Ophthalmic disease

Cell culture and mouse studies suggest inhibiting ADORA2A could help treat proliferative retinopathy. In a mouse model of the disease, retinal levels of ADORA2A were higher than in normal mice. In human microvascular retinal endothelial cells cultured under hypoxic conditions, siRNA targeting ADORA2A or an ADORA2A antagonist tool compound decreased proliferation compared with non-targeting siRNA or vehicle, respectively. Also in the mouse model, endothelial cell-specific knockout of ADORA2A decreased pathological neovascularization, disease-induced infiltration of non-ganglion cells and neovascular nuclei from the inner limiting membrane into the vitreous, and the numbers of proliferating vascular endothelial cells compared with mice with normal ADORA2A expression. Next steps include testing ADORA2A inhibition in additional models of proliferative retinopathy.

Kyowa Hakko Kirin Co. Ltd. markets the ADORA2A antagonist Nouriast istradefylline to treat Parkinson's disease...