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Extensive interest in the development of α-emitting radionuclides astatine-211 ( 211 At) stems from the potential superiority for the treatment of smaller tumors, disseminated disease, and metastatic disease. VP2, a small molecule fusion peptide, can specifically bind to the VPAC1 receptor which is over-expressed in malignant epithelial tumors. In our recent study, we performed the preparation of  211 At labelled VP2 through a one-step method. In this work, we explored the targeted radionuclide therapy with [ 211 At]At-SPC-VP2  in vitro  and  in vivo . The cytotoxicity and specific cell killing of [ 211 At]At-SPC-VP2 were evaluated using the CCK-8 assay. Compared with the [ 211 At]NaAt, the VPAC1-targeted radionuclide compound [ 211 At]At-SPC-VP2 showed more effective cytotoxicity  in vitro . Targeted radioactive therapy trial was carried out in non-small-cell lung cancer (NSCLC) xenograft mice. For the therapy experiment, 4 groups of mice were injected via the tail vein with 370 kBq, 550 kBq, 740 kBq, 3 × ∼246 kBq of [ 211 At]At-SPC-VP2, of which the second and third injections were given 4 and 8 days after the first injection, respectively. As controls, animals were treated with saline or 550 kBq [ 211 At]NaAt. The body weight and tumor size of mice were monitored before the administration and every 2 days thereafter. Cytotoxic radiation of partial tissue samples such as kidneys, liver and stomach of mice were assessed by immunohistochemical examination. The tumor growth was inhibited and significantly improved survival was achieved in mice treated with [ 211 At]At-SPC-VP2, two-fold prolongation of survival compared with the control group, which received normal saline or 550 kBq [ 211 At]NaAt. No renal or hepatic toxicity was observed in the mice receiving [ 211 At]At-SPC-VP2, but gastric pathological sections showed  211 At uptake in stomach resulting in later toxicity, highlighting the importance of further enhancing the stability of labelled compounds.

Astatine-211 labelled a small molecule peptide: specific cell killing in vitro and targeted therapy in a nude-mouse model