APX-115

APX-115 is an inhibitor of NADPH oxidase 1 (NOX1), NOX2, and NOX4 (K_is = 1.08, 0.57, and 0.63 µM, respectively, for the human enzymes).¹ It is selective for these enzymes over xanthine oxidase and glucose oxidase (K_is = >100 µM for both). APX-115 (10 or 20 µM) prevents RANKL-induced increases in reactive oxygen species (ROS) levels in primary mouse bone marrow-derived macrophages (BMDMs). It inhibits GM-CSF- and RANKL-induced primary mouse osteoclast differentiation when used at concentrations of 1.1, 3.3, or 10 µM. APX-115 (10 mg/kg per day) increases femur bone mass density and strength and reduces femur and tibia resorption areas in ovariectomized (OVX) mice. It reduces plasma and urinary levels of 8-isoprostane, a marker for lipid oxidation, plasma levels of insulin, triglycerides, HDL, LDL, and creatinine, urinary levels of albumin, as well as renal fibrosis, in a db/db mouse model of diabetic nephropathy when administered at a dose of 60 mg/kg per day.²

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1. Joo, J.H., Huh, J.E., Lee, J.H., et al. A novel pyrazole derivative protects from ovariectomy-induced osteoporosis through the inhibition of NADPH oxidase. Sci. Rep. 15(6), 22389 (2016).

2. Cha, J.J., Min, H.S., Kim, K.T., et al. APX-115, a first-in-class pan-NADPH oxidase (Nox) inhibitor, protects db/db mice from renal injury. Lab Invest. 97(4), 419-431 (2017).