Suvorexant efficacy in dogs corresponds to plasma exposures > 342 nM and OX2R occupancies > 65%. A. Suvorexant levels in satellite animals treated with suvorexant (1 or 3 mg/kg; p.o. in 20% Vitamin E TPGS) (n = 3, each time point). B. Calculated OX2R occupancy based on rat occupancy values, and normalized for free fraction of compound in rat (1.4%) and dog (1%). Gray shading indicates time points at which active wake was significantly attenuated in dogs treated with suvorexant (1 or 3 mg/kg), the plasma and occupancy range at which efficacy has been observed .
Gotter et al. BMC Neuroscience 2013 14:90 doi:10.1186/1471-2202-14-90