5bf9\u5468\u56f4\u7684\u7ec6\u80de\u4ea7\u751f\u6740\u4f24\u4f5c\u7528\u3002<\/span><\/p>\n


<\/p>\n

\u4f5c\u4e3a\u7b2c\u4e8c\u4ee3\u7684ADC\u836f\u7269\uff0cKadcyla\u65e0\u7591\u662f\u6210\u529f\u7684\uff0cEMILIA\u4e34\u5e8a\u8bd5\u9a8c\u8868\u793a\uff1a\u5165\u7ec4\u4e86991\u540d\u5df2\u7ecf\u81f3\u5c11\u63a5\u53d7\u8fc7\u66f2\u59a5\u73e0\u5355\u6297\u3001\u7d2b\u6749\u9187\u6cbb\u7597\u540e\u5931\u8d25\u7684\u665a\u671fHER2\u9633\u6027\u4e73\u817a\u764c\u60a3\u8005\uff0c\u4e00\u7ec4\u63a5\u53d7T-DM1\u6cbb\u7597\uff0c\u4e00\u7ec4\u63a5\u53d7\u62c9\u5e15\u66ff\u5c3c+\u5361\u57f9\u4ed6\u6ee8\u6cbb\u7597\u3002\u7ed3\u679c\u663e\u793a\uff1aT-DM1\u76f8\u6bd4\u4e8e\u62c9\u5e15\u66ff\u5c3c+\u5361\u57f9\u4ed6\u6ee8\uff0c\u6709\u6548\u7387\u66f4\u9ad8\uff0843.6% vs 30.8%\uff09\u3001\u4e2d\u4f4d\u65e0\u75be\u75c5\u8fdb\u5c55\u65f6\u95f4PFS\u66f4\u957f\uff089.6\u4e2a\u6708 vs 6.4\u4e2a\u6708\uff09\uff0c\u4e2d\u4f4d\u603b\u751f\u5b58\u671fOS\u66f4\u957f\uff0830.9\u4e2a\u6708 vs 25.1\u4e2a\u6708\uff09\uff0c\u526f\u4f5c\u7528\u66f4\u5c0f\uff083-4\u7ea7\u4e0d\u826f\u53cd\u5e94\u53d1\u751f\u7387\u4e3a41% vs 57%\uff09\u3002<\/span><\/p>\n


<\/p>\n

\u4f46Kadcyla\u5e76\u975e\u662f\u5b8c\u7f8e\u7684\uff0cKadcyla\u4ecd\u91c7\u7528\u7684\u662f\u5229\u7528\u6297\u4f53\u4e0a\u7684\u8d56\u6c28\u9178\u548c\u6d3b\u5316\u7684\u7fa7\u9178\u916f\u8fde\u63a5\u5b50\u901a\u8fc7\u9170\u80fa\u952e\u8fde\u63a5\u3002\u5f97\u5230\u7684\u4ecd\u7136\u662f0\uff5e8\u4e2a\u8f7d\u836f\u91cf\u7684\u5904\u4e8e\u4e0d\u540c\u4f4d\u7f6e\u7684\u975e\u5747\u4e00ADC\u836f\u7269\u3002\u8fd9\u4ecd\u7136\u6781\u5927\u7684\u5f71\u54cd\u4e86\u836f\u7269\u7684\u836f\u4ee3\u52a8\u6027\u8d28\u548c\u6cbb\u7597\u7a97\u53e3\u3002<\/span><\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"<\/p>\n


<\/p>\n

\u6240\u4ee5\uff0c\u89e3\u51b3\u4e0a\u8ff0\u95ee\u9898\u5c31\u662f\u4e0b\u4e00\u4ee3ADCs\u53d1\u5c55\u7684\u76ee\u6807\uff0c\u89e3\u51b3\u7684\u95ee\u9898\u7b56\u7565\u662f\u5b9a\u70b9\u5076\u8054\uff0c\u901a\u8fc7\u5b9a\u70b9\u5076\u8054\u624d\u4f1a\u5f97\u5230\u5747\u4e00\u7684\u9ad8\u8d28\u91cf\u7684\u65b0\u4e00\u4ee3ADCs\u3002<\/span><\/p>\n


<\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"
<\/p>\n

\u7b2c\u4e09\u4ee3\u6297\u4f53\u5076\u8054\u836f\u7269<\/strong><\/span><\/p>\n


<\/p>\n

\u76ee\u524d\u7ecf\u8fc7\u7814\u7a76\u8005\u7684\u5927\u91cf\u7684\u5de5\u4f5c\uff0c\u5df2\u7ecf\u5f00\u53d1\u51fa\u4e86\u591a\u79cd\u65b9\u6cd5\u53ef\u5b9e\u73b0\u7ec6\u80de\u6bd2\u6027\u836f\u7269\u4e0e\u786e\u5b9a\u4f4d\u70b9\u548c\u5316\u5b66\u8ba1\u91cf\u7684\u6297\u4f53\u7684\u5076\u8054\u3002\u7b14\u8005\u5217\u4e3e\u4e3b\u8981\u7684\u51e0\u79cd\u65b9\u5f0f\u5982\u4e0b\uff1a
<\/span><\/p>\n


<\/p>\n

1.Thiomab\u6280\u672f\uff1aThiomab\u6280\u672f\u6700\u65e9\u7531Genentech\u516c\u53f8\u7684 Junutula\u7b49\u62a5\u9053, \u4ed6\u4eec\u91c7\u7528\u57fa\u56e0\u5de5\u7a0b\u6280\u672f\u5728\u66f2\u59a5\u73e0\u5355\u6297(trastuzumab)\u7684\u8f7b\u94feV110C \u548c\u91cd\u94feA114C \u7279\u5b9a\u4f4d\u7f6e\u5904\u63d2\u5165\u534a\u80f1\u6c28\u9178\u6b8b\u57fa,  \u7136\u540e\u5c06\u534a\u80f1\u6c28\u9178\u4e0a\u7684\u5def\u57fa\u548c\u5355\u7532\u57fa auristatin E (MMAE)  \u5076\u8054\uff0c\u5408\u6210\u4e86\u4f4d\u70b9\u4e13\u4e00\u7684\u6297\u4f53\u2212\u836f\u7269\u5076\u8054\u7269\uff0c\u5176\u4e2d\u836f\u6297\u6bd4\u4e3a 2 \u7684\u4ea7\u7269\u9ad8\u8fbe 92.1%\u3002<\/span><\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"<\/p>\n


<\/p>\n

2.ThioBridge\u6280\u672f\uff1a\u5c06\u5355\u6297\u672c\u8eab\u7684\u4e8c\u786b\u952e\u8fd8\u539f\uff0c\u5229\u7528\u4e8c\u6eb4\uff08\u6216\u4e8c\u78fa\u9178\u76d0\uff09\u8bd5\u5242\u4e0e\u8fd8\u539f\u7684\u94fe\u95f4\u4e8c\u786b\u5316\u7269\u53cd\u5e94\uff0c\u4ee5\u63d0\u4f9b\u91cd\u65b0\u6865\u63a5\u7684mAb\uff0c\u5f97\u5230\u4e3b\u8981\u7684\u662f\u836f\u6297\u6bd4\u4e3a4\u7684\u4ea7\u7269\uff1a<\/span><\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"<\/p>\n


<\/p>\n

3.\u5f15\u5165\u975e\u5929\u7136\u6c28\u57fa\u9178\u6cd5\uff1a\u8be5\u65b9\u6cd5\u4f7f\u7528\u4e00\u4e2a\u8fdb\u5316\u8fc7\u7684\u53ef\u4ee5\u7279\u5f02\u6027\u8bc6\u522b\u975e\u5929\u7136\u6c28\u57fa\u9178\u7684\u916a\u6c28\u9170-t RNA\/\u6c28\u9170-t RNA \u5408\u6210\u9176,  \u901a\u8fc7\u4e2d\u56fd\u4ed3\u9f20\u5375\u5de2\u7ec6\u80de(CHO) \u8f6c\u67d3\u4ee5\u4ee3\u66ff\u7425\u73c0\u5bc6\u7801\u5b50\u7684\u7b2c21\u4e2a\u6c28\u57fa\u9178,  \u6240\u5f97\u7ec6\u80de\u5373\u53ef\u7528\u4e8e\u5408\u6210\u5e26\u6709\u57fa\u56e0\u8bd1\u7801\u2014\u2014\u5bf9\u4e59\u9170\u82ef\u4e19\u6c28\u9178\u6b8b\u57fa\u7684\u5404\u79cd\u6297\u4f53\uff0c\u7136\u540e\u5728\u4e8e\u7f9f\u80fa\u53d1\u751f\u809f\u5316\u53cd\u5e94\uff0c\u5f97\u5230\u4e3b\u8981\u7684\u662f\u836f\u6297\u6bd4\u4e3a2\u7684\u4ea7\u7269\uff1a<\/span><\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"<\/p>\n


<\/p>\n

4.\u9176\u50ac\u5316\u6cd5\uff1a\u5982\u5206\u9009\u9176 A (Srt A)\u662f\u4e00\u79cd\u5177\u6709\u819c\u7ed3\u5408\u5def\u57fa\u8f6c\u80bd\u9176\u50ac\u5316\u529f\u80fd\u7684\u9176,  \u5b83\u80fd\u8bc6\u522b\u86cb\u767d\u4e2d\u7684\u4e3b\u8981\u5e8f\u5217 LPETG, \u88c2\u89e3\u82cf\u6c28\u9178(threonine) \u548c\u7518\u6c28\u9178\u95f4\u7684\u80bd\u952e\u540e\u5f62\u6210\u4e00\u79cd\u7a33\u5b9a\u7684\u4e2d\u95f4\u4f53,  \u518d\u901a\u8fc7\u786b\u916f\u952e\u628a Srt A\u4e2d\u7684\u5def\u57fa\u8fde\u63a5\u5230\u82cf\u6c28\u9178\u7fa7\u57fa\u4e0a\u3002<\/span><\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"<\/p>\n


<\/p>\n

\u5728\u7b14\u8005\u770b\u6765\uff0cADC\u836f\u7269\u4ece\u8bbe\u8ba1\u7684\u7406\u5ff5\u4e0a\u6765\u8bf4\uff0c\u5176\u5b9e\u662f\u4e3a\u4e86\u6539\u8fdb\u5316\u7597\u836f\u7269\u3002\u56e0\u4e3a\u4f20\u7edf\u7684\u5316\u7597\u836f\u7269\u4e0d\u5177\u5907\u8bc6\u522b\u80bf\u7624\u7279\u5f02\u6027\uff0c\u800c\u6297\u4f53\u5c06\u7ec6\u80de\u6bd2\u6027\u836f\u7269\u9776\u5411\u9012\u9001\u81f3\u764c\u7ec6\u80de\u589e\u52a0\u4e86\u5230\u8fbe\u80bf\u7624\u7684\u836f\u7269\u5206\u5b50\u7684\u767e\u5206\u6bd4\uff0c\u4ece\u800c\u964d\u4f4e\u5316\u7597\u836f\u6700\u5c0f\u6709\u6548\u5242\u91cf\u5e76\u589e\u52a0\u6700\u5927\u8010\u53d7\u5242\u91cf\u3002\u4f46\u7b2c\u4e00\u4ee3\u548c\u7b2c\u4e8c\u4ee3ADC\u836f\u7269\u56e0\u4e3a\u8fde\u63a5\u5b50\u548c\u8fde\u63a5\u65b9\u5f0f\u7684\u539f\u56e0\uff0c\u4ecd\u7136\u5177\u6709\u8131\u9776\u6bd2\u6027\u548c\u4e0e\u4e0d\u5747\u4e00\u7684\u6297\u4f53\u5076\u8054\u7269\uff0c\u4f7f\u5f97\u8fd9\u4e9b\u4ed6\u4eec\u7684\u6cbb\u7597\u7a97\u53e3\u4ecd\u7136\u5f88\u7a84\u3002\u5982\u4eca\uff0c\u79d1\u5b66\u5bb6\u4eec\u5df2\u7ecf\u5f00\u53d1\u51fa\u4e86\u591a\u79cd\u7684\u5b9a\u70b9\u5076\u8054\u7684\u65b9\u5f0f\u3001\u8fde\u63a5\u5b50\u3001\u6bd2\u7d20\u5206\u5b50\uff0c ADC\u836f\u7269\u7684\u6cbb\u7597\u7a97\u53e3\u5df2\u7ecf\u5f97\u5230\u4e86\u6781\u5927\u7684\u6539\u5584\u3002<\/span><\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"<\/p>\n


<\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"
<\/p>\n

\u56fd\u5185\u5916ADC\u836f\u7269\u7814\u53d1\u8fdb\u5c55<\/strong><\/span><\/p>\n


<\/p>\n

\u622a\u81f3\u76ee\u524dFDA\u5df2\u7ecf\u6279\u51c6\u4e86\u56db\u4e2aADC\u836f\u7269\u4e0a\u5e02\uff0c\u6709\u4e00\u6b3e\u836f\u7269\u5904\u4e8e\u65b0\u836f\u7533\u8bf7\u9636\u6bb5\uff0c\u8fd110\u6b3e\u836f\u7269\u5904\u4e8e\u4e34\u5e8aIII\u671f\uff0c\u6709\u8d85\u8fc760\u4e2a\u836f\u7269\u9488\u5bf9\u591a\u79cd\u9776\u70b9\u5904\u4e8e\u4e34\u5e8a\u7684\u4e0d\u540c\u9636\u6bb5\u3002IMMU-132\u5728\u4e09\u9634\u4e73\u817a\u764c\u548c\u5c0f\u7ec6\u80de\u80ba\u764c\uff0cenfortumab vedotin\u5728\u665a\u671f\u6216\u8f6c\u79fb\u6027\u5c3f\u8def\u4e0a\u76ae\u764c\u3001Mirvetuximab soravtansine\u5728\u6cbb\u7597\u5375\u5de2\u764c\u3001\u4ee5\u53caGSK2857916\u5728\u591a\u53d1\u6027\u9aa8\u9ad3\u7624\uff0c\u7b49\u7b49\u8fd9\u4e9b\u5728\u7814\u7684ADC\u836f\u7269\u90fd\u7ed9\u7814\u7a76\u8005\u7559\u4e0b\u4e86\u6df1\u523b\u7684\u5370\u8c61\u3002\u73b0\u5c06\u56fd\u5916\u4e34\u5e8a\u5728\u7814ADC\u836f\u7269\u7684\u9776\u70b9\u3001\u8fde\u63a5\u65b9\u5f0f\u3001\u6bd2\u7d20\u7edf\u8ba1\u5982\u4e0b\uff1a<\/span><\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"<\/p>\n


<\/p>\n

\u548c\u56fd\u5916\u76f8\u540c\u7684\u662f\uff0c\u56fd\u5185\u4f17\u591a\u836f\u4f01\u7eb7\u7eb7\u5e03\u5c40ADC\u836f\u7269\u9886\u57df\uff0c\u5982\uff1a\u6d59\u6c5f\u533b\u836f\uff08\u65b0\u7801\u751f\u7269\uff09\u3001\u6052\u745e\u3001\u4e3d\u73e0\u5355\u6297\u3001\u7f8e\u96c5\u73c2\uff08\u4e50\u666e\uff09\u3001\u590d\u661f\u533b\u836f\u3001\u4e0a\u6d77\u533b\u836f\u3001\u79d1\u4f26\u836f\u4e1a\u3001\u534e\u6d77\u836f\u4e1a\u3001\u77f3\u836f\u96c6\u56e2\u3001\u5609\u548c\u751f\u7269\u3001\u4e1c\u66dc\u836f\u4e1a\u3001\u542f\u5fb7\u751f\u7269\u3001\u540c\u5b9c\u533b\u836f\u3001\u5929\u58eb\u529b\u3001\u7279\u745e\u601d\u3001\u767e\u5965\u6cf0\u751f\u7269\u3001\u9f50\u9c81\u5236\u836f\u3001\u8363\u660c\u751f\u7269\u7b49\u3002\u4f46\u548c\u56fd\u5916\u4e0d\u540c\u7684\u662f\uff0c\u56fd\u5185\u836f\u4f01\u5927\u591a\u624e\u5806\u5f00\u53d1HER2\u8fd9\u4e2a\u9776\u70b9\uff0c\u4e3b\u8981\u662f\u4eff\u5236\u5df2\u4e0a\u5e02\u7684Kadcyla\uff0c\u7ade\u4e89\u5341\u5206\u6fc0\u70c8\u3002\u56fd\u5185\u836f\u4f01ADC\u5728\u7814\u836f\u7269\u7edf\u8ba1\u5982\u4e0b\uff1a<\/span><\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"<\/p>\n


<\/p>\n


<\/p>\n

\"\u6297\u4f53\u5076\u8054\u836f\u7269\uff08ADC\uff09\u7684\u8fdb\u9636\u4e4b\u8def\"
<\/p>\n

\u603b\u7ed3<\/strong><\/span><\/p>\n


<\/p>\n

ADC\u9886\u57df\u5728\u8fc7\u53bb\u51e0\u5e74\u4e00\u76f4\u5904\u4e8e\u4f4e\u8c37\u671f\uff0c\u57282017\u5e74\u4ee5\u524d\uff0c\u5168\u7403\u4ec5\u6709\u4e24\u6b3e\u4e0a\u5e02\u836f\u7269\u3002\u4f46\u5f97\u76ca\u4e8e\u5b9a\u70b9\u5076\u8054\u6280\u672f\u7684\u53d1\u5c55\u3001\u66f4\u6709\u6548\u7684\u5c0f\u5206\u5b50\u7ec6\u80de\u6bd2\u7d20\u3001\u4ee5\u53ca\u66f4\u52a0\u5b8c\u5584\u7684\u6297\u4f53\u4fee\u9970\u6280\u672f\uff0c\u4f7f\u5f97ADC\u9886\u57df\u5f00\u59cb\u9010\u6e10\u56de\u6696\u3002\u4ece2017\u5e74\u5f00\u59cb\uff0c\u73b0\u6709\u4e0a\u5e02\u4ea7\u54c1\u9002\u5e94\u75c7\u9010\u6b65\u589e\u52a0\u3001\u66fe\u7ecf\u5386\u9000\u5e02\u7684\u7b2c\u4e00\u4e2aADC\u836f\u7269Mylotarg\u5728\u8c03\u6574\u4e86\u7ed9\u836f\u5242\u91cf\u3001\u9891\u7387\u548c\u9002\u7528\u60a3\u8005\uff0c\u53c8\u91cd\u65b0\u4e0a\u5e02\uff0c\u540c\u65f6\u53c8\u6709\u65b0\u7684\u4ea7\u54c1(\u8f89\u745eBesponsa)\u4e0a\u5e02\u7b49\u30022018\u5e745\u6708\uff0c\u56fd\u5bb6\u836f\u76d1\u5c40\u5728\u4e00\u4e2a\u6708\u5185\u6279\u51c6\u4e86\u516d\u6b3eADC\u836f\u7269\u7684\u4e34\u5e8a\u8bd5\u9a8c\u7533\u8bf7\uff0c\u8fd9\u4e9b\u90fd\u7ed9ADC\u836f\u7269\u7814\u53d1\u9886\u57df\u6253\u4e86\u4e00\u5242\u5f3a\u5fc3\u9488\u3002<\/span><\/p>\n


<\/p>\n

\u672c\u6587\u7740\u91cd\u8bb2\u4e86ADC\u836f\u7269\u4ece\u7b2c\u4e00\u4ee3\u5230\u7b2c\u4e09\u4ee3\u7684\u8fdb\u9636\u4e4b\u8def\uff0c\u4e3b\u8981\u4ecelinker\u7684\u89d2\u5ea6\u6765\u9610\u8ff0\u8fd9\u4e00\u6539\u8fdb\u3002\u76ee\u524d\u7684\u5b9a\u70b9\u5076\u8054\u6280\u672f\u548c\u8fde\u63a5\u65b9\u5f0f\u5df2\u7ecf\u80fd\u4fdd\u6301\u6bd2\u7d20\u5206\u5b50\u5728\u8840\u6db2\u4e2d\u7684\u7a33\u5b9a\u6027\u548cADC\u836f\u7269\u7684\u5747\u4e00\u6027\u3002\u4f46\u5b9e\u9645\u4e0aADC\u836f\u7269\u7684\u6311\u6218\u8fd8\u8fdc\u4e0d\u6b62\u4e8e\u6b64\uff0c\u6bd4\u5982\uff1a<\/span><\/p>\n


<\/p>\n

\u00b7\u65b0\u5f00\u53d1\u7684ADC\u836f\u7269\u9488\u5bf9\u7684\u75be\u75c5\u5206\u5b50\u673a\u7406\u4e86\u89e3\u4e0d\u8db3\u6216\u8005\u5408\u9002\u7684\u52a8\u7269\u6a21\u578b\u6bd4\u8f83\u6b20\u7f3a\u3002\u6bd4\u5982\uff0c\u6709\u4e9b\u4ee5\u4e3a\u662f\u9488\u5bf9\u80bf\u7624\u7279\u5f02\u6027\u5f00\u53d1\u7684\u9776\u70b9\uff0c\u4f46\u4e0a\u4e86\u4e34\u5e8a\u540e\uff0c\u624d\u53d1\u73b0\u90e8\u5206\u7684\u6b63\u5e38\u7ec4\u7ec7\u4e5f\u8868\u8fbe\uff0c\u9020\u6210\u672a\u9884\u671f\u7684\u6bd2\u6027\u3002\u6216\u8005\u4e34\u5e8a\u524d\u52a8\u7269\u6a21\u578b\u5bf9\u67d0\u4e2a\u9776\u70b9\u7684\u8868\u8fbe\u6c34\u5e73\u8fdc\u8fdc\u9ad8\u4e8e\u75c5\u4eba\u5b9e\u9645\u6c34\u5e73\uff0c\u5bfc\u81f4\u4e34\u5e8a\u524d\u8868\u73b0\u5f88\u597d\u7684\u836f\u7269\u4e0a\u4e86\u4e34\u5e8a\u540e\uff0c\u7f3a\u4e4f\u6709\u6548\u6027\u3002<\/span><\/p>\n


<\/p>\n

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

1.Beck, Alain, et al. “Strategies and challenges for the next generation of antibody\u2013drug conjugates.” Nature reviews Drug discovery 16.5 (2017): 315.<\/span><\/span><\/p>\n

2.Sau, Samaresh, et al. “Advances in antibody\u2013drug conjugates: a new era of targeted cancer therapy.” Drug discovery today (2017).<\/span><\/span><\/p>\n

3.Nagayama, Aiko, et al. “Antibody\u2013Drug Conjugates for the Treatment of Solid Tumors: Clinical Experience and Latest Developments.” Targeted oncology 12.6 (2017): 719-739.<\/span><\/span><\/p>\n

4.Dan, Nirnoy, et al. “Antibody-drug conjugates for cancer therapy: chemistry to clinical implications.” Pharmaceuticals 11.2 (2018): 32.<\/span><\/span><\/p>\n

5.Zhou, Qun. “Site-specific antibody conjugation for ADC and beyond.” Biomedicines 5.4 (2017): 64.<\/span><\/span><\/p>\n


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\u5fc3\u4f3c\u5e73\u539f\u8d70\u9a6c\uff0c\u6613\u653e\u96be\u6536\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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<\/p>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section><\/div>\n","protected":false},"excerpt":{"rendered":"

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