NUKLEONIKA 2010, 55(3):285-291

 


PREPARATION AND QUALITY CONTROL OF LUTETIUM-177 BLEOMYCIN AS A POSSIBLE THERAPEUTIC AGENT



Hassan Yousefnia, Amir R. Jalilian, Samaneh Zolghadri, Ali Bahrami-Samani,
Simindokht Shirvani-Arani, Mohammad Ghannadi-Maragheh


Radiopharmaceutical Research and Development Laboratory (RRDL),
Nuclear Science and Technology Research Institute (NSTRI),
Postal code: 14155-1339, Tehran, Iran



Due to interesting therapeutic properties of 177Lu and antineoblastic antibiotic, bleomycin (BLM), 177Lu-bleomycin (177Lu-BLM) was developed as a possible therapeutic compound. Lu-177 of 2.6–3 GBq/mg specific activity was obtained by irradiation of a natural Lu2O3 sample with a thermal neutron flux of 4 × 1013 n·cm–2·s–1. The product was converted into chloride form which was further used for labeling of BLM. In optimized conditions a radiochemical purity of 98% was obtained for 177Lu-BLM shown by instant thin-layer chromatography (ITLC) (specific activity, 740 GBq/mmole). Biodistribution studies of Lu-177 chloride and 177Lu-BLM were performed in wild-type rats. The accumulation of the radiolabeled compound in lungs, liver and spleen demonstrates a pattern similar to the other radiolabeled bleomycins. Lu-BLM is a possible therapeutic agent in human malignancies and the efficacy of the compound should be tested in various tumor-bearing models.


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