90Y-FAPI-46

90Y-FAPI-46 is an investigational, targeted radioligand therapy (RLT) consisting of the fibroblast activation protein (FAP) inhibitor FAPI-46 chelated to the beta-emitting radioisotope yttrium-90 (90Y). FAPI-46 is a small-molecule quinoline derivative that binds with high affinity to fibroblast activation protein alpha (FAPα), a cell-surface serine protease highly expressed on cancer-associated fibroblasts (CAFs) in the tumor microenvironment of various solid tumors, as well as on certain tumor cells such as sarcomas. Upon binding, 90Y-FAPI-46 delivers localized, high-energy beta radiation to destroy FAP-expressing cells and surrounding tumor tissue. Originally developed at Heidelberg University and the German Cancer Research Center (DKFZ), the therapeutic rights to FAPI-46 were licensed to iTheranostics (an affiliate of SOFIE Biosciences) and subsequently acquired by Novartis. 90Y-FAPI-46 has been evaluated in investigator-initiated trials and compassionate-use programs, particularly at University Hospital Essen, for the treatment of advanced solid tumors, including sarcomas (such as solitary fibrous tumors) and pancreatic ductal adenocarcinoma.

Other names

90Y-labeled FAPI-46yttrium Y-90 FAPI-46yttrium-90 FAPI-46yttrium90 FAPI-46yttrium 90 FAPI-46