Development of a 211 At-Tetrazine-PSMA Radioconjugate for Targeted α-Therapy (EANM 2026) - Sep 29, 2026 - Abstract #EP-0024; "Aim/Introduction: With the introduction of the PSMAtargeting radioligand [¹⁷⁷Lu]LuPSMA617 marking a major advance in the treatment of metastatic castration-resistant prostate cancer, there remains a need for further development due to response rates of 50-60% of patients... Four analogues containing the glutamate-urea-lysine pharmacophore and an isomer free trans-cyclooctadiene for labelling via tetrazine ligation were synthesized and evaluated for PSMA-binding affinity, internalization, and biodistribution in healthy rats. The most promising candidate [18F]PSMA-14 was further assessed in tumour-bearing mice, demonstrating a favourable biodistribution, and subsequently translated to the corresponding 211At-labeled radiopharmaceutical [211At] AstaProst, which delayed tumour growth and prolonged survival."
Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Prostate Cancer • Solid Tumor
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J. Schichler 1; U. M. Battisti 1, 2; L. Hvass 3; C. Poulie 1, 2; V. Shalgunov 1, 4; N. R. Bom Pedersen 1, 2; T. K. Gustavsson 2; S. Stotz 2; N. Billesborg Pedersen 2; L. A. Vázquez 2; A. I. Jensen 1; A. Kjaer 3; M. M. Herth 1, 2
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