Edicotinib hydrochloride

Edicotinib hydrochloride is a potent, selective, brain penetrant and orally activecolony-stimulating factor-1 receptor (CSF-1R)inhibitor with an IC50 of 3.2 nM. Edicotinib hydrochloride exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively[1]. Edicotinib hydrochloride limits microglial expansion and attenuates microglial proliferation and neurodegenerationin mice. Edicotinib hydrochloride has the potential for Alzheimer’s disease and rheumatoid arthritis research[1][2].

[1] Mancuso R, et al. CSF1RinhibitorJNJ-40346527attenuatesmicroglialproliferationandneurodegenerationinP301Smice.Brain.2019 Oct 1;142(10):3243-3264. DOI:10.1093/brain/awz241
[2] Genovese MC, et al. Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy.J Rheumatol. 2015 Oct;42(10):1752-60. DOI:10.3899/jrheum.141580