Recent progress of astatine-211 in endoradiotherapy:Great advances from fundamental properties to targeted radiopharmaceuticals

摘要

Astatine-211(^(211)At,t_(1/2)=7.21 h)emitting twoαparticles with energies of 5.87 and 7.45 MeV,can lead to a high linear energy transfer(LET=98.84 ke V/μm)and short tissue range(50~90μm).Since the 1950s,^(211)At had stepped into endoradiotherapy and has always been regarded as one of the most promisingα-emitters for targeted-alpha therapy(TAT)in various malignancies.In the past two decades,^(211)At related radiopharmaceuticals have achieved great progress in the studies of basic physicochemical properties of astatine,^(211)At labeling strategies,preclinical and clinical studies,producing profound effects in nuclear medicine.This work will give a panorama of^(211)At-related researches in the recent 20 years,which will cover both the fundamental insights of^(211)At radiochemistry and applied labeling compounds.It can provide some important hints for the studies of TAT and other radiopharmaceuticals applied in tumor radiotherapy.