161Tb-CTR-FAPI

161Tb-CTR-FAPI (also known as 161Tb-BRP-010) is an investigational, covalent targeted radioligand therapy (RLT) developed by Peking University and Boomray Pharmaceuticals. It consists of a fibroblast activation protein (FAP) inhibitor (FAPI) conjugated to the therapeutic radionuclide terbium-161 (161Tb). Unlike conventional reversible FAP-targeted agents, CTR-FAPI utilizes sulfur(VI)-fluoride exchange (SuFEx) chemistry to form an irreversible covalent bond with FAP, which is highly expressed on cancer-associated fibroblasts (CAFs) in the tumor microenvironment. This covalent binding significantly enhances tumor uptake and prolongs retention. Terbium-161 is a medical radionuclide that emits both beta-minus particles and low-energy Auger/conversion electrons, offering a highly localized radiation dose with superior therapeutic efficacy compared to lutetium-177 (177Lu). Preclinical studies have demonstrated that 161Tb-CTR-FAPI exhibits robust antitumor activity and a favorable safety profile, making it a promising candidate for the treatment of FAP-positive solid tumors.

Other names

161Tb-cr-FAPIterbium-161 CTR-FAPIterbium161 CTR-FAPIterbium 161 CTR-FAPIterbium-161 covalent targeted FAPIterbium161 covalent targeted FAPIterbium 161 covalent targeted FAPI