更新于：2024-11-21

Sodium Perrhenate [Re-188]

高铼[Re-188]酸钠

更新于：2024-11-21

概要

概要

基本信息

药物类型

小分子偶联药物、治疗用放射药物

别名

Na[188]ReO4、高铼[188Re]酸钠

靶点-

作用机制-

治疗领域-

在研适应症-

非在研适应症-

原研机构

上海原子科兴药业有限公司

在研机构-

非在研机构

上海原子科兴药业有限公司

最高研发阶段无进展临床1期

首次获批日期-

最高研发阶段(中国)无进展

特殊审评-

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结构

使用我们的ADC技术数据为新药研发加速。

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关联

100 项与高铼[Re-188]酸钠相关的临床结果

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100 项与高铼[Re-188]酸钠相关的转化医学

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100 项与高铼[Re-188]酸钠相关的专利（医药）

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项与高铼[Re-188]酸钠相关的文献（医药）

2019-10-01·Investigational New Drugs3区 · 医学

Biodistribution, pharmacokinetics and radioimmunotherapy of 188Re-cetuximab in NCI-H292 human lung tumor-bearing nude mice

3区 · 医学

Article

作者: Kuo, Wan-I ; Chang, Ya-Jen ; Ho, Chung-Li ; Cheng, Kai-Hung ; Lan, Keng-Li ; Lee, Wan-Chi ; Chang, Chih-Hsien

Background Cetuximab is a fully humanized IgG1 subclass monoclonal that binds specifically to the human epidermal growth factor receptor (EGFR). Although EGFR is expressed in normal cells, the overexpression of EGFR is detected in many human cancers, such as colon, rectum and lung tumors. In this study, cetuximab with a combination of radiotherapy nuclear ¹⁸⁸Re achieved better therapeutic effect on lung cancer. Methods¹⁸⁸Re-cetuximab administered by the i.v. route in human NCI-H292 lung tumor-bearing mice was investigated. NanoSPECT/CT images were taken to evaluate the distribution and tumor targeting of ¹⁸⁸Re-cetuximab in mice. The anti-tumor effect of ¹⁸⁸Re-cetuximab was assessed by the tumor growth inhibition, survival ratio. Results For nanoSPECT/CT imaging, a significant uptake in tumor was observed at 24 and 48 h following the injection of ¹⁸⁸Re-cetuximab. The anti-tumor effect of ¹⁸⁸Re-cetuximab was assessed by tumor growth inhibition and the survival ratio. The tumor-bearing mice treated with ¹⁸⁸Re-cetuximab showed a better mean tumor growth inhibition rate (MGI = 0.049) and longer median survival time and lifespan (62.50 d; 70.07%) than those treated with ¹⁸⁸Re-perrhenate and cetuximab only by single injection. A synergistic effect of tumor growth inhibition was observed with the combination index exceeding one for ¹⁸⁸Re-cetuximab (CI = 6.135 and 9.276). Conclusion The tumor targeting and localization of 188Re-cetuximab were confirmed in this study. Synergistic therapeutic efficacy was demonstrated for the radioimmunotherapy of ¹⁸⁸Re-cetuximab. The results of this study reveal the potential advantage and benefit obtained from ¹⁸⁸Re-cetuximab for diagnosis and therapy of oncology applications in the future.

2018-01-01·Indian Journal of Nuclear Medicine

Rhenium-188 hydroxyethane 1,1-diphosphonic acid (HEDP) for bone pain palliation using BARC-HEDP kits versus Pars-HEDP kits: A comparison on preparation and performance aspects at hospital radiopharmacy

Article

作者: Mallia, Madhava Balakrishna ; Kameswaran, Mythili ; Pandiyan, Arun ; Chirayil, Viju ; Dash, Ashutosh ; Ramakurup, Radhakrishnan Edathuruthy Kalarickal ; Shinto, Ajit

PURPOSE OF THE STUDYRhenium-188 hydroxyethane 1,1-diphosphonic acid (HEDP) is a clinically established radiopharmaceutical for palliation of bone pain due to osseous metastases. Recently, the Bhabha Atomic Research Centre (BARC) had developed a freeze-dried kit for the preparation of rhenium-188 HEDP. The present study compares the radiochemistry aspects of indigenous BARC-HEDP kits with commercially available HEDP kits from Pars Isotope Company, Iran.MATERIALS AND METHODSFreeze-dried HEDP kits were obtained from Radiopharmaceuticals Division, BARC, and Pars Isotope Company, Iran. Following recommended procedures, rhenium-188 HEDP was prepared using freeze-dried kits from both sources using freshly eluted rhenium-188 sodium perrhenate obtained from a commercial tungsten-188/rhenium-188 generator.RESULTSBoth kits could be used for the preparation of rhenium-188 HEDP in >95% radiochemical purity (RCP). Rhenium-188 HEDP prepared from both kits showed comparable in vitro stability as well as pharmacokinetic properties. The normal bone-to-soft tissue ratio observed for rhenium-188 HEDP prepared using BARC-HEDP kit and Pars-HEDP kit was 1.993 and 1.416, respectively.CONCLUSIONSBoth HEDP kits provided a user-friendly solution for the preparation of rhenium-188 HEDP. While Pars-HEDP-kit permits the addition of only 2 mL of rhenium-188 perrhenate solution per kit vial, BARC-HEDP-kit allows up to 5 mL. This feature permits the preparation of patient dose of rhenium-188 HEDP even with older generators providing rhenium-188 perrhenate having a low radioactive concentration (activity/mL). In addition, availability of an indigenous product is always preferable over imported options.

2012-12-01·International Journal of Radiation Biology4区 · 医学

Reduction in clonogenic survival of sodium-iodide symporter (NIS)-positive cells following intracellular uptake of^99mTc versus¹⁸⁸Re

4区 · 医学

Article

作者: Freudenberg, Robert ; Wendisch, Maria ; Wunderlich, Gerd ; Kotzerke, Joerg ; Runge, Roswitha

PURPOSECellular radionuclide uptake increases the heterogeneity of absorbed dose to biological structures. Dose increase depends on uptake yield and emission characteristics of radioisotopes. We used an in vitro model to compare the impact of cellular uptake of (188)Re-perrhenate and (99m)Tc-pertechnetate on cellular survival.MATERIALS AND METHODSRat thyroid PC Cl3 cells in culture were incubated with (188)Re or (99m)Tc in the presence or absence of perchlorate for 1 hour. Clonogenic cell survival was measured by colony formation. In addition, intracellular radionuclide uptake was quantified.RESULTSDose effect curves were established for (188)Re and (99m)Tc for various extra- and intracellular distributions of the radioactivity. In the presence of perchlorate, no uptake of radionuclides was detected and (188)Re reduced cell survival more efficiently than (99m)Tc. A(37), the activity that is necessary to yield 37% cell survival was 14 MBq/ml for (188)Re and 480 MBq/ml for (99m)Tc. In the absence of perchlorate, both radionuclides showed similar uptakes; however, A(37) was reduced by 30% for the beta-emitter and by 95% for (99m)Tc. The dose D(37) that yields 37% cell survival was between 2.3 and 2.8 Gy for both radionuclides.CONCLUSIONSUptake of (188)Re and (99m)Tc decreased cell survival. Intracellular (99m)Tc yielded a dose increase that was higher compared to (188)Re due to emitted Auger and internal conversion-electrons. Up to 5 Gy there was no difference in radiotoxicity of (188)Re and (99m)Tc. At doses higher than 5 Gy intracellular (99m)Tc became less radiotoxic than (188)Re, probably due to a non-uniform lognormal radionuclide uptake.

100 项与高铼[Re-188]酸钠相关的药物交易

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