Terbium-161 in nuclear medicine: Preclinical and clinical progress in comparison with lutetium-177

IF 3.6 4区 医学 Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING
František Trejtnar , Pavel Bárta , Ján Kozempel , Martin Vlk , Anna Ďurinová , Monika Kuchařová , Petr Pávek
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Abstract

The use of new radiopharmaceuticals labeled with lutetium-177 represents a successful translation of experimental results into clinical practice. Recent experimental data suggests that terbium-161 might well follow the example of lutetium-177 regarding applicability in nuclear medicine. Similarly to lutetium-177, the terbium-161 emits beta particles and gamma-radiation, although terbium-161 emits short-ranged conversion and Auger electrons, creating an effect that may eliminate smaller tumor metastases more effectively than lutetium-177. Terbium-161 may exert a higher radiobiological effect in the target tissues in comparison with lutetium-177, a difference which makes possible a reduction in the doses of radioactivity administered. Further, due to the similar chemical properties of lutetium-177 and terbium-161, similar radiolabeling techniques can be used. The differences found in preclinical experiments on radiotoxicity of the counterparts seem to be minor. Despite intensive progress, the number of preclinical studies on 161Tb-labeled agents is still not comparable to studies on lutetium-177. Clinical trials with 161Tb-labeled radiopharmaceuticals focused on the treatment of prostate cancer and selected neuroendocrine tumors have already begun, although none of them have been completed yet.

Abstract Image

terium -161与luteium -177在核医学中的临床前与临床研究进展
使用标记有镥-177的新型放射性药物代表了将实验结果成功地转化为临床实践。最近的实验数据表明,terium -161很可能效仿luteium -177在核医学中的适用性。与镥-177类似,铽-161释放出β粒子和γ辐射,尽管铽-161释放出短程转换电子和俄歇电子,产生的效果可能比镥-177更有效地消除较小的肿瘤转移。与镥-177相比,铽-161可能在靶组织中发挥更高的放射生物学效应,这一差异使得减少所施用的放射性剂量成为可能。此外,由于镥-177和铽-161的化学性质相似,可以使用类似的放射性标记技术。在临床前实验中发现的放射性毒性差异似乎很小。尽管进展迅速,但161tb标记药物的临床前研究数量仍无法与luteium -177的研究相比。用161tb标记的放射性药物治疗前列腺癌和特定神经内分泌肿瘤的临床试验已经开始,尽管还没有完成。
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来源期刊
Nuclear medicine and biology
Nuclear medicine and biology 医学-核医学
CiteScore
6.00
自引率
9.70%
发文量
479
审稿时长
51 days
期刊介绍: Nuclear Medicine and Biology publishes original research addressing all aspects of radiopharmaceutical science: synthesis, in vitro and ex vivo studies, in vivo biodistribution by dissection or imaging, radiopharmacology, radiopharmacy, and translational clinical studies of new targeted radiotracers. The importance of the target to an unmet clinical need should be the first consideration. If the synthesis of a new radiopharmaceutical is submitted without in vitro or in vivo data, then the uniqueness of the chemistry must be emphasized. These multidisciplinary studies should validate the mechanism of localization whether the probe is based on binding to a receptor, enzyme, tumor antigen, or another well-defined target. The studies should be aimed at evaluating how the chemical and radiopharmaceutical properties affect pharmacokinetics, pharmacodynamics, or therapeutic efficacy. Ideally, the study would address the sensitivity of the probe to changes in disease or treatment, although studies validating mechanism alone are acceptable. Radiopharmacy practice, addressing the issues of preparation, automation, quality control, dispensing, and regulations applicable to qualification and administration of radiopharmaceuticals to humans, is an important aspect of the developmental process, but only if the study has a significant impact on the field. Contributions on the subject of therapeutic radiopharmaceuticals also are appropriate provided that the specificity of labeled compound localization and therapeutic effect have been addressed.
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