The purpose of this study is to compare the rate and extent of absorption (relative bioavailability) of seltorexant Phase 3 test formulation(s) relative to a reference Phase 2b tablet formulation dosed in the evening under fasted and semi-fasted conditions (3 hours after meal); to assess the effect of type and timing of the meal on the rate and extent of absorption of seltorexant Phase 3 tablet formulation (low dose and high dose strength) in healthy male and female participants; and to assess the pharmacokinetic of single-dose administration of low dose and high dose of seltorexant in healthy male and female participants 3 hours after meal.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
OTHER
Masking
NONE
Enrollment
151
In Part 1, Part 2, and Part 3 (3A and 3C), Seltorexant high dose (either a high dose tablet or two low dose tablets) will be administered orally.
In Part 3 (3B and 3C), Seltorexant low dose will be administered orally.
PRAHS
Salt Lake City, Utah, United States
Maximum Observed Plasma Concentration (Cmax)
Cmax is the maximum observed plasma concentration.
Time frame: Predose up to 48 hours postdose
Area Under the Plasma Concentration-Time Curve from the Time of Dosing to the Last Measurable Plasma Concentration (AUC[0-last])
AUC(0-last) is the area under the plasma concentration-time curve from the time of dosing to the last measurable plasma concentration.
Time frame: Predose up to 48 hours postdose
Area Under the Plasma Concentration-Time Curve Extrapolated to Infinite Time (AUC[0-infinity])
AUC (0-infinity) is the area under the plasma concentration-time curve from time zero to infinite time, calculated using the observed value of the last non-zero plasma concentration.
Time frame: Predose, up to 48 hours postdose
Number of Participants with Adverse Events as a Measure of Safety and Tolerability
An adverse event is any untoward medical event that occurs in a participant administered an investigational product, and it does not necessarily indicate only events with clear causal relationship with the relevant investigational product.
Time frame: Part 1: approximately 16 weeks; Part 2: approximately 10 weeks; Part 3: approximately 39 weeks
Dose-Proportionality of Seltorexant Based on Cmax
Dose proportionality of single doses of low dose and high dose of seltorexant from the Cmax will be assessed.
Time frame: Predose up to 48 hours postdose
Dose-Proportionality of Seltorexant Based on AUC(0-last)
Dose proportionality of single doses of low dose and high dose of seltorexant from the AUC(0-last) will be assessed.
Time frame: Predose up to 48 hours postdose
Dose-Proportionality of Seltorexant Based on AUC(0-infinity)
Dose proportionality of single doses of low dose and high dose of seltorexant from the AUC(0-infinity) will be assessed.
Time frame: Predose up to 48 hours postdose
Plasma Protein Binding (PPB) of Seltorexant and Its Metabolites (M12 and M16)
Plasma protein binding (PPB) of seltorexant and its metabolites (M12 and M16) will be determined by using a qualified liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS) method.
Time frame: Predose up to 12 hours postdose
Change from Baseline in Karolinska Sleepiness Scale (KSS) Score
The KSS is a self reported, assessment of level of drowsiness at the time of scale administration. This scale is focused mainly on the propensity to fall asleep and has a high validity in measuring sleepiness. It consists of a 9-point Likert scale with response options from: 1=extremely alert, 2=very alert, 3=alert, 4=rather alert, 5=neither alert nor sleepy, 6= some signs of sleepiness, 7=sleepy (but no effort to keep awake), 8= sleepy, some effort to keep awake , 9=very sleepy (fighting sleep).
Time frame: Baseline, Day 1, and Day 2
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