1025796-31-9Relevant articles and documents
A Bivalent Inhibitor of Prostate Specific Membrane Antigen Radiolabeled with Copper-64 with High Tumor Uptake and Retention
Zia, Nicholas A.,Cullinane, Carleen,Van Zuylekom, Jessica K.,Waldeck, Kelly,McInnes, Lachlan E.,Buncic, Gojko,Haskali, Mohammad B.,Roselt, Peter D.,Hicks, Rodney J.,Donnelly, Paul S.
, p. 14991 - 14994 (2019)
Molecules containing lysine-ureido-glutamate functional groups bind to the active site of prostate specific membrane antigen, which is overexpressed in prostate cancer. To prepare copper radiopharmaceuticals for the diagnosis and therapy of prostate cancer, macrobicyclic sarcophagine ligands tethered to either one or two lysine-ureido-glutamate functional groups through an appropriate linker have been prepared. Sarcophagine ligands can be readily radiolabeled with positron-emitting copper-64 at room temperature. The bivalent agent, in which two targeting groups are tethered to a single copper complex, dramatically outperforms the monomeric agent with respect to tumor uptake and retention. The high tumor uptake, low background, and prolonged tumor retention, even at 24 hours post injection, suggest the bivalent agent is a promising diagnostic for prostate cancer and could be used for prospective dosimetry for therapy with a copper-67 variant.
Chemically synthesized molecules with the targeting and effector functions of antibodies
McEnaney, Patrick J.,Fitzgerald, Kelly J.,Zhang, Andrew X.,Douglass, Eugene F.,Shan, Weifang,Balog, Aaron,Kolesnikova, Mariya D.,Spiegel, David A.
, p. 18034 - 18043 (2014)
This article reports the design, synthesis, and evaluation of a novel class of molecules of intermediate size (approximately 7000 Da), which possess both the targeting and effector functions of antibodies. These compounds-called synthetic antibody mimics targeting prostate cancer (SyAM-Ps)-bind simultaneously to prostate-specific membrane antigen and Fc gamma receptor I, thus eliciting highly selective cancer cell phagocytosis. SyAMs have the potential to combine the advantages of both small-molecule and biologic therapies, and may address many drawbacks associated with available treatments for cancer and other diseases.
Synthesis and automated fluorine-18 radiolabeling of new PSMA-617 derivatives with a CuAAC radiosynthetic approach
Iannone, Marco N.,Stucchi, Stefano,Turolla, Elia A.,Beretta, Chiara,Ciceri, Samuele,Chinello, Clizia,Pagani, Lisa,Todde, Sergio,Ferraboschi, Patrizia
, p. 48 - 62 (2022/01/19)
In the last decade, the development of new radiopharmaceuticals for the imaging and therapy of prostate cancer has been a highly active and important area of research, especially focusing on the prostate-specific membrane antigen (PSMA), an antigen which
Hybrid chelator-based PSMA radiopharmaceuticals: Translational approach
Greifenstein, Lukas,Grus, Tilmann,Lahnif, Hanane,Pektor, Stefanie,R?sch, Frank,Schreckenberger, Mathias
, (2021/11/01)
(1) Background: Prostate-specific membrane antigen (PSMA) has been extensively studied in the last decade. It became a promising biological target in the diagnosis and therapy of PSMAexpressing cancer diseases. Although there are several radiolabeled PSMA
TARGETED RADIOPHARMACEUTICALS FOR THE DIAGNOSIS AND TREATMENT OF PROSTATE CANCER
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, (2021/01/29)
A compound of general formula (I): wherein: n is 1, 2 or 3; R1, R2, R3 and R4, independently represent OH or Q; and 20 Q represents a tissue-targeting moeity selected from the group consisting of or a stereoisomer, a hydrate, a solvate, or a salt thereof, or a mixture of same, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said 25 compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of soft tissue diseases, as a sole agent or in combination with other active ingredients.