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211At-APA
- Development stage
- Unknown
- Lead developer
- Telix Pharmaceuticals
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intra-arterial, Intravenous
01
Overview
211At-APA (also known as TLX102) is an investigational, small-molecule targeted alpha therapy (TAT) radiopharmaceutical developed by Telix Pharmaceuticals. It consists of the amino acid L-phenylalanine labeled with the alpha-emitting radioisotope astatine-211 (211At). 211At-APA targets L-type amino acid transporter 1 (LAT1, encoded by SLC7A5), which is highly expressed on the blood-brain barrier and overexpressed in various cancers, including glioblastoma multiforme (GBM), leptomeningeal disease (LMD), and multiple myeloma. By binding to LAT1, 211At-APA is internalized into cancer cells, where the decay of astatine-211 releases high-energy, short-range alpha particles that induce lethal double-strand DNA breaks, while minimizing damage to surrounding healthy tissues.
- Other names
- 211At-astato-L-phenylalanine4-[211At]APA4-[211At]astato-L-phenylalanine4-[211At]astatophenylalanine4-APA4-astatophenylalanineastatine-211-phenylalanineastatine211-phenylalanineastatine 211-phenylalanine
02
Targets
SLC7A5 (Large neutral amino acid transporter small subunit 1)
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