CTP-499

CTP-499 is an orally bioavailable, deuterated small molecule drug candidate developed by Concert Pharmaceuticals for the treatment of chronic kidney disease (CKD), with a primary focus on diabetic nephropathy. It was developed using the proprietary DCE Platform (deuterated chemical entity platform) by incorporating deuterium into 1-((S)-5-hydroxyhexyl)-3,7-dimethylxanthine (HDX), which is an active metabolite of the non-selective phosphodiesterase inhibitor pentoxifylline. This deuteration is intended to enhance the metabolic stability and pharmacokinetic profile of the drug, leading to more consistent plasma levels of both the parent compound and its active metabolites. CTP-499 acts as a multisubtype selective inhibitor of phosphodiesterases (PDEs), exerting anti-inflammatory, anti-oxidant, and anti-fibrotic effects. It was designed to be administered as an adjunct to standard-of-care therapies, such as ACE inhibitors or ARBs, to slow the progression of renal damage.

Other names

deuterated HDXdeuterated 1-((S)-5-hydroxyhexyl)-3,7-dimethylxanthine