Preclinical Evaluation in Animals for the Efficacy, Dosimetry, and Safety of [⁶⁸Ga]Ga/[¹⁷⁷Lu]Lu-TVS-PSMA Radioligands, and First-in-Human Study of [⁶⁸Ga]Ga-TVS-PSMA-1.

Authors

Yuduo Wan, Yang Wang, Wanlu Feng, Liping Yang, Qinghong Sun, Huanyu Chen, Ya Liu, Yan Zhu, He Zhang, Haoyuan Ding, Zibo Li, Li Wang

Published in

Bioconjugate chemistry. Jul 17, 2026. Epub Jul 17, 2026.

Abstract

To improve the theranostic efficacy of PSMA-targeted radiopharmaceuticals on patients with medium-to-low PSMA expression, we radiolabeled a series of novel designed PSMA-targeting dimer agents to improve tumor imaging and treatment outcomes under challenging conditions. All agents were successfully radiolabeled with ⁶⁸Ga in moderate decay-corrected labeling yield and high radiochemical purity. Among them, [⁶⁸Ga]Ga-TVS-PSMA-1 exhibited high tumor uptake in both LNCaP and 22RV1 models. [¹⁷⁷Lu]Lu-TVS-PSMA-1 demonstrated significantly improved treatment efficacy with a lower dose and good safety profile compared with [¹⁷⁷Lu]Lu-PSMA-617. A first-in-human [⁶⁸Ga]Ga-TVS-PSMA-1 PET/CT scan was performed in a 66-year-old male prostate cancer patient. Two metastatic lesions in the lumbar vertebrae were clearly visualized, and the primary tumor exhibited an SUVmax of 30.3. The [⁶⁸Ga]Ga-TVS-PSMA-1 showed lower salivary gland uptake compared with previously reported values for [⁶⁸Ga]Ga-PSMA-11; however, confirmation in larger patient cohorts is required. This study demonstrates that the dimer agent TVS-PSMA-1 holds great potential as a next-generation theranostic agent for prostate cancer.

PMID:
42464640
Bibliographic data and abstract were imported from PubMed on 17 Jul 2026.

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