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PSMA and Integrin αvβ3 Dual-Targeted Radioligands for Prostate Cancer Targeted Radionuclide Therapy
Xunhao Qi1, Zhihao Li1, Junhong Wang1
1State Key Laboratory of Radiation Medicine and Protection, School of Radiation Medicine and Protection, Collaborative Innovation Center of Radiation Medicine of Jiangsu Higher Education Institutions, Soochow University, Suzhou 215123, China.
A new dual-targeting radioligand, 177Lu-PSMA-3-RGD, effectively targets both prostate-specific membrane antigen (PSMA) and integrin αvβ3 in prostate cancer. This innovative approach shows promise for improved theranostic applications in metastatic castration-resistant prostate cancer.
Area of Science:
- Nuclear medicine
- Oncology
- Radiopharmaceutical chemistry
Background:
- Metastatic castration-resistant prostate cancer (mCRPC) poses significant treatment challenges due to tumor heterogeneity.
- Single-target radiopharmaceuticals have limitations, including variable antigen expression, necessitating novel therapeutic strategies.
Purpose of the Study:
- To develop and evaluate a novel dual-targeting radioligand, 177Lu-PSMA-3-RGD, for enhanced prostate cancer theranostics.
- To assess the efficacy and safety of this dual-targeting approach compared to single-targeted agents.
Main Methods:
- Solid-phase synthesis and click chemistry were employed to create the 177Lu-PSMA-3-RGD radioligand.
- In vitro studies assessed radiochemical purity, radiostability, and cellular uptake.
- In vivo studies utilized xenograft models to evaluate tumor accumulation, retention, specificity, and therapeutic efficacy.
Main Results:
- The radioligand exhibited high radiochemical purity and stability, with selective uptake in PSMA-positive cells.
- In vivo studies demonstrated rapid tumor accumulation, prolonged retention, and specific targeting confirmed by receptor-blocking.
- Therapeutic administration led to significant tumor growth delay compared to single-targeted radioligands, with no observed systemic toxicity.
Conclusions:
- The dual-targeting radioligand 177Lu-PSMA-3-RGD effectively targets both PSMA and integrin αvβ3 in prostate cancer models.
- This dual-targeting strategy offers superior therapeutic efficacy and a promising theranostic potential for prostate cancer.
- Further preclinical and clinical investigations are warranted for this novel radioligand.
