Czech Technical University in Prague, Faculty of Nuclear Sciences and Physical Engineering, Prague CZ-11519, Czech Republic.
Vernadsky Institute of Geochemistry and Analytical Chemistry, Moscow 119991, Russia.
Molecules. 2018 Mar 5;23(3):581. doi: 10.3390/molecules23030581.
This review summarizes recent progress and developments as well as the most important pitfalls in targeted alpha-particle therapy, covering single alpha-particle emitters as well as alpha-particle generators. It discusses the production of radionuclides like At, Ra, Ac/Bi, labelling and delivery employing various targeting vectors (small molecules, chelators for alpha-emitting nuclides and their biomolecular targets as well as nanocarriers), general radiopharmaceutical issues, preclinical studies, and clinical trials including the possibilities of therapy prognosis and follow-up imaging. Special attention is given to the nuclear recoil effect and its impacts on the possible use of alpha emitters for cancer treatment, proper dose estimation, and labelling chemistry. The most recent and important achievements in the development of alpha emitters carrying vectors for preclinical and clinical use are highlighted along with an outlook for future developments.
本文综述了靶向 α 粒子治疗的最新进展和发展，以及最重要的陷阱，涵盖了单 α 粒子发射体和 α 粒子发生器。它讨论了放射性核素的生产，如 At、Ra、Ac/Bi，使用各种靶向载体（小分子、α 发射核素及其生物分子靶标以及纳米载体）进行标记和输送，一般放射性药物问题，临床前研究和临床试验，包括治疗预后和随访成像的可能性。特别关注核反冲效应及其对可能将 α 发射器用于癌症治疗、适当剂量估计和标记化学的影响。重点介绍了用于临床前和临床应用的携带载体的 α 发射器的最新和重要进展，并展望了未来的发展。
