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177Lu-DOTA-2P(FAPI)2
- Development stage
- Unknown
- Lead developer
- National University of Singapore
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous
01
Overview
177Lu-DOTA-2P(FAPI)2 is a novel dimeric fibroblast activation protein (FAP)-targeting radiopharmaceutical. It consists of a homodimeric FAP inhibitor (FAPI) ligand based on the FAPI-46 scaffold, linked via PEG spacers, chelated with DOTA, and radiolabeled with the therapeutic beta-emitting radionuclide lutetium-177 (177Lu). By leveraging the polyvalency effect, the dimeric structure of 177Lu-DOTA-2P(FAPI)2 provides significantly enhanced tumor uptake and prolonged tumor retention compared to monomeric FAPIs (such as FAPI-46), making it a highly promising candidate for FAP-targeted radioligand therapy (RLT). Preclinical and early clinical studies have demonstrated its safety and efficacy in treating FAP-positive solid tumors, particularly when combined with immune checkpoint inhibitors (such as anti-PD-L1 antibodies) to reprogram the tumor microenvironment and enhance antitumor immunity.
- Other names
- 177Lu-DOTA-2P(FAPi)2177Lu-FAPI dimer177Lu-FAPI-dimer[177Lu]DOTA-2P(FAPI)2[177Lu]Lu-DOTA-2P(FAPI)2
02
Targets
FAP (Fibroblast activation protein alpha)
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