⁶⁸Ga/¹⁷⁷Lu-labeled DOTA-TATE shows similar imaging and biodistribution in neuroendocrine tumor model

Somatostatin receptors are overexpressed in neuroendocrine tumors, whose endogenous ligands are somatostatin. DOTA-TATE is an analogue of somatostatin, which shows high binding affinity to somatostatin receptors. We aim to evaluate the ⁶⁸Ga/¹⁷⁷Lu-labeling DOTA-TATE kit in neuroendocrine tumor model for molecular imaging and to try human-positron emission tomography/computed tomography imaging of ⁶⁸Ga-DOTA-TATE in neuroendocrine tumor patients. DOTA-TATE kits were formulated and radiolabeled with ⁶⁸Ga/¹⁷⁷Lu for ⁶⁸Ga/¹⁷⁷Lu-DOTA-TATE (M-DOTA-TATE). In vitro and in vivo stability of ¹⁷⁷Lu-DOTA-TATE were performed. Nude mice bearing human tumors were injected with ⁶⁸Ga-DOTA-TATE or ¹⁷⁷Lu-DOTA-TATE for micro-positron emission tomography and micro-single-photon emission computed tomography/computed tomography imaging separately, and clinical positron emission tomography/computed tomography images of ⁶⁸Ga-DOTA-TATE were obtained at 1 h post-intravenous injection from patients with neuroendocrine tumors. Micro-positron emission tomography and micro-single-photon emission computed tomography/computed tomography imaging of ⁶⁸Ga-DOTA-TATE and ¹⁷⁷Lu-DOTA-TATE both showed clear tumor uptake which could be blocked by excess DOTA-TATE. In addition, ⁶⁸Ga-DOTA-TATE-positron emission tomography/computed tomography imaging in neuroendocrine tumor patients could show primary and metastatic lesions. ⁶⁸Ga-DOTA-TATE and ¹⁷⁷Lu-DOTA-TATE could accumulate in tumors in animal models, paving the way for better clinical peptide receptor radionuclide therapy for neuroendocrine tumor patients in Asian population.