mk-3697

Description: MK-3697 is a novel and potent isonicotinamide small molecule that acts as an orally bioavailable, selective Orexin 2 receptor antagonist with Ki of 0.95 nM. Orexin receptor antagonists have demonstrated clinical utility for the treatment of insomnia. The majority of clinical efforts to date have focused on the development of dual orexin receptor antagonists (DORAs), small molecules that antagonize both the orexin 1 and orexin 2 receptors. MK-3697 is also the third insomnia drug that is currently being developed by Merck. MK-3697 has Ki = 0.95 nM. Orexin receptor antagonists have demonstrated clinical utility for the treatment of insomnia. In vivo tests results on MK-3697 demonstrated improved stability and TDI profiles as well as excellent sleep efficacy across species.

References: Bioorg Med Chem Lett. 2014 Oct 15; 24(20):4884-90.