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¹¹¹In-labeled 1,4,7,10-Tetraazacyclododecane-N,N',N'',N'''-tetraacetic Acid-Lys⁸-Vasotocin

A New Powerful Radioligand for Oxytocin Receptor-expressing Tumors¹

Department of Biomedical Sciences and Human Oncology, University of Torino, 10126 Torino [G. B., P. C.]; Division of Nuclear Medicine, European Institute of Oncology, 20141 Milan [M. C., A. N., G. P.]; and Consiglio Nazionale delle Ricerche Cellular and Molecular Pharmacology Center, 20129 Milan [B. C.], Italy

We developed a radioactive ligand for tumors expressing oxytocin receptors (OTRs) by linking the chelating agent 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA) to Lys⁸-vasotocin (LVT), an analogue of oxytocin with high affinity for OTRs. The new reagent (DOTA-LVT) retained high affinity for human OTRs, as proved by in vitro affinity binding to cells endogenously expressing OTRs, such as MCF7 breast carcinoma and MOG-U-V-W glioblastoma cells lines, as well as to transiently transfected COS7 cells. In in vivo experiments, DOTA-LVT carrying ¹¹¹In showed specific binding activity to OTR-positive TS/A mouse mammary tumors. The present study opens new perspectives for imaging and, possibly, therapy of OTR-positive human tumors such as breast and endometrial carcinomas, neuroblastomas, and glioblastomas.

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