Drug intelligence / Profile preview

131I-FAP-2286

Development stage
Unknown
Lead developer
Clovis Oncology
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

131I-FAP-2286 is a radiopharmaceutical consisting of the radionuclide iodine-131 conjugated to FAP-2286, a peptide ligand that specifically targets fibroblast activation protein (FAP), which is overexpressed in cancer-associated fibroblasts (CAFs) in the tumor microenvironment. Upon intravenous administration, the drug selectively accumulates in FAP-positive stromal cells within tumors, delivering targeted beta-emitting radiation for therapeutic effect. In preclinical models, 131I-FAP-2286 showed effective tumor uptake and retention, suppression of tumor growth, and induction of autophagy in pancreatic cancer cells. Its antitumor efficacy is further enhanced with concurrent autophagy inhibition. This compound exemplifies the targeted radionuclide therapy (TRT) class.[1][3]

Other names
131I-labeled FAP-2286131I-FAP-2286-Tyr
02

Targets

FAP (Fibroblast activation protein alpha)

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