palosuran

Palosuran (ACT-058362) is an orally active, selective, small-molecule antagonist of the urotensin-2 receptor (UTS2R). Developed by Actelion Pharmaceuticals, palosuran was investigated as a first-in-class therapeutic for diabetic nephropathy and other cardiorenal diseases. While preclinical studies in diabetic rat models demonstrated improvements in renal blood flow, proteinuria, and insulin secretion, Phase II clinical trials in patients with type 2 diabetic nephropathy failed to show significant efficacy in reducing albuminuria or blood pressure. Additionally, palosuran has been shown to interact with somatostatin receptors, acting as an antagonist at SSTR2 and an agonist at SSTR5. Due to the lack of clinical efficacy, Actelion discontinued the development of palosuran.

Other names

1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-ureapalosuran sulfate