@article{oai:repo.qst.go.jp:00085578, author = {Yasuhiro, Oshima and Hiroyuki, Suzuki and Hirofumi, Hanaoka and Ichiro, Sasaki and Shigeki, Watanabe and Hiromitsu, Haba and Yasushi, Arano and Yoshito, Tsushima and Noriko, Ishioka and Yasuhiro, Oshima and Ichiro, Sasaki and Shigeki, Watanabe and Noriko, Ishioka}, journal = {QST Takasaki Annual Report 2020}, month = {Mar}, note = {Targeted α-radionuclide therapy has attracted attention as a promising therapy for refractory cancers. However, the application is limited to certain types of cancer. Since L-type amino acid transporter 1 (LAT1) is highly expressed in various human cancers, radiopharmaceuticals targeting LAT1 would enable the wider use of targeted α-therapy. We previously developed fluorine-18 (18F)- or bromine-76 (76Br)-labeled amino acid tracers targeting LAT1. Among them, 2-[18F]- or 2-[76Br]-labeled α-methyl-L-phenylalanine analog was specifically taken up by tumor via LAT1, while they were rapidly cleared from body and excreted into urine. Since 18F and 76Br belong to radiohalogen, astatine-211 (211At), an α-emitting halogen, labeled α-methyl-L-phenylalanine is expected to show high tumor accumulation and preferred pharmacokinetics. In this study, we newly synthesized 2-[211At]astato-α-methyl-L-phenylalanine (2-[211At]AAMP), and evaluated its potential as a therapeutic agent.}, pages = {90--90}, title = {Preclinical evaluation of new α-radionuclide therapy targeting LAT1: 2-[211At]astato-α-methyl-L-phenylalanine in tumor-bearing model}, year = {2022} }