This open-label, Phase I trial (n=12) will investigate the effects of different methods of esketamine administration (28 mg nasal spray vs. 28 mg oral solution) with and without CYP3A4 inhibitors (grapefruit juice or cobicistat) on drug absorption and metabolism.
Conducted by Helsinki University Central Hospital, this study aims to determine how these factors influence esketamine concentration in the bloodstream.
The trial follows a four-phase, randomised, crossover design, where healthy adult participants (ages 18–45) will receive esketamine under different conditions. Blood samples will be collected over 24 hours to measure drug levels, with the primary outcome being the area under the plasma concentration-time curve (AUC). Secondary measures include peak concentration, time to peak, and drug half-life. The findings may help optimise esketamine dosing strategies for medical use.
Trial Details
Esketamine is a drug which is used for depression treatment, to relieve pain and, in larger doses, in anesthesia. Spravato nasal spray is the only esketamine product on the market used for the treatment of depression, but the high price limits the use of the drug. The aim of this study is to compare the concentration of esketamine after nasal (licensed product Spravato) and oral administration with and without a CYP3A4 inhibitor. Grapefruit juice and cobicistat are studied as CYP3A4 inhibitors in the study. In an open four-phase, randomized, alternating study with 12 healthy volunteers, the subjects will receive Spravato 28 mg nasal or esketamine 28 mg oral with either grapefruit juice, cobicistat or water in the study facilities. Blood samples will be collected and esketamine pharmacokinetics will be monitored up to 24 hours postdose. Primary endpoint is area under the plasma concentration-time curve of esketamine.Trial Number NCT06726382
Sponsors & Collaborators
University of HelsinkiThe Korpi Lab at the University of Helsinki is focused on understanding the neurochemical basis of behaviour and has done so using LSD.