In vitro activity: Edicotinib, formerly known as JNJ-40346527, is a novel selective and orally bioavailable inhibitor of colony-stimulating factor-1 (CSF-1) receptor kinase. It is undergoing clinical investigation and acts to inhibit macrophage survival, proliferation, and differentiation in patients with active rheumatoid arthritis (RA) despite disease-modifying antirheumatic drug (DMARD) therapy. Pharmacokinetic exposure to JNJ-40346527 and its active metabolites was above the projected concentration needed for pharmacologic activity, and effective target engagement and proof of activity were demonstrated by increased levels of CSF-1 and decreased CD16+ monocytes in JNJ-40346527-treated, but not placebo-treated, patients. Thirty-seven (58.7%) JNJ-40346527-treated and 16 (50.0%) placebo-treated patients reported ≥ 1 adverse event (AE); 1 (1.6%) JNJ-40346527-treated and 3 (9.4%) placebo-treated patients reported ≥ 1 serious AE.

Kinase Assay: Edicotinib, formerly known as JNJ-40346527, is a novel selective and orally bioavailable inhibitor of colony-stimulating factor-1 (CSF-1) receptor kinase.