cligosiban

Cligosiban is an orally bioavailable, brain-penetrant, small-molecule oxytocin receptor antagonist developed primarily for the treatment of premature ejaculation (PE). It selectively blocks the human oxytocin receptor with nanomolar potency and shows high central penetration, aiming to modulate oxytocin-mediated ejaculatory control pathways in the brain and spinal cord.[7][13][16] In clinical pharmacology studies, cligosiban demonstrated a favorable safety and tolerability profile and pharmacokinetics consistent with once-daily or on-demand dosing 1–6 hours before intercourse.[7][8][10] A flexible-dose phase II trial (PEPIX) in men with severe lifelong PE showed that on-demand cligosiban (400–800 mg) significantly prolonged intravaginal ejaculatory latency time and improved patient-reported outcomes versus placebo, whereas a subsequent larger fixed-dose phase IIb study (PEDRIX) failed to demonstrate efficacy, leading to uncertainty about further development for PE.[2][4][5][7][10] Preclinical and ex vivo data also indicate that cligosiban reduces oxytocin-induced contractility in human prostate tissue, suggesting potential utility in benign prostatic hyperplasia by inhibiting oxytocin-driven smooth muscle contraction and promoting oxytocin receptor internalization.[1][18]

Other names

cligosiban