NCT01634178

Effect of Food on the Pharmacokinetics of Apremilast (CC-10004) in Healthy Adults

Completed Phase 1 Results posted Last updated 21 April 2021

What this trial tests

Phase 1 trial testing Apremilast in Healthy Volunteer in 46 participants. Completed in 1 March 2012.

Timeline

1 February 2012

Primary endpoint
1 March 2012

1 March 2012

Quick facts

Lead sponsor	Amgen
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	randomized
Design	crossover
Masking	none
Primary purpose	treatment
Enrollment	46
Start date	1 February 2012
Primary completion	1 March 2012
Estimated completion	1 March 2012
Sites	1 location across United States

Drugs / interventions tested

• Apremilast (APREMILAST) — full drug profile →

Conditions studied

• Healthy Volunteer — all drugs for Healthy Volunteer →

Sponsor

Amgen — full company profile →

Who can join

Adults 18 to 65, any sex, with Healthy Volunteer. Patients with the condition only — healthy volunteers not accepted.

Results — posted to ClinicalTrials.gov

Per-arm endpoint measurements with 95% confidence intervals where reported. Source: trial results section.

Maximum Observed Plasma Concentration (Cmax) of Apremilast Primary · Day 1 of each treatment period at pre-dose, and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.

Plasma concentrations of apremilast were determined by using a validated liquid chromatography-tandem mass spectrometry assay.

Group	Value	95% CI
Apremilast - Fasted	339.86	± 26.5
Apremilast - Fed	333.85	± 30.0

Number of Participants With Adverse Events Secondary · From first dose of study drug in Period 1 up to 5 to 10 days after dosing in Period 2, approximately 20 days.

An adverse event (AE) was any noxious, unintended, or untoward medical occurrence that appeared or worsened in a participant during the course of this 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 preexisting condition) was considered an AE.

Any adverse event

Group	Value	95% CI
Apremilast - Fasted	9
Apremilast - Fed	5

Adverse events related to study drug

Group	Value	95% CI
Apremilast - Fasted	4
Apremilast - Fed	3

Serious adverse events

Group	Value	95% CI
Apremilast - Fasted	0
Apremilast - Fed	0

Discontinued due to adverse event

Group	Value	95% CI
Apremilast - Fasted	0
Apremilast - Fed	2

Discontinued due to adverse event related to study drug

Group	Value	95% CI
Apremilast - Fasted	0
Apremilast - Fed	1

Time to Maximum Observed Plasma Concentration (Tmax) of Apremilast Primary · Day 1 of each treatment period at pre-dose, and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.

Plasma concentrations of apremilast were determined by using a validated liquid chromatography-tandem mass spectrometry assay.

Group	Value	95% CI
Apremilast - Fasted	2.50	0.62 – 5.02
Apremilast - Fed	3.00	1.00 – 8.00

Area Under the Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration (AUC0-t) of Apremilast Primary · Day 1 of each treatment period at pre-dose, and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.

Plasma concentrations of apremilast were determined by using a validated liquid chromatography-tandem mass spectrometry assay. AUC0-t was calculated using the linear trapezoidal method (linear up log down) when concentrations were increasing and the logarithmic trapezoidal method when concentrations were decreasing.

Group	Value	95% CI
Apremilast - Fasted	3083.05	± 34.0
Apremilast - Fed	3436.39	± 33.0

Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC0-∞) of Apremilast Primary · Day 1 of each treatment period at pre-dose, and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.

Plasma concentrations of apremilast were determined by using a validated liquid chromatography-tandem mass spectrometry assay.

Group	Value	95% CI
Apremilast - Fasted	3157.96	± 34.6
Apremilast - Fed	3506.19	± 33.9

Estimate of Terminal Elimination Half-life of Apremilast in Plasma (t1/2) Primary · Day 1 of each treatment period at pre-dose, and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.

Plasma concentrations of apremilast were determined by using a validated liquid chromatography-tandem mass spectrometry assay.

Group	Value	95% CI
Apremilast - Fasted	8.88	± 21.2
Apremilast - Fed	7.99	± 18.9

Apparent Total Plasma Clearance When Dosed Orally (CL/F) of Apremilast Primary · Day 1 of each treatment period at pre-dose, and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.

Plasma concentrations of apremilast were determined by using a validated liquid chromatography-tandem mass spectrometry assay.

Group	Value	95% CI
Apremilast - Fasted	9499.80	± 34.6
Apremilast - Fed	8556.28	± 33.9

Apparent Total Volume of Distribution When Dosed Orally (Vz/F) of Apremilast Primary · Day 1 of each treatment period at pre-dose, and at 0.5, 1, 1.5, 2, 2.5, 3, 5, 8, 12, 24, 36, and 48 hours after dosing.

Plasma concentrations of apremilast were determined by using a validated liquid chromatography-tandem mass spectrometry assay.

Group	Value	95% CI
Apremilast - Fasted	121735.96	± 38.2
Apremilast - Fed	98582.15	± 28.0

Adverse events — posted to ClinicalTrials.gov

Time frame: From first dose of study drug in Period 1 up to 5 to 10 days after dosing in Period 2, approximately 20 days.. Reporting threshold: 5%. Adverse-event reports describe events observed during the trial — not all are caused by the drug.

Apremilast - Fasted

Serious: 0/45 (0%)

Deaths: —

Apremilast - Fed

Serious: 0/46 (0%)

Deaths: —

Total

Serious: 0/46 (0%)

Deaths: —

Other adverse events (2 terms — click to expand)

Reaction	System	Apremilast - Fasted	Apremilast - Fed	Total
Nausea	Gastrointestinal disorders	—	—	—
Headache	Nervous system disorders	—	—	—

Data from ClinicalTrials.gov NCT01634178 adverse events section.

Sponsor's own description

The purpose of the study is to evaluate the effects of a high fat meal on the pharmacokinetics of a single dose of 30 mg apremilast in healthy adults.

Publications & conference data

No peer-reviewed publications indexed yet for this trial. Completed trials usually publish results within 12-18 months.