Open AccessRealizing Clinical Trials with Astatine-211: The Chemistry Infrastructure
Author(s) -
Sture Lindegren,
Per Albertsson,
Tom Bäck,
Holger Jensen,
Stig Palm,
Emma Aneheim
Publication year - 2020
Publication title -
cancer biotherapy and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.716
H-Index - 59
eISSN - 1557-8852
pISSN - 1084-9785
DOI - 10.1089/cbr.2019.3055
Subject(s) - nuclide , biochemical engineering , radiochemistry , computer science , chemistry , medical physics , medicine , engineering , physics , nuclear physics
Despite the consensus around the clinical potential of the α-emitting radionuclide astatine-211 ( 211 At), there are only a limited number of research facilities that work with this nuclide. There are three main reasons for this: (1) Scarce availability of the nuclide. Despite a relatively large number of globally existing cyclotrons capable of producing 211 At, few cyclotron facilities produce the nuclide on a regular basis. (2) Lack of a chemical infrastructure, that is, isolation of 211 At from irradiated targets and the subsequent synthesis of an astatinated product. At present, the research groups that work with 211 At depend on custom systems for recovering 211 At from the irradiated targets. Setting up and implementing such custom units require long lead times to provide a proper working system. (3) The chemistry of 211 At. Compared with radiometals there are no well-established and generally accepted synthesis methods for forming sufficiently stable bonds between 211 At and the tumor-specific vector to allow for systemic applications. Herein we present an overview of the infrastructure of producing 211 At radiopharmaceuticals, from target to radiolabeled product including chemical strategies to overcome hurdles for advancement into clinical trials with 211 At.