Ga/Lu-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 68 Ga/ 177 Lu-labeling DOTA-TATE kit in neuroendocrine tumor mod...

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Main Authors: Fei Liu, Hua Zhu, Jiangyuan Yu, Xuedi Han, Qinghua Xie, Teli Liu, Chuanqin Xia, Nan Li, Zhi Yang
Format: Article
Language:English
Published: SAGE Publishing 2017-05-01
Series:Tumor Biology
Online Access:https://doi.org/10.1177/1010428317705519
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author Fei Liu
Hua Zhu
Jiangyuan Yu
Xuedi Han
Qinghua Xie
Teli Liu
Chuanqin Xia
Nan Li
Zhi Yang
author_facet Fei Liu
Hua Zhu
Jiangyuan Yu
Xuedi Han
Qinghua Xie
Teli Liu
Chuanqin Xia
Nan Li
Zhi Yang
author_sort Fei Liu
collection DOAJ
description 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 68 Ga/ 177 Lu-labeling DOTA-TATE kit in neuroendocrine tumor model for molecular imaging and to try human–positron emission tomography/computed tomography imaging of 68 Ga-DOTA-TATE in neuroendocrine tumor patients. DOTA-TATE kits were formulated and radiolabeled with 68 Ga/ 177 Lu for 68 Ga/ 177 Lu-DOTA-TATE (M-DOTA-TATE). In vitro and in vivo stability of 177 Lu-DOTA-TATE were performed. Nude mice bearing human tumors were injected with 68 Ga-DOTA-TATE or 177 Lu-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 68 Ga-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 68 Ga-DOTA-TATE and 177 Lu-DOTA-TATE both showed clear tumor uptake which could be blocked by excess DOTA-TATE. In addition, 68 Ga-DOTA-TATE–positron emission tomography/computed tomography imaging in neuroendocrine tumor patients could show primary and metastatic lesions. 68 Ga-DOTA-TATE and 177 Lu-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.
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spelling doaj-art-d008df44a09044dfbe99c70c730c17cb2025-08-20T03:39:15ZengSAGE PublishingTumor Biology1423-03802017-05-013910.1177/1010428317705519Ga/Lu-labeled DOTA-TATE shows similar imaging and biodistribution in neuroendocrine tumor modelFei Liu0Hua Zhu1Jiangyuan Yu2Xuedi Han3Qinghua Xie4Teli Liu5Chuanqin Xia6Nan Li7Zhi Yang8Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing, ChinaKey Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing, ChinaKey Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing, ChinaKey Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing, ChinaCollege of Chemistry, Sichuan University, Chengdu, ChinaKey Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing, ChinaCollege of Chemistry, Sichuan University, Chengdu, ChinaKey Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing, ChinaKey Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing, ChinaSomatostatin 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 68 Ga/ 177 Lu-labeling DOTA-TATE kit in neuroendocrine tumor model for molecular imaging and to try human–positron emission tomography/computed tomography imaging of 68 Ga-DOTA-TATE in neuroendocrine tumor patients. DOTA-TATE kits were formulated and radiolabeled with 68 Ga/ 177 Lu for 68 Ga/ 177 Lu-DOTA-TATE (M-DOTA-TATE). In vitro and in vivo stability of 177 Lu-DOTA-TATE were performed. Nude mice bearing human tumors were injected with 68 Ga-DOTA-TATE or 177 Lu-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 68 Ga-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 68 Ga-DOTA-TATE and 177 Lu-DOTA-TATE both showed clear tumor uptake which could be blocked by excess DOTA-TATE. In addition, 68 Ga-DOTA-TATE–positron emission tomography/computed tomography imaging in neuroendocrine tumor patients could show primary and metastatic lesions. 68 Ga-DOTA-TATE and 177 Lu-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.https://doi.org/10.1177/1010428317705519
spellingShingle Fei Liu
Hua Zhu
Jiangyuan Yu
Xuedi Han
Qinghua Xie
Teli Liu
Chuanqin Xia
Nan Li
Zhi Yang
Ga/Lu-labeled DOTA-TATE shows similar imaging and biodistribution in neuroendocrine tumor model
Tumor Biology
title Ga/Lu-labeled DOTA-TATE shows similar imaging and biodistribution in neuroendocrine tumor model
title_full Ga/Lu-labeled DOTA-TATE shows similar imaging and biodistribution in neuroendocrine tumor model
title_fullStr Ga/Lu-labeled DOTA-TATE shows similar imaging and biodistribution in neuroendocrine tumor model
title_full_unstemmed Ga/Lu-labeled DOTA-TATE shows similar imaging and biodistribution in neuroendocrine tumor model
title_short Ga/Lu-labeled DOTA-TATE shows similar imaging and biodistribution in neuroendocrine tumor model
title_sort ga lu labeled dota tate shows similar imaging and biodistribution in neuroendocrine tumor model
url https://doi.org/10.1177/1010428317705519
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