epelsiban

Epelsiban is an orally bioavailable, highly selective, and potent non-peptide oxytocin receptor antagonist developed by GlaxoSmithKline. It exhibits sub-nanomolar affinity for the human oxytocin receptor (Ki = 0.13 nM) and demonstrates over 50,000-fold selectivity against vasopressin receptors (V1a, V1b, V2). Epelsiban was investigated for the treatment of premature ejaculation in men and infertility due to adenomyosis in women. Its mechanism of action involves antagonism of the oxytocin receptor (OXTR), thereby inhibiting physiological processes such as uterine contractions and ejaculation that are mediated by oxytocin signaling[1][2][3][5]. Despite promising pharmacological properties—including good oral bioavailability and favorable pharmacokinetics—clinical development was discontinued after phase II trials failed to demonstrate sufficient efficacy[3][6].

Other names

epelsiban besilate