68Ga/177Lu-labeled DOTA-TATE shows similar imaging and biodistribution in neuroendocrine tumor model
68Ga/177Lu-labeled DOTA-TATE shows similar imaging and biodistribution in neuroendocrine tumor model
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68Ga/177Lu 标记的 DOTA-TATE 在神经内分泌肿瘤模型中显示出相似的成像和生物分布
DOI：
10.1177/1010428317705519
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发表时间：
2017-06-15
期刊：
影响因子：
--
通讯作者：
Yang, Zhi
中科院分区：
文献类型：
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作者：
Liu, Fei;Zhu, Hua;Yang, Zhi
生长激素抑制素受体在神经内分泌肿瘤中过表达，其内源性配体是生长激素抑制素。DOTA-TATE是生长抑素的类似物，其显示出对生长抑素受体的高结合亲和力。我们的目的是评估68 Ga/177 Lu标记的DOTA-TATE试剂盒在神经内分泌肿瘤模型中的分子成像，并尝试在神经内分泌肿瘤患者中进行68 Ga-DOTA-TATE的人体正电子发射断层扫描/计算机断层扫描成像。配制DOTA-TATE试剂盒并用68 Ga/177 Lu放射性标记68 Ga/177 Lu-DOTA-TATE（M-DOTA-TATE）。进行177 Lu-DOTA-TATE的体外和体内稳定性。将68 Ga-DOTA-TATE或177 Lu-DOTA-TATE分别注射到荷人肿瘤的裸鼠中进行微正电子发射断层扫描和微单光子发射计算机断层扫描/计算机断层扫描成像，并在静脉注射后1 h从神经内分泌肿瘤患者获得68 Ga-DOTA-TATE的临床正电子发射断层扫描/计算机断层扫描图像。68 Ga-DOTA-TATE和177 Lu-DOTA-TATE的微型正电子发射断层扫描和微型单光子发射计算机断层扫描/计算机断层扫描成像均显示出清晰的肿瘤吸收，这可以被过量的DOTA-TATE阻断。此外，神经内分泌肿瘤患者的68 Ga-DOTA-TATE-正电子发射断层扫描/计算机断层扫描成像可显示原发性和转移性病变。68 Ga-DOTA-TATE和177 Lu-DOTA-TATE在动物模型中可以在肿瘤中蓄积，为亚洲人群神经内分泌肿瘤患者更好的临床肽受体放射性核素治疗铺平了道路。
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.