OX2R occupancy by suvorexant sufficient for sleep-promoting efficacy: restricted to 8 h following treatment. The time courses of plasma levels of suvorexant in humans collected in Phase 1 clinical trials following administration of suvorexant (indicated doses) are shown relative to the plasma values (0.33 μM) calculated to correspond to the exposure required for 65% OX2R occupancy (dashed line). The gray shaded area represents the predicted efficacy range based upon this value. occ, occupancy.
Gotter et al. BMC Neuroscience 2013 14:90 doi:10.1186/1471-2202-14-90