Department of Pharmaceutics and Pharmaceutical Chemistry/CCCD, University of Utah, Salt Lake City, UT 84112, USA.
Macromol Biosci. 2012 Mar;12(3):412-22. doi: 10.1002/mabi.201100340.
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 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.
在荷前列腺癌 C4-2 移植瘤 nude 小鼠中评价了前列腺癌靶向 HPMA 共聚物/多西紫杉醇偶联物的生物分布、药代动力学和疗效。PSMA 特异性单克隆抗体 3F/11 用作靶向部分。与靶向偶联物相比,对照偶联物的肿瘤积累到总背景器官(心、肺、肾、肝、脾和血液)的积累随时间显著增加,48 h 的比值是 6 h 的 7 倍。体内偶联物疗效的初步评价表明,所有 HPMA 共聚物/多西紫杉醇偶联物均能抑制肿瘤生长。