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铼-188:来自(188)W/(188)Re发生器的可获得性及当前应用状况

Rhenium-188: availability from the (188)W/(188)Re generator and status of current applications.

作者信息

Pillai M R A, Dash Ashutosh, Knapp F F

机构信息

Radiopharmceuticals Division, Bhabha Atomic Research Centre, Mumbai 400 085, India.

出版信息

Curr Radiopharm. 2012 Jul;5(3):228-43. doi: 10.2174/1874471011205030228.

Abstract

Rhenium-188 is one of the most readily available generator derived and useful radionuclides for therapy emitting β(-) particles (2.12 MeV, 71.1% and 1.965 MeV, 25.6%) and imageable gammas (155 keV, 15.1%). The (188)W/(188)Re generator is an ideal source for the long term (4-6 months) continuous availability of no carrier added (nca) (188)Re suitable for the preparation of radiopharmaceuticals for radionuclide therapy. The challenges associated with the double neutron capture route of production of the parent (188)W radionuclide have been a major impediment in the progress of application of (188)Re. Tungsten-188 of adequate specific activity can be prepared only in 2-3 of the high flux reactors operating in the World. Several useful technologies have been developed for the preparation of clinical grade (188)W/(188)Re generators. Since the specific activity of (188)W used in the generator is relatively low 185 GBq( < 5 Ci)/g], the eluted (188)ReO(4)(-) can have low radioactive concentration often insufficient for radiopharmaceutical preparation. However, several efficient post elution concentration techniques have been developed that yield clinically useful (188)ReO(4)(-) solutions. Rhenium-188 has been used for the preparation of therapeutic radiopharmaceuticals for the management of diseases such as bone metastasis, rheumatoid arthritis and primary cancers. Several early phase clinical studies using radiopharmaceuticals based on (188)Re-labeled phosphonates, antibodies, peptides, lipiodol and particulates have been reported. This article reviews the availability and use of (188)Re including a discussion of why broader use of (188)Re has not progressed as expected as a popular radionuclide for therapy.

摘要

铼-188是最容易从发生器获得且对治疗有用的放射性核素之一,它发射β(-)粒子(2.12兆电子伏,71.1%;1.965兆电子伏,25.6%)以及可用于成像的γ射线(155千电子伏,15.1%)。(188)钨/(188)铼发生器是长期(4 - 6个月)持续提供无载体添加(nca)(188)铼的理想来源,这种铼适用于制备放射性核素治疗的放射性药物。与母体(188)钨放射性核素的双中子俘获生产途径相关的挑战一直是(188)铼应用进展的主要障碍。具有足够比活度的钨-188只能在世界上运行的2 - 3座高通量反应堆中制备。已经开发了几种用于制备临床级(188)钨/(188)铼发生器的有用技术。由于发生器中使用的(188)钨的比活度相对较低[185吉贝可(<5居里)/克],洗脱的(188)ReO(4)(-)可能具有低放射性浓度,这对于放射性药物制备往往是不够的。然而,已经开发了几种有效的洗脱后浓缩技术,可产生临床上有用的(188)ReO(4)(-)溶液。铼-188已用于制备治疗性放射性药物,用于治疗骨转移、类风湿性关节炎和原发性癌症等疾病。已经报道了几项使用基于(188)铼标记的膦酸盐、抗体、肽、碘油和微粒的放射性药物的早期临床研究。本文综述了(188)铼的可得性和用途,包括讨论为什么(188)铼作为一种流行的治疗放射性核素,其更广泛的应用没有如预期那样取得进展。

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