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Prostate‐Cancer‐Targeted N‐(2‐Hydroxypropyl)methacrylamide Copolymer/Docetaxel Conjugates
Authors:Jihua Liu  Pavla Kopečková  Huaizhong Pan  Monika Sima  Patrick Bühler  Philipp Wolf  Ursula Elsässer‐Beile  Jindřich Kopeček
Affiliation:1. Department of Pharmaceutics and Pharmaceutical Chemistry/CCCD, University of Utah, Salt Lake City, UT84112, USA;2. Department of Bioengineering, University of Utah, Salt Lake City, UT84112, USA;3. Department of Urology, Experimental Urology, University of Freiburg, Freiburg, Germany
Abstract: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.
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Keywords:antibody 3F/11  biodistribution  prostate cancer treatment  targeted HPMA copolymer/docetaxel conjugates  tumor accumulation
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