Drug intelligence / Profile preview

Tb-161-DOTAGA-Glu-(FAPI)2

Development stage
Unknown
Lead developer
Telix Pharmaceuticals
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

Tb-161-DOTAGA-Glu-(FAPI)2 is an investigational, next-generation dimeric radioligand therapy designed to target fibroblast activation protein (FAP). The drug consists of a dimeric FAP inhibitor (DOTAGA-Glu-(FAPI)2) labeled with the therapeutic radionuclide terbium-161 (Tb-161). The dimeric structure of the targeting ligand provides enhanced tumor uptake and prolonged tumor retention compared to monomeric FAP inhibitors. Terbium-161 is an emerging radionuclide that offers a therapeutic advantage over lutetium-177 by emitting both low-energy beta particles and short-range Auger electrons, delivering a highly localized radiation dose to micro-metastases while sparing surrounding healthy tissue. The agent is being developed by Telix Pharmaceuticals (as part of its TLX400 program) in collaboration with the Thera4Care consortium for the treatment of FAP-expressing advanced solid tumors, including sarcomas, ovarian cancer, and pancreatic cancer.

Other names
161Tb-DOTAGA-Glu-(FAPI)2161Tb-DOTAGA.Glu.(FAPi)2161Tb-TLX400Tb-161-DOTAGA.Glu.(FAPi)2Tb-161-TLX400Tb161-TLX400Tb 161-TLX400terbium-161-DOTAGA-Glu-(FAPI)2
02

Targets

FAP (Fibroblast activation protein alpha)

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