Development of a 99Mtc-Labeled Cxcr4 Antagonist Derivative As a New Tumor Radiotracer Publisher Pubmed



Mikaeili A¹ ; Erfani M² ; Shafiei M² ; Kobarfard F³ ; Abdi K¹ ; Sabzevari O⁴
Source: Cancer Biotherapy and Radiopharmaceuticals Published:2018

Abstract

Due to high expression of CXCR4 (CXC chemokine receptor type 4) receptors in many tumors and metastasis, synthesis and labeling of CXCR4 receptor-targeted analogs as tumor imaging agents have been encouraged. Herein, CXCR4 receptor-targeted peptide antagonist was prepared and thereafter its labeling with 99mTc by a bifunctional chelating agent and tricine coligand was developed. Radiotracer purity, stability, and tumor cell binding were assessed. Bioevaluation of radiotracer was performed in mice bearing xenograft tumor. More than 95% labeling yield and stability up to 24 hours were observed. Radiotracer-related tumor accumulation was 3.61 ± 0.15% ID/g at 1 hour postinjection. High stability and specific tumor uptake are important characteristics of the radiotracer that could nominate this as a targeted imaging agent in the future. © Copyright 2018, Mary Ann Liebert, Inc.