A Randomized, Double-Blind, Placebo-Controlled, Crossover Study to Evaluate the Safety, Tolerability, Pharmacokinetic, and Pharmacodynamic Interactions Between Alcohol and Sunobinop in Healthy Participants.

BACKGROUND

Sunobinop is a potent, selective partial agonist at nociception/orphanin-FQ receptors with therapeutic potential in a variety of clinical disorders. This study assessed safety, tolerability, pharmacodynamics, and pharmacokinetic interactions of sunobinop and alcohol in healthy adults.

METHODS

This was a single-center, randomized, blinded, crossover study in 48 participants. Single doses of placebo, sunobinop 2 mg (therapeutic), and 6 mg (supratherapeutic), were administered in the morning with alcohol or placebo. Pharmacokinetic and pharmacodynamic profiles were compared.

RESULTS

Coadministration with alcohol did not alter the pharmacokinetics of alcohol or of sunobinop at either dose. A dose-effect relationship in the magnitude/duration of impairment in psychomotor/cognitive parameters was observed, with transient additive effects at 2 mg and greater-than-additive effects at 6 mg that resolved by 5 hours post administration. The most common treatment-emergent adverse event was somnolence, which was mild to moderate.

CONCLUSIONS

A single oral dose of sunobinop was safe and tolerated alone and in combination with alcohol. No pharmacokinetic interaction between sunobinop and alcohol was observed. An additive or greater-than-additive effect was observed for psychomotor/cognitive measures consistent with sunobinop's sleep-promoting effect, and would peak and resolve during a typical night's sleep.