Edicotinib

Edicotinib is an inhibitor of colony stimulating factor 1 receptor (CSF1R; IC₅₀ = 3.2 nM).¹ It is selective for CSF1R over KIT and FMS-related tyrosine kinase 3 (FLT3; IC₅₀s = 20 and 190 nM, respectively). Edicotinib (0.1-1,000 nM) reduces CSF1-induced phosphorylation of CSF1R and ERK1/2 in N13 microglia. It reduces spinal motor neuron degeneration and increases the latency to fall in the rotarod test in the P301S mouse model of tauopathy. Edicotinib (15 mg/kg) reduces increases in the colonic weight-to-length ratio, as well as decreases colonic infiltration of macrophages, neutrophils, and CD3⁺ T cells, in an adoptive T cell transfer-induced mouse model of colitis.² It also reduces the viability of L-1236 Hodgkin lymphoma cells with an IC₅₀ value of 264 nM.³

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1. Mancuso, R., Fryatt, G., Cleal, M., et al. CSF1R inhibitor JNJ-40346527 attenuates microglial proliferation and neurodegeneration in P301S mice. Brain 142(10), 3243-3264 (2019).

2. Manthey, C.L., Moore, B.A., Chen, Y., et al. The CSF-1-receptor inhibitor, JNJ-40346527 (PRV-6527), reduced inflammatory macrophage recruitment to the intestinal mucosa and suppressed murine T cell mediated colitis. PLoS One 14(11), e0223918 (2019).

3. Campion, L., Deangelis, N., Ferrante, C., et al. Abstract B269: Effects of blocking aberrantly expressed CSF-1R in Hodgkin lymphoma. Mol. Cancer Ther. 12(11_Supplement), B269 (2014).