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Prostate‐Cancer‐Targeted N‐ (2‐Hydroxypropyl)methacrylamide Copolymer/Docetaxel Conjugates
Author(s) -
Liu Jihua,
Kopečková Pavla,
Pan Huaizhong,
Sima Monika,
Bühler Patrick,
Wolf Philipp,
ElsässerBeile Ursula,
Kopeček Jindřich
Publication year - 2012
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201100340
Subject(s) - biodistribution , conjugate , chemistry , prostate cancer , pharmacokinetics , methacrylamide , docetaxel , cancer research , in vivo , prostate , monoclonal antibody , cancer , pharmacology , medicine , antibody , copolymer , biochemistry , in vitro , immunology , biology , mathematical analysis , acrylamide , mathematics , microbiology and biotechnology , organic chemistry , polymer
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.