Tehran University of Medical Sciences
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Davood Beiki

Synthesis and Evaluation of [67Ga]-AMD3100; a novel imaging agent for targeting chemokine receptor CXCR4

Authors: Aghanejad A, Jalilian AR, Fazaeli Y, Alirezapoor B, Pouladi M, Beiki D, Maus S, Khalaj A,
Keywords: 67Ga, CXCR4, Biodistribution, SPECT, breast carcinoma
Scientia Pharmaceutica, Vol.82, No., 2014,Page:29-42

In order to develop a possible C-X-C chemokine receptor type 4 (CXCR4) imaging agent for oncological scintigraphy, [67Ga]labeled 1,1′-[1,4-Phenylenebis(methylene)] bis-1,4,8,11-tetraazacyclo- tetradecane ([67Ga]-AMD3100) was prepared using [67Ga]GaCl3 and AMD-3100 for 2h at 50C (radiochemical purity: >95% ITLC, >99% HPLC, specific activity: 1800-2000 TBq/mmol) in acetate buffer. Stability of the complex was checked in presence of human serum (37ºC) and in final formulation for 4 days. The biodistribution of the labeled compound in vital organs of wild-type Sprague-Dawdley rats were determined and compared with that of free Ga3+ cation up to 48h. Considering spleen as the target organ the best target:non target ratios were obtained 48 h post injection (spleen:blood ratio; 14.5 and spleen:muscle ratio ;88.4). Initial SPECT images and biodistribution results in wild type rats matched each other and demonstrate rapid wash out of the tracer from urinal tract. SPECT images in human breast carcinoma-bearing mice demonstrated detectable tumor uptake in
48 h post injection.