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: Jihua Liu, Pavla Kopečková, Huaizhong Pan, Monika Sima, Patrick Bühler, Philipp Wolf, Ursula Elsässer-Beile, Jindřich Kopeček
• Journal: Macromolecular bioscience (Macromol Biosci) Vol. 12 Issue 3 Pg. 412-22 (Mar 2012) ISSN: 1616-5195 [Electronic] Germany
• PMID: 22493797 (Publication Type: Journal Article, Research Support, N.I.H., Extramural)

Chemical References

• Acrylamides
• Antibodies, Monoclonal
• Antigens, Surface
• Immunoconjugates
• Iodine Radioisotopes
• Polymers
• Taxoids
• Docetaxel
• FOLH1 protein, human
• Glutamate Carboxypeptidase II
• N-(2-hydroxypropyl)methacrylamide

Topics

• Acrylamides (chemical synthesis, pharmacokinetics)
• Animals
• Antibodies, Monoclonal (chemistry, immunology)
• Antigens, Surface (immunology)
• Docetaxel
• Drug Delivery Systems
• Glutamate Carboxypeptidase II (immunology)
• Humans
• Immunoconjugates (chemistry, pharmacokinetics)
• Iodine Radioisotopes
• Male
• Mice
• Mice, Nude
• Polymers (chemical synthesis, pharmacokinetics)
• Prostatic Neoplasms (drug therapy, immunology, pathology)
• Taxoids (chemistry, pharmacokinetics)
• Tissue Distribution
• Xenograft Model Antitumor Assays