Endocrine / Metabolic

Patient samples, cell culture, and mouse studies suggest P2RX7 inhibitors could help treat diabetic nephropathy. In glomeruli samples from diabetes patients, P2RX7 expression was higher in patients with nephropathy than in patients without renal impairment. In a mouse model of diabetes, P2RX7 knockdown decreased the number of macrophages and area of collagen IV accumulation in glomeruli compared with normal P2RX7 expression. In a rat model of diabetes, a P2RX7 inhibitor tool compound decreased numbers of macrophages in tubulointerstitial compartments compared with vehicle. Next steps include clinical testing of P2X7 inhibitors in diabetic nephropathy patients.

Evotec AG and Zhejiang Conba Pharmaceutical Co. Ltd. have EVT401, an oral small molecule P2RX7 antagonist, in Phase II testing for inflammation and Phase I testing for rheumatoid arthritis...