Drug intelligence / Profile preview

131I-FAPi-5

Development stage
Preclinical
Lead developer
University of Copenhagen
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Peptides
Administration
Intravenous
01

Overview

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
02

Targets

FAP (Fibroblast activation protein alpha)

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