Evaluation of astatine-211-labeled octreotide as a potential radiotherapeutic agent for NSCLC treatment.
Evaluation of astatine-211-labeled octreotide as a potential radiotherapeutic agent for NSCLC treatment.
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DOI：
10.1016/j.bmc.2018.01.023
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发表时间：
2018-03
影响因子：
3.5
通讯作者：
Bing-kun Zhao;ShanShan Qin;Li Chai;Gaixia Lu;Yuanyou Yang;H. Cai;Xueyu Yuan;Suyun Fan;Qingqing Huang;Fei Yu
中科院分区：
文献类型：
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作者：
Bing-kun Zhao;ShanShan Qin;Li Chai;Gaixia Lu;Yuanyou Yang;H. Cai;Xueyu Yuan;Suyun Fan;Qingqing Huang;Fei Yu
奥曲肽是一种生长抑素（SST）类似物，目前用于治疗神经内分泌肿瘤（NETs），与生长抑素受体-2 （SSTR2）具有高结合亲和力，该受体-2在非小细胞肺癌细胞（NSCLC）中也过表达。发射α粒子的砹-211 （2111at）是一种很有前途的放射性核素，具有适当的物理和化学性质，可用于靶向抗癌治疗。为了获得一种治疗非小细胞肺癌的额外药物，我们首次研究了2111at标记的奥曲肽作为一种潜在的α -放射性核素治疗非小细胞肺癌的可能性。2111at - spc -奥曲肽在肺、脾、胃和肠中的摄取明显高于其他组织。通过组织学检查，211at - spc -奥曲肽的致死性明显高于对照组（PBS、奥曲肽和free211At）。这些有希望的临床前结果表明，2111at标记的奥曲肽作为一种新的NSCLC抗癌药物值得进一步开发。
Octreotide is a somatostatin (SST) analogue currently used in the treatment of neuroendocrine tumors (NETs) with high binding affinity for the somatostatin receptor-2 (SSTR2) that is also overexpressed in non-small cell lung cancer cell (NSCLC). Alpha-particle-emitting astatine-211 (211At) is a promising radionuclide with appropriate physical and chemical properties for use in targeted anticancer therapies. To obtain an additional pharmacological agent for the treatment of NSCLC, we present the first investigation of the possible use of211At-labeled octreotide as a potential alpha-radionuclide therapeutic agent for NSCLC treatment.211At-SPC-octreotide exhibited observable higher uptake in lung, spleen, stomach and intestines than in other tissues. Through histological examination,211At-SPC-octreotide demonstrated much more lethal effect than control groups (PBS, octreotide and free211At). These promising preclinical results suggested that211At labeled octreotide deserved to be further developed as a new anticancer agent for NSCLC.