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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
Authors
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Authors Affiliations
  1. 1. Department of Radiopharmacy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), P.O. Box: 14395-836, Tehran, 1439951113, Iran
  3. 3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
  4. 4. Department of Toxicology and Pharmacology, Faculty of Pharmacy, Toxicology and Poisoning Research Centre, Tehran University of Medical Sciences, P.O. Box: 14155-6451, Tehran, 1417614411, Iran

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.