enrupatinib

EI-1071 (enrupatinib) is an orally administered, brain-penetrant small molecule inhibitor of the colony stimulating factor-1 receptor (CSF-1R), a tyrosine kinase. It selectively inhibits CSF-1R activity and is being developed primarily for neurodegenerative diseases such as Alzheimer's disease and for idiopathic pulmonary fibrosis. In preclinical models, EI-1071 reduces activated microglia around amyloid plaques, decreases neuroinflammation and neuronal injury, preserves homeostatic microglia, and improves cognitive function. The drug has also shown efficacy in reducing tumor-associated macrophages in cancer models and decreasing lung fibrosis in pulmonary fibrosis models. Phase 1 clinical trials demonstrated that EI-1071 is well-tolerated with only mild adverse events unrelated to dosing. It has received Orphan Drug Designation from the FDA for idiopathic pulmonary fibrosis and is currently being evaluated in phase 2 trials for Alzheimer's disease[1][3][4][5][7].

Other names

enrupatinib