Radiopharmaceutical composition targeting glypican 3 and its use

Radiopharmaceutical conjugates with GPC3-binding peptides and radionuclides offer improved therapeutic efficacy by specifically targeting GPC3-expressing tumors, addressing the limitations of existing GPC3-targeting therapies.

JP2026520154APending Publication Date: 2026-06-22RAYZEBIO INC
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Patent Information

Application Number
JP2025570864
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2023-06-07
Filing Date
2024-06-06
Publication Date
2026-06-22

AI Technical Summary

Technical Problem

Current therapies targeting glypican 3 (GPC3) expression in tumors, such as the GC33 antibody, have shown limited efficacy in clinical trials, necessitating the development of more effective GPC3-binding agents for cancer treatment.

Method used

Development of radiopharmaceutical conjugates comprising peptides with specific avidity to GPC3, covalently bonded to a metal chelating agent capable of binding radionuclides, which can be used to target and treat GPC3-expressing tumors.

Benefits of technology

The radiopharmaceutical conjugates provide enhanced targeting and therapeutic efficacy by delivering radionuclides specifically to GPC3-expressing tumors, potentially improving treatment outcomes for cancers like hepatocellular carcinoma.

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Abstract

Radiopharmaceuticals and conjugates targeting GPC3, as well as their compositions and uses, are provided herein. In one embodiment, a conjugate comprising a peptide having avidity to GPC3 and a metal chelating agent configured to bind to a radionuclide is provided herein. The conjugate described herein may further comprise a linker connecting the chelating agent and the peptide. The conjugate described herein may further comprise a radionuclide. In one embodiment, a radiopharmaceutical comprising a peptide and a metal chelating agent binding to a radionuclide is provided herein. The conjugate described herein may further comprise a linker connecting the chelating agent and the peptide. Methods for treating cancer by administering the radiopharmaceuticals, conjugates, and compositions thereof are further provided herein.
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