131I-FAPi-5

131I-FAPi-5 is a dimeric radiopharmaceutical designed for targeted radionuclide therapy (TRT) of tumors expressing fibroblast activation protein (FAP). It consists of two FAP-targeting inhibitor (FAPi) subunits linked and labeled with the beta-emitting radioisotope Iodine-131 (131I) via a tetrazine-trans-cyclooctene (T4CO) ligation method. This dimeric structure is engineered to enhance tumor retention and increase the radiation dose delivered to the tumor microenvironment compared to monomeric counterparts. Preclinical evaluation in human glioblastoma (U87-MG) xenograft models has shown that 131I-FAPi-5 achieves high and sustained tumor uptake with primary renal excretion, leading to significant tumor regression and improved survival rates. It is being investigated as a scalable and cost-effective alternative to radiometal-based FAP therapies.

Other names

131I-labeled FAPi dimerIodine-131 labeled FAP inhibitor dimerIodine131 labeled FAP inhibitor dimerIodine 131 labeled FAP inhibitor dimer