Prostate-cancer-targeted N-(2-hydroxypropyl)methacrylamide copolymer/docetaxel conjugates.
Prostate-cancer-targeted N-(2-hydroxypropyl)methacrylamide copolymer/docetaxel conjugates.
复制标题
DOI：
10.1002/mabi.201100340
复制
发表时间：
2012-03
影响因子：
4.6
通讯作者：
Kopeček J
中科院分区：
文献类型：
--
作者：
Liu J;Kopečková P;Pan H;Sima M;Bühler P;Wolf P;Elsässer-Beile U;Kopeček J
在携带前列腺癌C4-2异种移植物的裸鼠中评价前列腺癌靶向HPMA共聚物/DTX缀合物的生物分布、药代动力学和功效。PSMA特异性单克隆抗体3F/11用作靶向部分。对照缀合物含有非特异性IgG或不含IgG。对于靶向缀合物，肿瘤蓄积与总背景器官（心、肺、肾、肝、脾和血液）蓄积的比率随时间显著增加，并且48小时的比率比6小时高7倍。对缀合物在体内的功效的初步评价表明，所有HPMA共聚物/DTX缀合物都具有肿瘤生长抑制作用。
Biodistribution, pharmacokinetics, and efficacy of prostate-cancer-targeted HPMA copolymer/DTX conjugates are evaluated in nude mice bearing prostate cancer C4-2 xenografts. PSMA-specific monoclonal antibodies 3F/11 are used as the targeting moiety. Control conjugates contain either non-specific IgG or no IgG. The ratios of tumor accumulation to total background organs (heart, lung, kidney, liver, spleen and blood) accumulation increase substantially with time for the targeted conjugate, and the ratio at 48 h is 7-fold higher than that at 6 h. Preliminary evaluation of the efficacy of the conjugates in vivo show tumor growth inhibition for all HPMA copolymer/DTX conjugates.