relcovaptan

Relcovaptan is a potent, orally active non-peptide small molecule that acts as a selective antagonist of the vasopressin V1a receptor (also known as arginine vasopressin receptor 1A). It was developed for potential use in conditions such as Raynaud's disease, dysmenorrhoea, preterm labor (as a tocolytic), coronary spasm, heart failure, hypertension, and small cell lung cancer. Relcovaptan blocks the mitogenic signals triggered by vasopressin at the V1a receptor and has demonstrated dose-dependent inhibition of vasopressin-induced uterine activity in vitro and in vivo. Despite positive initial results and an excellent safety profile in early studies, clinical development was discontinued before approval for any indication[1][3][5][6].

Other names

relcovaptanum