Evaluation of Astatine-211-Labeled Octreotide as a Potential Radiotherapeutic Agent for NSCLC Treatment

Publication date: Available online 31 January 2018
Source:Bioorganic & Medicinal Chemistry
Author(s): Bingkun Zhao, Shanshan Qin, Li Chai, Gaixia Lu, Yuanyou Yang, Huawei Cai, Xueyu Yuan, Suyun Fan, Qingqing Huang, Fei Yu
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 of ²¹¹At-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 free ²¹¹At). These promising preclinical results suggested that ²¹¹At labeled octreotide deserved to be further developed as a new anticancer agent for NSCLC.

Graphical abstract

http://ift.tt/2DTYtbu