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Title:
IMPROVED PROSTATE-SPECIFIC MEMBRANE ANTIGEN TARGETING RADIOPHARMACEUTICALS AND USES THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/253785
Kind Code:
A3
Abstract:
The present invention relates to diagnosis and treatment of malignancies characterised by prostate-specific membrane antigen (PSMA) expression. The invention particularly relates to improved radiopharmaceuticals which selectively bind to PSMA and are suitable for planar imaging of PSMA expression in subjects to diagnose and/or monitor malignancies wherein PSMA is (over)expressed. Additionally, the invention relates to improved radiopharmaceuticals which selectively bind to PSMA and are suitable to act as radionuclide treatment agents. The radiopharmaceuticals rely on a pharmacophore capable of interacting with PSMA and N-terminal mercaptoacetyltripeptides capable of coordinating radioactive metals such as technetium and rhenium.

Inventors:
GIESEL FREDERIK (DE)
CARDINALE JENS (DE)
KRATOCHWIL CLEMENS (DE)
HABERKORN UWE (DE)
Application Number:
PCT/EP2022/064668
Publication Date:
March 23, 2023
Filing Date:
May 31, 2022
Export Citation:
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Assignee:
UNIV HEIDELBERG (DE)
TELIX INT PTY LTD (AU)
International Classes:
C07B59/00; A61K51/04; A61P35/00; C07C275/16; C07F13/00
Domestic Patent References:
WO2022167681A12022-08-11
Foreign References:
US20210121585A12021-04-29
Other References:
DERKS YVONNE H. W. ET AL: "Strain-Promoted Azide-Alkyne Cycloaddition-Based PSMA-Targeting Ligands for Multimodal Intraoperative Tumor Detection of Prostate Cancer", BIOCONJUGATE CHEMISTRY, vol. 33, no. 1, 19 January 2022 (2022-01-19), US, pages 194 - 205, XP055972764, ISSN: 1043-1802, Retrieved from the Internet DOI: 10.1021/acs.bioconjchem.1c00537
ELENI GOURNI ET AL: "Metal-Based PSMA Radioligands", MOLECULES, vol. 22, no. 4, 24 March 2017 (2017-03-24), pages 523, XP055580174, DOI: 10.3390/molecules22040523
Attorney, Agent or Firm:
DE CLERCQ & PARTNERS (BE)
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