Compound for dual targeting of tumor cell, and preparation method therefor and use thereof

By developing dual-targeted tumor cell compounds, combined with PSMA and SSTR2, the problem of insufficient sensitivity of prostate cancer imaging technology was solved, and efficient diagnosis and treatment of neuroendocrine prostate cancer was achieved.

WO2025151982A1 Publication Date: 2025-07-24PEKING UNION MEDICAL COLLEGE HOSPITAL +1
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Patent Information

Application Number
PCT/CN2024/072279
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Filing Date
2024-01-15
Publication Date
2025-07-24

AI Technical Summary

Technical Problem

The prior art is difficult to effectively solve neuroendocrine prostate cancer with PSMA negative or insufficient expression in the diagnosis and treatment of prostate cancer, and the sensitivity of traditional imaging technology is limited, so it is impossible to accurately locate and evaluate the degree of disease recurrence.

Method used

A compound that dual-targets tumor cells is developed, combining prostate-specific membrane antigen PSMA and somatostatin receptor 2 (SSTR2), and high affinity and specific targeting for PSMA and SSTR2 are achieved by labeling different radionuclides, and radioactive metal complexes are prepared to improve the accuracy of imaging diagnosis and treatment.

Benefits of technology

It improves the detection rate of neuroendocrine prostate cancer lesions, achieves more accurate tumor staging and disease prognosis, and provides the possibility of targeted radionuclide therapy.

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Abstract

The present invention belongs to the technical field of radiopharmaceutical chemistry and nuclear medicine diagnosis and treatment. Disclosed are a compound for dual targeting of a tumor cell, a preparation method therefor and the use thereof. The compound for dual targeting of a tumor cell has general formulas as represented by formula (I) and formula (II), wherein L1 and L3 are linking groups between a chelator and a PSMA-targeting structure; L2 and L4 are linking groups between the chelator and Peptide1; the Peptide1 and Peptide2 are polypeptide molecules having an SSTR2 targeting property, such as JR11, LM3, LM4, TATE, TOC and NOC; and Chelator1 and Chelator2 are chelators or chelating structures. In the present invention, a PSMA-targeting group and an SSTR2-targeting group are simultaneously linked to a metal chelator (HBED-CC, DOTAGA, DOTA(GA)2, etc.) for the first time for labeling a radioactive metal nuclide such as 68Ga, 18F-AlF, 177Lu, 90Y, 44Sc, 225Ac, 212Pb and 213Bi. The dual targeting function on PSMA and SSTR2 is beneficial to improving the lesion detection rate of neuroendocrine prostate cancer, and achieving more accurate tumor staging and disease prognosis, and is expected to be used for radionuclide targeted therapy.
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