Prostate-specific membrane antigen(PSMA) is a useful target for diagnostic and therapeutic applications,and it is demonstrated that ^(68) Ga in conjugation with DKFZPSMA-617 is better than ^(68)Ga-PSMA-1 in biodistrib...Prostate-specific membrane antigen(PSMA) is a useful target for diagnostic and therapeutic applications,and it is demonstrated that ^(68) Ga in conjugation with DKFZPSMA-617 is better than ^(68)Ga-PSMA-1 in biodistribution data after 1 h,but more preclinical data are still required.In this paper,we presented the additional preclinical data for ^(68)Ga-DKFZ-PSMA-617 and relevant aspects of its production.^(68) Ga was obtained from the SnO_2-based ^(68)Ge/ ^(68) Ga generator.Optimum conditions(p H,temperature,time and ligand concentration) for ^(68)Ga-DKFZPSMA-617 preparation were studied.Radiochemical purity of the radiolabeled compound was determined by HPLC and RTLC.After stability assessments,the complex was intravenously injected into rats.HPLC and ITLC characterizations indicated that the radiopharmaceutical could be prepared with radiochemical purity of [96 % and specific activity of 308.3 TBq/mmol at the optimized conditions(p H of 3.5–4,ligand amount of 2.4 nmol,temperature of90–95 C and reaction time of 10 min).Also,the biodistribution data showed no undesirable uptake in nontarget organs at any interval after injection.In fact,the activity is cleaned from blood and excreted rapidly via the kidneys.Generally,this compound can be considered as a wellestablished PET imaging agent.展开更多
Bleomycins(BLMs), as tumor-seeking antibiotics, have been used for over 20 years in treatment of several types of cancers. Several radioisotopes are used in radiolabeling of BLMs for therapeutic and diagnostic purpose...Bleomycins(BLMs), as tumor-seeking antibiotics, have been used for over 20 years in treatment of several types of cancers. Several radioisotopes are used in radiolabeling of BLMs for therapeutic and diagnostic purposes. An important points in developing new radiopharmaceuticals, especially therapeutic agents, is the absorbed dose delivered in critical organs. In this work, absorbed dose to organs after injection of ^(153)Sm-,^(177)Lu- and ^(166)Ho-labeled BLM was investigated by radiation dose assessment resource(RADAR) method based on biodistribution data in wild-type rats. The absorbed dose effect of the radionuclides was evaluated. The maximum absorbed dose for the complexes was observed in the kidneys, liver and lungs. For all the radiolabeled BLMs,bone and red marrow received considerable absorbed dose. Due to the high energy beta particles emitted by ^(166)Ho, higher absorbed dose is observed for ^(166)Ho-BLM in the most organs. The reported data can be useful for the determination of the maximum permissible injected activity of the radiolabeled BLMs in the treatment planning programs.展开更多
文摘Prostate-specific membrane antigen(PSMA) is a useful target for diagnostic and therapeutic applications,and it is demonstrated that ^(68) Ga in conjugation with DKFZPSMA-617 is better than ^(68)Ga-PSMA-1 in biodistribution data after 1 h,but more preclinical data are still required.In this paper,we presented the additional preclinical data for ^(68)Ga-DKFZ-PSMA-617 and relevant aspects of its production.^(68) Ga was obtained from the SnO_2-based ^(68)Ge/ ^(68) Ga generator.Optimum conditions(p H,temperature,time and ligand concentration) for ^(68)Ga-DKFZPSMA-617 preparation were studied.Radiochemical purity of the radiolabeled compound was determined by HPLC and RTLC.After stability assessments,the complex was intravenously injected into rats.HPLC and ITLC characterizations indicated that the radiopharmaceutical could be prepared with radiochemical purity of [96 % and specific activity of 308.3 TBq/mmol at the optimized conditions(p H of 3.5–4,ligand amount of 2.4 nmol,temperature of90–95 C and reaction time of 10 min).Also,the biodistribution data showed no undesirable uptake in nontarget organs at any interval after injection.In fact,the activity is cleaned from blood and excreted rapidly via the kidneys.Generally,this compound can be considered as a wellestablished PET imaging agent.
文摘Bleomycins(BLMs), as tumor-seeking antibiotics, have been used for over 20 years in treatment of several types of cancers. Several radioisotopes are used in radiolabeling of BLMs for therapeutic and diagnostic purposes. An important points in developing new radiopharmaceuticals, especially therapeutic agents, is the absorbed dose delivered in critical organs. In this work, absorbed dose to organs after injection of ^(153)Sm-,^(177)Lu- and ^(166)Ho-labeled BLM was investigated by radiation dose assessment resource(RADAR) method based on biodistribution data in wild-type rats. The absorbed dose effect of the radionuclides was evaluated. The maximum absorbed dose for the complexes was observed in the kidneys, liver and lungs. For all the radiolabeled BLMs,bone and red marrow received considerable absorbed dose. Due to the high energy beta particles emitted by ^(166)Ho, higher absorbed dose is observed for ^(166)Ho-BLM in the most organs. The reported data can be useful for the determination of the maximum permissible injected activity of the radiolabeled BLMs in the treatment planning programs.
