linsitinib

Linsitinib is an orally available, small-molecule dual inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) and the insulin receptor (IR). It works by binding to the cytoplasmic tyrosine kinase domain, inhibiting autophosphorylation and blocking downstream signaling pathways such as AKT and ERK. Originally developed for oncology indications, including adrenocortical carcinoma and small cell lung cancer, it is currently being repurposed by Sling Therapeutics for the treatment of thyroid eye disease (TED). In TED, IGF-1R is overexpressed and forms complexes with the thyroid-stimulating hormone receptor (TSHR), driving orbital inflammation and tissue remodeling. Linsitinib has demonstrated clinical significance in reducing proptosis in a Phase 2b/3 trial (LIDS) and is progressing toward a confirmatory Phase 3 registrational trial.

Other names

OSI-906OSI906OSI 906