Novel [ 111 In]In-BnDTPA-EphA2-230-1 Antibody for Single-Photon Emission Computed Tomography Imaging Tracer Targeting of EphA2

Takenori Furukawa; Hiroyuki Kimura; Minon Sasaki; Takumu Yamada; Takumi Iwasawa; Yusuke Yagi; Kazunori Kato; Hiroyuki Yasui

doi:10.1021/acsomega.2c07849

Novel [ ¹¹¹ In]In-BnDTPA-EphA2-230-1 Antibody for Single-Photon Emission Computed Tomography Imaging Tracer Targeting of EphA2

ACS Omega. 2023 Feb 9;8(7):7030-7035. doi: 10.1021/acsomega.2c07849. eCollection 2023 Feb 21.

Authors

Takenori Furukawa¹, Hiroyuki Kimura¹, Minon Sasaki¹, Takumu Yamada², Takumi Iwasawa², Yusuke Yagi^{1

3}, Kazunori Kato², Hiroyuki Yasui¹

Affiliations

¹ Department of Analytical and Bioinorganic Chemistry, Division of Analytical and Physical Science, Kyoto Pharmaceutical University, 5 Nakauchi-cho, Misasagi, Yamashina-ku, Kyoto 607-8414, Japan.
² Department of Biomedical Engineering, Faculty of Science and Engineering, Toyo University, 2100 Nakanodai, Kujirai, Kawagoe, Saitama 350-0815, Japan.
³ Department of Radiological Technology, Faculty of Medicinal Science, Kyoto College of Medical Science, 1-3 Imakita, Oyama-higashi, Sonobe, Nantan, Kyoto 622-0022, Japan.

Abstract

Erythropoietin-producing hepatocellular receptor A2 (EphA2) is overexpressed in cancer cells and causes abnormal cell proliferation. Therefore, it has attracted attention as a target for diagnostic agents. In this study, the EphA2-230-1 monoclonal antibody (EphA2-230-1) was labeled with [¹¹¹In]In and evaluated as an imaging tracer for single-photon emission computed tomography (SPECT) of EphA2. EphA2-230-1 was conjugated with 2-(4-isothiocyanatobenzyl)-diethylenetriaminepentaacetic acid (p-SCN-BnDTPA) and then labeled with [¹¹¹In]In. [¹¹¹In]In-BnDTPA-EphA2-230-1 was evaluated in cell-binding, biodistribution, and SPECT/computed tomography (CT) studies. The cellular uptake ratio of [¹¹¹In]In-BnDTPA-EphA2-230-1 was 14.0 ± 2.1%/mg protein at 4 h in the cell-binding study. In the biodistribution study, a high uptake of [¹¹¹In]In-BnDTPA-EphA2-230-1 was observed in tumor tissue (14.6 ± 3.2% injected dose/g at 72 h). The superior accumulation of [¹¹¹In]In-BnDTPA-EphA2-230-1 in tumors was also confirmed using SPECT/CT. Therefore, [¹¹¹In]In-BnDTPA-EphA2-230-1 has potential as a SPECT imaging tracer for EphA2.