The primary objective of this study is to assess the pharmacokinetics (PK) of lemborexant and metabolites (M4, M9, and M10) in plasma in healthy Chinese participants following single and multiple oral doses of lemborexant.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
OTHER
Masking
NONE
Enrollment
26
Lemborexant oral tablets.
Xuhui Central Hospital
Shanghai, China
Cmax: Maximum Observed Plasma Concentration for Lemborexant and Its Metabolites (M4, M9, and M10) Following Single Dose in All Cohorts
Time frame: All Cohorts, Day 1: 0-240 hours post single dose
Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Lemborexant and Its Metabolites (M4, M9, and M10) Following Single Dose in All Cohorts
Time frame: All Cohorts, Day 1: 0-240 hours post single dose
AUC(0-8h): Area Under the Concentration-time Curve From Zero Time to 8 Hours Postdose for Lemborexant and Its Metabolites (M4, M9, and M10) Following Single Dose in All Cohorts
Time frame: All Cohorts, Day 1: 0-8 hours post single dose
AUC(0-24h): Area Under the Concentration-time Curve From Zero Time to 24 Hours Postdose for Lemborexant and Its Metabolites (M4, M9, and M10) Following Single Dose in All Cohorts
Time frame: All Cohorts, Day 1: 0-24 hours post single dose
AUC(0-t): Area Under the Concentration-time Curve From Zero Time to Time of Last Quantifiable Concentration for Lemborexant and Its Metabolites (M4, M9, and M10) Following Single Dose in All Cohorts
Time frame: All Cohorts, Day 1: 0-240 hours post single dose
AUC(0-inf): Area Under the Concentration-time Curve From Zero Time Extrapolated to Infinite Time for Lemborexant and Its Metabolites (M4, M9, and M10) Following Single Dose in All Cohorts
Time frame: All Cohorts, Day 1: 0-240 hours post single dose
λz: Terminal Phase Rate Constant for Lemborexant and Its Metabolites (M4, M9, and M10) Following Single Dose in All Cohorts
Time frame: All Cohorts, Day 1: 0-240 hours post single dose
t½: Terminal Elimination Phase Half-life for Lemborexant and Its Metabolites (M4, M9, and M10) Following Single Dose in All Cohorts
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Time frame: All Cohorts, Day 1: 0-240 hours post single dose
MRT: Mean Residence Time for Lemborexant and Its Metabolites (M4, M9, and M10) Following Single Dose in All Cohorts
Time frame: All Cohorts, Day 1: 0-240 hours post single dose
Vz/F: Apparent Volume of Distribution at Terminal Phase for Lemborexant Following Single Dose in All Cohorts
Time frame: All Cohorts, Day 1: 0-240 hours post single dose
CL/F: Apparent Total Clearance Following Extravascular Administration for Lemborexant Following Single Dose in All Cohorts
Time frame: All Cohorts, Day 1: 0-240 hours post single dose
Metabolite to Lemborexant Area Under the Concentration-time Curve From Zero Time Extrapolated to Infinite Time Ratio Following Molecular Weight Correction to Lemborexant Equivalents After Single Dose in All Cohorts
Time frame: All Cohorts, Day 1: 0-240 hours post single dose
Cmax: Maximum Observed Plasma Concentration for Lemborexant and Its Metabolites (M4, M9, and M10) Following Single Dose (Day 15 dosing) in Cohort 2
Time frame: Cohort 2, Day 15: 0-24 hours post single dose
Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Lemborexant and Its Metabolites (M4, M9, and M10) Following Single Dose (Day 15 dosing) in Cohort 2
Time frame: Cohort 2, Day 15: 0-24 hours post single dose
AUC(0-8h): Area Under the Concentration-time Curve From Zero Time to 8 Hours Postdose for Lemborexant and Its Metabolites (M4, M9, and M10) Following Single Dose (Day 15 dosing) in Cohort 2
Time frame: Cohort 2, Day 15: 0-8 hours post single dose
AUC(0-24h): Area Under the Concentration-time Curve From Zero Time to 24 Hours Postdose for Lemborexant and Its Metabolites (M4, M9, and M10) Following Single Dose (Day 15 dosing) in Cohort 2
Time frame: Cohort 2, Day 15: 0-24 hours post single dose
AUC(0-8h): Area Under the Concentration-time Curve From Zero Time to 8 Hours Postdose for Lemborexant and Its Metabolites (M4, M9, and M10) Following Multiple Doses (Day 28 dosing) in Cohort 2
Time frame: Cohort 2, Day 28: 0-8 hours post multiple dose
AUC(0-τ): Area Under the Concentration-time Curve Over the Dosing Interval for Lemborexant and Its Metabolites (M4, M9, and M10) Following Multiple Doses in Cohort 2
Time frame: Cohort 2, Day 28: 0-324 hours post multiple dose
Css,avg: Average Steady State Concentration for Lemborexant and Its Metabolites (M4, M9, and M10) Following Multiple Doses in Cohort 2
Time frame: Cohort 2, Day 28: 0-324 hours post multiple dose
Css,max: Maximum Observed Concentration at Steady State for Lemborexant and Its Metabolites (M4, M9, and M10) Following Multiple Doses in Cohort 2
Time frame: Cohort 2, Day 28: 0-324 hours post multiple dose
Css,min: Minimum Observed Concentration at Steady State for Lemborexant and Its Metabolites (M4, M9, and M10) Following Multiple Doses in Cohort 2
Time frame: Cohort 2, Day 28: 0-324 hours post multiple dose
PTF: Peak-trough Fluctuation for Lemborexant and Its Metabolites (M4, M9, and M10) Following Multiple Doses in Cohort 2
Time frame: Cohort 2, Day 28: 0-324 hours post multiple dose
Tss,max: Time to Reach the Maximum Plasma Concentration (Cmax) for Lemborexant and Its Metabolites (M4, M9, and M10) Following Multiple Doses at Steady State in Cohort 2
Time frame: Cohort 2, Day 28: 0-324 hours post multiple dose
λz: Terminal Phase Rate Constant for Lemborexant and Its Metabolites (M4, M9, and M10) Following Multiple Doses in Cohort 2
Time frame: Cohort 2, Day 28: 0-324 hours post multiple dose
t½: Terminal Elimination Phase Half-life for Lemborexant and Its Metabolites (M4, M9, and M10) Following Multiple Doses in Cohort 2
Time frame: Cohort 2, Day 28: 0-324 hours post multiple dose
MRT: Mean Residence Time for Lemborexant and Its Metabolites (M4, M9, and M10) Following Multiple Doses in Cohort 2
Time frame: Cohort 2, Day 28: 0-324 hours post multiple dose
Vz/F: Apparent Volume of Distribution at Terminal Phase for Lemborexant Following Multiple Doses in Cohort 2
Time frame: Cohort 2, Day 28: 0-324 hours post multiple dose
CLss/F: Apparent Total Clearance Following Extravascular Administration at Steady-state for Lemborexant Following Multiple Doses in Cohort 2
Time frame: Cohort 2, Day 28: 0-324 hours post multiple dose
Rac: Accumulation Ratio for Lemborexant and Its Metabolites (M4, M9, and M10) Following Multiple Doses in Cohort 2
Time frame: Cohort 2, Day 28: 0-324 hours post multiple dose
Metabolite to Lemborexant Area Under the Concentration-time Curve Over the Dosing Interval Ratio Following Molecular Weight Correction to Lemborexant Equivalents After Multiple Doses in Cohort 2
Time frame: Cohort 2, Day 28: 0-324 hours post multiple dose