title: Prostate-cancer-targeted N-(2-hydroxypropyl)methacrylamide copolymer/docetaxel conjugates.
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 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.
authors.affiliation: Department of Pharmaceutics and Pharmaceutical Chemistry/CCCD, University of Utah, Salt Lake City, UT 84112, USA.
authors.forename: Jihua
authors.initials: J
authors.lastname: Liu
authors.forename: Pavla
authors.initials: P
authors.lastname: Kopečková
authors.forename: Huaizhong
authors.initials: H
authors.lastname: Pan
authors.forename: Monika
authors.initials: M
authors.lastname: Sima
authors.forename: Patrick
authors.initials: P
authors.lastname: Bühler
authors.forename: Philipp
authors.initials: P
authors.lastname: Wolf
authors.forename: Ursula
authors.initials: U
authors.lastname: Elsässer-Beile
authors.forename: Jindřich
authors.initials: J
authors.lastname: Kopeček
mesh_terms: D000178:Acrylamides / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D000818:Animals; D000911:Antibodies, Monoclonal / Q000737:chemistry* / Q000276:immunology; D000954:Antigens, Surface / Q000276:immunology; D000077143:Docetaxel; D016503:Drug Delivery Systems; D043425:Glutamate Carboxypeptidase II / Q000276:immunology; D006801:Humans; D018796:Immunoconjugates / Q000737:chemistry / Q000493:pharmacokinetics*; D007457:Iodine Radioisotopes; D008297:Male; D051379:Mice; D008819:Mice, Nude; D011108:Polymers / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D011471:Prostatic Neoplasms / Q000188:drug therapy / Q000276:immunology / Q000473:pathology; D043823:Taxoids / Q000737:chemistry* / Q000493:pharmacokinetics; D014018:Tissue Distribution; D023041:Xenograft Model Antitumor Assays
chemical_list: D000178:Acrylamides; D000911:Antibodies, Monoclonal; D000954:Antigens, Surface; D018796:Immunoconjugates; D007457:Iodine Radioisotopes; D011108:Polymers; D043823:Taxoids; D000077143:Docetaxel; C473848:FOLH1 protein, human; D043425:Glutamate Carboxypeptidase II; C032976:N-(2-hydroxypropyl)methacrylamide