The heterobivalent (SSTR2/albumin) radioligand [⁶⁷Cu]Cu-NODAGA-cLAB4-TATE enables efficient somatostatin receptor radionuclide theranostics.

ABSTRACT: Somatostatin type 2 receptor (SSTR2) radionuclide therapy using β^- particle-emitting radioligands has entered clinical practice for the treatment of neuroendocrine neoplasms (NENs). Despite the initial success of [¹⁷⁷Lu]Lu‑DOTA-TATE, theranostic SSTR2 radioligands require improved pharmacokinetics and enhanced compatibility with alternative radionuclides. Consequently, this study evaluates the pharmacokinetic effects of the albumin-binding domain cLAB4 on theranostic performance of copper‑67-labeled NODAGA-TATE variants in an SSTR2-positive mouse pheochromocytoma (MPC) model. Methods: Binding, uptake, and release of radioligands as well as growth-inhibiting effects were characterized in cells grown as monolayers and spheroids. Tissue pharmacokinetics, absorbed

SUBMITTER: Ullrich M 

PROVIDER: S-EPMC11413788 | biostudies-literature | 2024

REPOSITORIES: biostudies-literature