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Drug intelligence / Profile preview
177Lu-DOTAGA.(SA.FAPi)2
- Development stage
- Unknown
- Lead developer
- AIIMS New Delhi
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous
01
Overview
`177Lu-DOTAGA.(SA.FAPi)2` (also written as `[177Lu]Lu-DOTAGA.(SA.FAPi)2`) is an investigational, dimeric fibroblast activation protein (FAP) inhibitor radiopharmaceutical designed for targeted radioligand therapy. It consists of a dimeric FAP-targeting ligand built on a squaric acid (SA) linker and a DOTAGA chelator, which complexes the beta-emitting radionuclide lutetium-177 (177Lu). The dimeric design is engineered to enhance binding avidity and prolong tumor retention compared to monomeric FAP inhibitors. The therapeutic agent targets FAP, which is highly expressed on cancer-associated fibroblasts (CAFs) in the tumor stroma of various solid tumors, as well as on activated synovial fibroblasts in inflammatory joint diseases. It is being clinically evaluated for the treatment of FAP-expressing solid tumors, including radioiodine-refractory differentiated thyroid cancer, medullary thyroid cancer, low SSTR-expressing neuroendocrine tumors, metastatic breast cancer, and difficult-to-treat inflammatory arthritis (such as rheumatoid arthritis and psoriatic arthritis).
- Other names
- 177Lu-DOTAGA.(SA.FAPI)2177Lu-DOTAGA.FAPi dimer177Lu-DOTAGA(SA.FAPi)2[177Lu]Lu-DOTAGA.(SA.FAPI)2[177Lu]Lu-DOTAGA.FAPi dimer[177Lu]Lu-DOTAGA(SA.FAPi)2
02
Targets
FAP (Fibroblast activation protein alpha)
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