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Drug intelligence / Profile preview
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
DOTAGA.Glu.(FAPi)2 is a next-generation homodimeric fibroblast activation protein (FAP) inhibitor (FAPi) designed for theranostic applications in nuclear medicine. It consists of two FAP-targeting UAMC-1110-based moieties connected via a central glutamic acid (Glu) linker to a DOTAGA chelator. This dimeric structure enhances tumor uptake and prolongs tumor retention compared to monomeric FAP inhibitors, while maintaining rapid renal clearance and low off-target accumulation. DOTAGA.Glu.(FAPi)2 can be radiolabeled with various isotopes, including gallium-68 (68Ga) for positron emission tomography (PET) imaging, and lutetium-177 (177Lu), actinium-225 (225Ac), or terbium-161 (161Tb) for targeted radionuclide therapy. Originally developed by researchers at the Johannes Gutenberg University Mainz, the candidate was in-licensed globally by Telix Pharmaceuticals in March 2025 under the development code TLX400. It is being evaluated in clinical trials for several solid tumors, including radioiodine-refractory thyroid cancer, sarcoma, glioblastoma, and bladder cancer.
- Other names
- 177Lu-DOTAGA-Glu-(FAPi)2177Lu-DOTAGA.Glu.(FAPi)2225Ac-DOTAGA.Glu.(FAPi)268Ga-DOTAGA.Glu.(FAPi)2DOTAGA-Glu-(FAPi)2DOTAGA-Glu(FAPi)2DOTAGA.Glu(FAPi)2DOTAGA.Glu.(FAPI)2DOTAGA.Glu.FAPi dimerLutetium-177-DOTAGA.Glu.(FAPi)2
02
Targets
FAP (Fibroblast activation protein alpha)
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