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3rd International Congress 3rd International of Nuclear Congress Medicine of Nuclear & 15th Medicine Iranian Annual & 15th Iranian Congress Annual of Nuclear Congress Medicine of Nuclear Medicine Shahid Beheshti Shahid Beheshti University University of Medical Sciences of Medical 19-21 Sciences May 201119-21 May 2011 Development of [177Lu]-Tetra phenyl porphyrin complexes as possible imaging agents Hassan Yousefnia 1 , Amir Reza Jalilian 1 , Samaneh Zolghadri 1 , Yousef Fazaeli 2 , Ali Bahrami Samani 1 , Mohammad Ghannadi-Maragheh 1 1 Nuclear Science and Technology Research Institute 2 Agriculture, Medicine and Industry Research School Due to interesting therapeutic properties of 177Lu and tumor avidity of tetraphenyl porphyrins (TPPs), 177Lu-tetraphenyl porphyrin (177Lu-TPP) was developed as a possible therapeutic compound. Lu- 177 of 2.6-3 GBq/mg specific activity was obtained by irradiation of natural Lu2O3 sample with thermal neutron flux of 4—1013 n.cm- 2.s-1. [17Lu]labeled tetraphenyl porphyrin ([177Lu]-TPP) was prepared using freshly prepared [177Lu]-LuCl3 and tetraphenyl porphyrin (TPPH2) for 30-60 min at 25°C (radiochemical purity: >97±1% ITLC, >98±0.5 % HPLC, specific activity: 13-14 GBq/mmol). Stability of the complex was checked in final formulation and human serum for 24 h. The partition coefficient was calculated for the compound (log P. 1.89). The biodistribution of the labeled compound in vital organs of wild-type rats was studied using scarification studies and SPECT imaging up to 24 h. A detailed comparative pharmacokinetic study performed for 177Lu cation and [177Lu]-TPP. The complex is mostly washed out from the circulation through kidneys and can be an interesting tumor imaging/targeting agent due to low liver uptake and rapid excretion through the urinary tract. Keywords: 177Lu, tetra phenyl prophyrin, biodistribution 152
3rd International Congress of of Nuclear Medicine & & 15th 15th Iranian Annual Annual Congress of Congress of Nuclear Medicine Shahid Beheshti Shahid Beheshti University University of Medical of Medical Sciences Sciences 19-21 19-21 May May 2011 Production, quality control and biological evaluation of 177Lu- 1,2-propylene di-amino tetra(methy1enephosphonicAcid) as a possible bone palliation agent Hassan Yousefnia, Amir Reza Jalilian, Samaneh Zolghadri, Zohreh Naseri, Ali Bahrami-Samani, Mohammad Ghannadi Maragheh Nuclear Science and Technology Research Institute In this study, production, quality control and biodistribution studies of a newly developed therapeutic compound have been presented followed by imaging studies in wild-type rodents. In this study, 177Lu-1,2-propylene di-amino tetra(methy1enephosphonicAcid) (PDTMP) complex was prepared successfully using synthesized PDTMP ligand and 177LuCl3. Lu-177 chloride was obtained by thermal neutron irradiation (4—1013 n.cm-2s-1) of natural Lu2O3 samples. Radiochemical purity of 177Lu-PDTMP was checked by ITLC (>99%). Stability studies of the complex in the final preparation and in the presence of human serum were performed up to 72h. The biodistribution of 177Lu-PDTMP and 177LuCl3 in wild-type rats was checked in animal tissues up to 7 days. The produced 177Lu-PDTMP properties suggest a possible new bone palliative therapeutic to overcome the metastatic bone pains. Keywords: Lu-177, PDTMP, Radiopharmaceutical, Therapy, Biodistribution 153
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