The purpose of the study is to evaluate the effects of age and sex on the pharmacokinetics and safety of a single oral dose of 30 mg apremilast in healthy adults.
This is an open-label, parallel group study where eligible elderly adults (aged 65-85 years inclusive) and younger adults (aged 18-55 years inclusive) and who are matched to the elderly participants by sex and body mass index (BMI) (± 10%) will receive a single dose of 30 mg apremilast under fasting conditions.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
OTHER
Masking
NONE
Enrollment
36
One oral 30 mg dose of apremilast
PRA International
Lenexa, Kansas, United States
Clinical Development Services
Dallas, Texas, United States
Area Under the Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration (AUC0-t) of Apremilast
The lower limit of quantitation for apremilast plasma concentrations was 1.0 ng/mL. AUC0-t was calculated using the linear trapezoidal method when concentrations were increasing and the logarithmic trapezoidal method when concentrations were decreasing.
Time frame: Day 1 predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.
AUC From Time Zero to Time of Last Quantifiable Concentration (AUC0-t) of Apremilast by Sex
The lower limit of quantitation for apremilast plasma concentrations was 1.0 ng/mL. AUC0-t was calculated using the linear trapezoidal method when concentrations were increasing and the logarithmic trapezoidal method when concentrations were decreasing.
Time frame: Day 1 predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.
Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC0-∞) of Apremilast
The lower limit of quantitation for apremilast plasma concentrations was 1.0 ng/mL.
Time frame: Day 1 predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.
AUC From Time Zero Extrapolated to Infinity (AUC0-∞) of Apremilast by Sex
The lower limit of quantitation for apremilast plasma concentrations was 1.0 ng/mL.
Time frame: Day 1 predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.
Maximum Observed Plasma Concentration (Cmax) of Apremilast
The lower limit of quantitation for apremilast plasma concentrations was 1.0 ng/mL.
Time frame: Day 1 predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.
Maximum Observed Plasma Concentration of Apremilast by Sex
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The lower limit of quantitation for apremilast plasma concentrations was 1.0 ng/mL.
Time frame: Day 1 predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.
Time to Maximum Observed Plasma Concentration (Tmax) of Apremilast
The lower limit of quantitation for apremilast plasma concentrations was 1.0 ng/mL.
Time frame: Day 1 predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.
Time to Maximum Observed Plasma Concentration (Tmax) of Apremilast by Sex
The lower limit of quantitation for apremilast plasma concentrations was 1.0 ng/mL.
Time frame: Day 1 predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.
Estimate of Terminal Elimination Half-life of Apremilast in Plasma (t1/2)
Time frame: Day 1 predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.
Estimate of Terminal Elimination Half-life of Apremilast in Plasma by Sex
Time frame: Day 1 predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.
Apparent Total Plasma Clearance When Dosed Orally (CL/F) of Apremilast
Time frame: Day 1 predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.
Apparent Total Plasma Clearance When Dosed Orally of Apremilast by Sex
Time frame: Day 1 predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.
Apparent Total Volume of Distribution When Dosed Orally (Vz/F) of Apremilast
Time frame: Day 1 predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.
Apparent Total Volume of Distribution When Dosed Orally (Vz/F) of Apremilast by Sex
Time frame: Day 1 predose and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.
Number of Participants With Adverse Events
An adverse event (AE) was any noxious, unintended, or untoward medical occurrence that appeared or worsened in a participant during the course of the study. It could have been a new intercurrent illness, a worsening concomitant illness, an injury, or any concomitant impairment of the participant's health including laboratory test values, regardless of etiology. Any worsening (i.e., any clinically significant adverse change in the frequency or intensity of a pre-existing condition) was considered an AE.
Time frame: From first dose of study drug up to 11 days