[90Y]Y-FAPI-46

[90Y]Y-FAPI-46 is a targeted radiopharmaceutical therapy (radioligand therapy) consisting of the fibroblast activation protein (FAP) inhibitor FAPI-46 labeled with 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), which is highly expressed on cancer-associated fibroblasts (CAFs) in the tumor microenvironment of various solid tumors, particularly sarcomas and pancreatic ductal adenocarcinoma. Upon binding, the Yttrium-90 isotope delivers localized beta radiation, causing DNA damage and cell death in both FAP-expressing stromal cells and adjacent tumor cells. Originally developed at Heidelberg University, the therapeutic rights to FAPI-46 were licensed to Novartis (via iTheranostics, an affiliate of SOFIE Biosciences). Clinical evaluation of [90Y]Y-FAPI-46 has been primarily conducted through investigator-initiated trials at the University Hospital Essen, demonstrating promising efficacy and safety in patients with advanced-stage solid tumors, particularly sarcomas such as solitary fibrous tumors.

Other names

90Y-FAPI-4690Y-FAPI-46-RLT90Y-FAPI4690Y-labeled FAPI-4690Y-labeled fibroblast activation protein inhibitor 4690Y-labeled fibroblast activation protein inhibitor-46[90Y]Y-FAPI-46