filorexant

Filorexant is a small molecule, orally bioavailable dual orexin receptor antagonist that was developed by Merck for the treatment of insomnia and investigated for other indications such as major depressive disorder, diabetic neuropathy, and migraine. It acts as a reversible antagonist at both orexin receptor type 1 (OX1R) and type 2 (OX2R), with high potency at both targets. Filorexant was shown to improve sleep onset and maintenance by inhibiting the activity of wake-promoting orexin neuropeptides in the brain. Despite demonstrating efficacy in phase II trials for insomnia, it did not show significant benefit in clinical trials for depression, migraine prevention, or painful diabetic neuropathy. Development was discontinued after phase II due to lack of differentiation from other drugs in its class or insufficient efficacy in non-insomnia indications[1][3][5][7].

Other names

filorexant [USAN]filorexant [INN]filorexantumUNII-E6BTT8VA5ZUNII-E-6BTT8VA5ZUNII-E 6BTT8VA5ZE6BTT8VA5ZE-6BTT8VA5ZE 6BTT8VA5Z