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TLX102

Development stage
Preclinical
Lead developer
Telix Pharmaceuticals
Modality
Alpha Emitters → Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta Emitters → Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
01

Overview

TLX102 is an investigational targeted alpha radiopharmaceutical consisting of the amino acid analog 4-[211At]astato-L-phenylalanine labeled with the alpha-emitting radionuclide astatine-211, being developed by Telix Pharmaceuticals as a LAT1-targeted therapy for malignancies such as multiple myeloma and brain cancers. It exploits overexpression of the large neutral amino acid transporter LAT1/LAT2 on tumor and blood–brain barrier cells to deliver high–linear energy transfer alpha radiation selectively to cancer cells, causing potent, localized DNA damage while aiming to spare surrounding normal tissues. TLX102 has received FDA Orphan Drug Designation for multiple myeloma and is currently in preclinical development as a potential complement to Telix’s iodine-131–labeled LAT1 agent TLX101 and related LAT1 theranostic programs.

Other names
4-[211At]astato-L-phenylalanine4-[211At] astato-l-phenylalanine
02

Targets

SLC7A5 (Large neutral amino acid transporter small subunit 1)

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