α-Emitting cancer therapy using 211 At-AAMT targeting LAT1.

α-Methyl-L-tyrosine (AMT) has high affinity for the cancer-specific L-type amino acid transporter 1 (LAT1). Thus, we establish an anti-cancer therapy, with 211 At-labeled α-methyl-L-tyrosine (211 At-AAMT) as a carrier of 211 At into tumors. 211 At-AAMT had high affinity for LAT1, inhibited tumor cell growth, and induced DNA double-strand breaks in vitro. We evaluated the accumulation of 211 At-AAMT in vivo and the role of LAT1. Treatment with 0.4 MBq/mouse 211 At-AAMT inhibited tumor growth in the PANC-1 tumor model and 1 MBq/mouse 211 At-AAMT inhibited metastasis in the lung of the B16F10 metastasis model. Our results suggest that 211 At is useful for anti-cancer therapy and LAT1 was suitable as a target for radionuclide therapy. This article is protected by copyright. All rights reserved.