retosiban

Retosiban is a small molecule oxytocin receptor antagonist developed by GlaxoSmithKline for the management of preterm labor. It is an orally and intravenously administered drug that selectively blocks the oxytocin receptor, with over 1400-fold selectivity compared to vasopressin receptors. Retosiban acts as an inverse agonist at the oxytocin receptor, reducing both spontaneous and stretch-induced uterine contractions in preclinical models and human myometrial tissue. Clinical studies have shown that retosiban can prolong pregnancy in women experiencing spontaneous preterm labor, with a favorable safety profile observed in phase I–III trials. Despite promising results, development for this indication has been discontinued after phase III trials[1][3][4][5][8].

Other names

retosiban820957-38-8