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ACT-462206 is a dual orexin receptor antagonist which has been investigated for the treatment of insomnia. In human trials, ACT-462206 produced dose-dependent sedative effects and was generally well tolerated, with residual sleepiness and headache being the most common adverse events.
In humans, the sedative effects of ACT-462206 began 45 minutes after oral administration, and dissispated within 8 hours - consistent with a favorable pharmacodynamic profile for the treatment of insomnia. However, the pharmacokinetic profile of ACT-462206 diverges significantly from what would be expected based on behavioral effects. Elevated plasma concentrations of ACT-462206 are sustained for over 24–36 hours after administration - despite behvioral measures of sedation disappearing within 8 hours of administration.