Targeted alpha therapy using short-lived alpha-particles and the promise of nanobodies as targeting vehicle.
Targeted alpha therapy using short-lived alpha-particles and the promise of nanobodies as targeting vehicle.
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DOI：
10.1080/14712598.2016.1185412
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发表时间：
2016-08
影响因子：
4.6
通讯作者：
Devoogdt N
中科院分区：
文献类型：
--
作者：
Dekempeneer Y;Keyaerts M;Krasniqi A;Puttemans J;Muyldermans S;Lahoutte T;D'huyvetter M;Devoogdt N
简介：专门定义靶点的靶向生物分子和提供细胞毒性有效负载的放射性核素的组合提供了一种破坏癌细胞的特定方法。靶向放射性核素治疗 (TRNT) 旨在向癌细胞提供细胞毒性辐射，并对周围健康组织造成最小的毒性。使用 α 粒子辐射的最新进展强调了它们以高度局部化和有毒的方式产生辐射的潜力，因为它们的电离水平高且在组织中的范围短。 涵盖领域：我们回顾了靶向α疗法（TAT）的重要性，并重点关注纳米抗体作为潜在的有益载体。近年来，纳米抗体作为分子成像和 TRNT 的独特抗原特异性载体受到了广泛的评估。 专家观点：我们预计纳米抗体的高效靶向能力和快速清除能力为TAT提供了巨大的潜力。更具体地说，我们认为纳米抗体的药代动力学特性与短寿命α粒子发射放射性核素Astatine-211和Bismuth-213的有趣的衰变特性完美匹配，并提供了一种有趣的治疗选择，特别是针对微转移癌和残留疾病。
Introduction: The combination of a targeted biomolecule that specifically defines the target and a radionuclide that delivers a cytotoxic payload offers a specific way to destroy cancer cells. Targeted radionuclide therapy (TRNT) aims to deliver cytotoxic radiation to cancer cells and causes minimal toxicity to surrounding healthy tissues. Recent advances using α-particle radiation emphasizes their potential to generate radiation in a highly localized and toxic manner because of their high level of ionization and short range in tissue. Areas covered: We review the importance of targeted alpha therapy (TAT) and focus on nanobodies as potential beneficial vehicles. In recent years, nanobodies have been evaluated intensively as unique antigen-specific vehicles for molecular imaging and TRNT. Expert opinion: We expect that the efficient targeting capacity and fast clearance of nanobodies offer a high potential for TAT. More particularly, we argue that the nanobodies’ pharmacokinetic properties match perfectly with the interesting decay properties of the short-lived α-particle emitting radionuclides Astatine-211 and Bismuth-213 and offer an interesting treatment option particularly for micrometastatic cancer and residual disease.