PSMA-targeted dendrimers: A patent evaluation (WO2012078534) Journal Article


Authors: Akhtar, N. H.; Osborne, J. R.; Fareedy, S. B.; Tagawa, S. T.
Article Title: PSMA-targeted dendrimers: A patent evaluation (WO2012078534)
Abstract: Prostate-specific membrane antigen (PSMA) is a cell surface protein expressed primarily in prostate cancer and solid tumor neovasculature. PSMA has been a target for both imaging and therapeutic investigations due to its increased expression in advanced disease and in prostate cancer patients receiving hormonal therapy. The recent approval of new androgen receptor pathway targeted drugs for prostate cancer has sharply increased this interest in creating novel probes to measure this disease-specific biomarker. Monoclonal antibodies and small molecules targeting PSMA, however, have been investigated for diagnostic and therapeutic purposes, with only limited success. In fact, only one agent (monoclonal antibody agent-capromab pendetide) has been FDA-approved for human use. PSMA-targeting dendrimers may provide a targeting method that might maintain the specificity of monoclonal antibodies, achieve high levels of tumor concentration (similar to small molecule antagonist ligands) and avoid accumulation in non-target sites of PSMA expression (such as renal tubules). The current patent application provides theoretical evidence for the advantage of PSMA-targeting dendrimers with in vitro data for PSMA binding, but lacks sufficient preclinical animal binding, dosimetry and toxicology data. © 2013 Informa UK, Ltd.
Keywords: unclassified drug; doxorubicin; nonhuman; antineoplastic agents; drug targeting; positron emission tomography; lymph node metastasis; binding affinity; antigen expression; animals; tumor markers, biological; drug design; monoclonal antibody; cancer hormone therapy; prostate cancer; drug delivery systems; prostatic neoplasms; capromab pendetide in 111; prostate specific membrane antigen; antibodies, monoclonal; tissue distribution; radiopharmaceutical agent; androgen receptor; antigen binding; single photon emission computer tomography; glutamic acid; macrogol; synthesis; lysine; glutamate carboxypeptidase ii; antigens, surface; urea; kidney tubule; edetic acid; prostate-specific membrane antigen; dendrimers; dendrimer; polyamidoamine; targeted theragnostic; 2 [3 [1 carboxy 5 [(6 fluoro pyridine 3 carbonyl)amino]pentyl]ureido]pentanedioic acid f 18; 2,2 bis(hydroxymethyl)propionic acid; patents as topic
Journal Title: Expert Opinion on Therapeutic Patents
Volume: 23
Issue: 5
ISSN: 1354-3776
Publisher: Informa Healthcare  
Date Published: 2013-05-01
Start Page: 665
End Page: 668
Language: English
DOI: 10.1517/13543776.2013.789501
PROVIDER: scopus
PUBMED: 23581819
DOI/URL:
Notes: --- - "Export Date: 3 June 2013" - "CODEN: EOTPE" - "Source: Scopus"
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  1. Joseph R Osborne
    61 Osborne