Radiolabeled bombesin-derived compounds for in vivo imaging of gastrin-releasing peptide receptor (GRPR) and treatment of GRPR-related disorders

JP7883776B2Inactive Publication Date: 2026-07-02PROVINCIAL HEALTH SERVICES AUTHORITY
View PDF 4 Cites 0 Cited by

Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
PROVINCIAL HEALTH SERVICES AUTHORITY
Filing Date
2024-05-31
Publication Date
2026-07-02
Estimated Expiration
Not applicable · inactive patent

Smart Images

  • Figure 0007883776000049
    Figure 0007883776000049
  • Figure 0007883776000050
    Figure 0007883776000050
  • Figure 0007883776000051
    Figure 0007883776000051
Patent Text Reader

Abstract

To provide an improved radiotherapeutic agent for treating a disease associated with abnormal expression of a gastrin-releasing peptide receptor.SOLUTION: Provided is a bombesin-derived compound of formula Ia (RX-L-Xaa1-Gln-Trp-Ala-Val-Xaa2-His-Xaa3-ψ-Xaa4-NH2). RX includes a radionuclide chelator or trifluoroborate-containing prosthetic group. L is a linker. Xaa1 is D-Phe or the like, and Xaa2 is Gly or the like. Xaa3 is Leu or the like, and Xaa4 is Pro or the like. A symbol ψ denotes reduced peptide bond between Xaa3 and Xaa4. In the case where Xaa4 is Pro or the like, ψ is CH2-N, or in the case where Xaa4 is Phe or Nle, ψ is CH2 N(R). R is H or a C1-C5 linear or branched alkyl. Use of the compound as a contrast medium or therapeutic agent is also provided.SELECTED DRAWING: None
Need to check novelty before this filing date? Find Prior Art

Citation Information

Patent Citations

  • Targeted cytotoxic anthracycline analogues

    JP2000502055A

  • Pharmaceutical for treating hepatoma

    JP2010150253A

  • Bombesin analog peptide antagonist complex

    JP2011515338A

  • GRPR antagonists for the detection, diagnosis, and treatment of GRPR-positive cancers

    JP2015533119A