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Drug intelligence / Profile preview
terbium-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
terbium-161 DOTAGA.Glu.(FAPi)2 (also known as 161Tb-DOTAGA.Glu.(FAPi)2 or TLX400) is a next-generation, dimeric fibroblast activation protein (FAP)-targeted radioligand therapeutic candidate. It consists of a FAP-inhibiting homodimer (FAPi)2 connected via a central glutamic acid (Glu) linker to a DOTAGA chelator, which is radiolabeled with the isotope terbium-161 (161Tb). Originally developed at the Johannes Gutenberg-Universität Mainz and subsequently in-licensed by Telix Pharmaceuticals, the candidate targets FAP, which is highly expressed on cancer-associated fibroblasts (CAFs) within the tumor microenvironment of various solid tumors. Terbium-161 is a promising therapeutic radionuclide that emits both beta-minus particles and low-energy Auger/conversion electrons. The short-range Auger electrons deliver highly localized radiation, making the agent particularly effective at destroying micro-metastatic disease while sparing surrounding healthy tissue. The drug is being evaluated in clinical trials for FAP-expressing metastatic solid tumors, including ovarian cancer, pancreatic cancer, and sarcomas.
- Other names
- 161Tb-DOTAGA.Glu.(FAPi)2terbium (161Tb) DOTAGA.Glu.(FAPi)2terbium-161 DOTAGA.Glu.(FAPi)2
02
Targets
FAP (Fibroblast activation protein alpha)
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