GENZ-882706

GENZ-882706 is a potent colony stimulating factor-1 receptor (CSF-1R) Inhibitor extracted from patent WO 2017015267A1. IC50 & Target: Target: CSF-1R^[1] In Vitro: Genz-882706 induces an increased level of proliferative activity on unstimulated cells 48 hours post treatment and the reason for this effect is unclear^[1]. In Vivo: Daily treatment with Genz-882706 significantly reduces experimental autoimmune encephalomyelitis. Treatment with Genz-882706 in experimental autoimmune encephalomyelitis (EAE) mice results in significant decreases in MCP-1, IL-6, IL-Ιβ and IP-10 levels in spinal cord homogenates when compared to Vehicle treated animals. Treatment with Genz-882706 shows a significant increase in TNF-a levels in the spinal cord when compared to the vehicle treated group. Genz-882706 at both the 30 mg/kg and the 100 mg/kg dose significantly reduces the number of microglia and monocytes/macrophages in the brain and spinal cord compared to the vehicle and LPS controls. Treatment with Genz-882706 modestly reduces CD80 expression on monocytes/macrophages in the brain^[1].