WAY-VNA-932.: Treatment of central diabetes insipidus, Treatment of nocturnal enuresis, Treatment of nocturia, Vasopressin V2 agonist.

WAY-VNA-932 is a novel, orally active nonpeptide small molecule which exhibits vasopressin V-2 receptor agonism. In CHO cells transfected with human V-1a, V-2, V-1b and oxytocin receptors, WAY-VNA-932 is a potent agonist at the V-2 receptor with an EC50 for second messenger generation (CAMP) of 0.7 nM. In water loaded normotensive rats, Brattleboro rats, dogs and cynomolgus monkeys WAY-VNA-932 lowers urine output in a dose-dependent manner with a concomitant increase in osmolality. It is expected that WAY-VNA-932 will offer several advantages over desmopressin, a peptidic vasopressin V-2 agonist, including greater and more consistent bioavailability and the lack of pressor activity. WAY-VNA-932 is expected to be useful in conditions characterized by excessive production and/or dilution of urine such as central diabetes insipidus and nocturnal enuresis as well as in conditions characterized by inappropriate production of vasopressin. WAY-VNA-932 is the first nonpeptide vasopressin V-2 agonist to enter phase I trials.