First-in-human study with ACT-539313, a novel selective orexin-1 receptor antagonist.

ABSTRACT:

Aims

The orexin system is involved in anxiety behaviour and corresponding physiological reactions and constitutes a target for treatment of anxiety disorders. ACT-539313 is a potent, selective orexin-1 receptor antagonist being developed for the treatment of anxiety disorders. This first-in-human study investigated its single-dose pharmacokinetics (PK) including food effect, pharmacodynamics (PD), safety and tolerability.

Methods

This double-blind, placebo-controlled, randomized study included 40 healthy male subjects. Ascending oral doses of 10-400 mg ACT-539313 were investigated in 5 dose groups of 8 subjects (of whom 2 received placebo per dose group). At 100 mg, subjects received ACT-539313 in fasted and fed conditions in a fixed sequential design. PK, PD (objective and

SUBMITTER: Kaufmann P 

PROVIDER: S-EPMC7319015 | biostudies-literature | 2020 Jul

REPOSITORIES: biostudies-literature