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CompletedNCT01634178Updated Apr 21, 2021Results posted

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

A Phase 1 interventional study of Apremilast in Healthy Volunteer, sponsored by Amgen. Completed at 1 site in United States. Open to participants aged 18 Years to 65 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2021-04-21.

Sponsored by Amgen · Phase 1, Interventional, and Treatment

From the registry’s dates

  • Registered 5 months after the study started (first participant enrolled Feb 2012, registered Jul 2012).
Phase
Phase 1
Study type
Interventional
Enrollment
46
Allocation
Randomized
Ages
18 Years to 65 Years
Sex
All
01

Study summary

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.

Read the detailed description

Participants will be randomized to receive a single dose of 30 mg apremilast during each of the 2 periods; once under fasting conditions and once after a high fat meal. Participants will be randomly assigned to receive apremilast either fasted first, then fed, or fed first then fasted. Participants will check into the study center on Day -1 of each period, will be dosed on Day 1, and discharged from the study center on Day 3 after all scheduled pharmacokinetic blood draws and safety evaluations. After a washout of 5 to 10 days, participants will return for period 2 during which they will receive apremilast according to their assigned sequence.

02

Conditions studied

  • Healthy Volunteer

Keywords

  • Apremilast,
  • pharmacokinetic
  • safety
  • Safety and pharmacokinetics in healthy volunteer subjects
03

In context

Lead sponsor

Amgen is the lead sponsor of 1,015 studies on the registry; 49 are open to participants now.

Of its 245 completed or terminated interventional studies of FDA-regulated products, 159 (65%) have results posted.

Counted across the registry records on this site, refreshed daily.

04

Who can participate

Ages eligible
18 Years to 65 Years
Sexes eligible
All
Accepts healthy volunteers
Yes

Inclusion criteria

  1. Healthy male or female subjects of any ethnic origin between ages of 18 and 65 inclusive with a body mass index (BMI) between 18 and 33.

  2. Females who are able to become pregnant have a negative pregnancy test at screening and baseline, and must agree to use one of the following:

    • a highly effective form of contraception (ex. Non-oral hormonal, intrauterine device) OR
    • oral hormonal contraceptive plus one additional form of barrier contraception OR
    • Two forms of barrier contraception These must be effective by the time of screening.
  3. All other females must have been surgically sterilized at least 6 months prior to screening or be postmenopausal (to be confirmed by lab tests).
  4. Males must agree to use latex or polyurethane condoms when engaging in sex during the study and for at least 28 days after dosing.

Exclusion criteria

Exclusion Criteria:

  1. Any condition, including the presence of laboratory abnormalities, or psychiatric illness, that would prevent the subject from signing the Informed Consent form, places the subject at unacceptable risk if he were to participate in the study, or confounds the ability to interpret data from the study.
  2. Presence of any surgical or medical conditions possibly affecting drug absorption, distribution, metabolism, and excretion, or plans to have elective or medical procedures during the conduct of the trial.
  3. Exposure to an investigational drug (new chemical entity) within 30 days prior to the first dose administration or 5 half-lives of that investigational drug, if known (whichever is longer).
  4. Subjects with known serum hepatitis, is a known carrier of hepatitis B surface antigen, hepatitis C antibody, or human immunodeficiency virus antibody.
  5. Subjects who have used prescription systemic or topical medications within 30 days of dosing, unless it is being used to treat a stable, chronic medical condition. This includes medication that is an inhibitor or inducer of P-glycoprotein transporter and CYP-3A4/5 used within 14 days of dosing.
05

Study design

Phase
Phase 1
Primary purpose
Treatment
Allocation
Randomized
Intervention model
Crossover assignment
Masking
None (open label)
Enrollment
46 participants (actual)

Study arms

  • Experimental
    Sequence 1: Apremilast Fasted / Fed

    In Period 1 participants will receive a single 30 mg apremilast tablet administered under fasted conditions and in Period 2 participants will receive a single 30 mg apremilast tablet administered after a high fat meal.

    Drug: Apremilast

  • Experimental
    Sequence 2: Apremilast Fed / Fasted

    In Period 1 participants will receive a single 30 mg apremilast tablet administered after a high fat meal and in Period 2 participants will receive a single 30 mg apremilast tablet administered under fasted conditions.

    Drug: Apremilast

Interventions

  • DrugApremilast

    Tablet for oral administration

    Also known as: CC-10004, Otezla®

06

What researchers measure

Primary outcomes

  1. Maximum Observed Plasma Concentration (Cmax) of Apremilast

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

    Time frame: 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.

  2. Time to Maximum Observed Plasma Concentration (Tmax) of Apremilast

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

    Time frame: 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.

  3. Area Under the Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration (AUC0-t) of Apremilast

    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.

    Time frame: 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.

  4. Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC0-∞) of Apremilast

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

    Time frame: 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.

  5. Estimate of Terminal Elimination Half-life of Apremilast in Plasma (t1/2)

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

    Time frame: 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.

  6. Apparent Total Plasma Clearance When Dosed Orally (CL/F) of Apremilast

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

    Time frame: 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.

  7. Apparent Total Volume of Distribution When Dosed Orally (Vz/F) of Apremilast

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

    Time frame: 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.

Secondary outcomes

  1. 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 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.

    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.

07

Results

Posted Apr 21, 2021

Participant flow

This study was conducted at one clinical research site in the United States.

Treatment Period 1
Participant flow — Treatment Period 1
MilestoneSequence 1: Apremilast Fasted / FedSequence 2: Apremilast Fed / Fasted
Started2323
Completed2322
Not completed01
Withdrew: Adverse event01
Treatment Period 2
Participant flow — Treatment Period 2
MilestoneSequence 1: Apremilast Fasted / FedSequence 2: Apremilast Fed / Fasted
Started2322
Completed2222
Not completed10
Withdrew: Adverse event10

Outcome measures

PrimaryMaximum Observed Plasma Concentration (Cmax) of Apremilast

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

Time frame:
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.
Reported as:
Geometric mean · ng/mL
Maximum Observed Plasma Concentration (Cmax) of Apremilast
ng/mLApremilast - FastedApremilast - Fed
Maximum Observed Plasma Concentration (Cmax) of Apremilast339.86 ± 26.5333.85 ± 30.0
Statistical analysis
  • Apremilast - Fasted vs Apremilast - Fed · Ratio of geometric least squares means: 98.3 · 90% CI 90.7 to 106.6Ratio of the geometric LS means (Fed/Fasted), reported as percentages.
SecondaryNumber 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 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.

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.
Reported as:
Count of participants · Participants
Number of Participants With Adverse Events
ParticipantsApremilast - FastedApremilast - Fed
Any adverse event95
Adverse events related to study drug43
Serious adverse events00
Discontinued due to adverse event02
Discontinued due to adverse event related to study drug01
PrimaryTime to Maximum Observed Plasma Concentration (Tmax) of Apremilast

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

Time frame:
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.
Reported as:
Median · hours
Time to Maximum Observed Plasma Concentration (Tmax) of Apremilast
hoursApremilast - FastedApremilast - Fed
Time to Maximum Observed Plasma Concentration (Tmax) of Apremilast2.50 (0.62 to 5.02)3.00 (1.00 to 8.00)
Statistical analysis
  • Apremilast - Fasted vs Apremilast - Fed · Wilcoxon signed-rank test · p = 0.0077 · Median difference: 0.75 · 90% CI 0.25 to 1.25Median difference (Fed - Fasted) calculated from the Hodges-Lehmann estimate.
PrimaryArea Under the Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration (AUC0-t) of Apremilast

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.

Time frame:
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.
Reported as:
Geometric mean · ng*hr/mL
Area Under the Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration (AUC0-t) of Apremilast
ng*hr/mLApremilast - FastedApremilast - Fed
Area Under the Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration (AUC0-t) of Apremilast3083.05 ± 34.03436.39 ± 33.0
Statistical analysis
  • Apremilast - Fasted vs Apremilast - Fed · Ratio of geometric ls means: 112.4 · 90% CI 109.3 to 115.6Ratio of the geometric LS means (Fed/Fasted), reported as percentages.
PrimaryArea Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC0-∞) of Apremilast

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

Time frame:
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.
Reported as:
Geometric mean · ng*hr/mL
Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC0-∞) of Apremilast
ng*hr/mLApremilast - FastedApremilast - Fed
Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC0-∞) of Apremilast3157.96 ± 34.63506.19 ± 33.9
Statistical analysis
  • Apremilast - Fasted vs Apremilast - Fed · Ratio of geometric least squares means: 112.0 · 90% CI 108.9 to 115.1Ratio of the geometric LS means (Fed/Fasted), reported as percentages.
PrimaryEstimate of Terminal Elimination Half-life of Apremilast in Plasma (t1/2)

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

Time frame:
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.
Reported as:
Geometric mean · hours
Estimate of Terminal Elimination Half-life of Apremilast in Plasma (t1/2)
hoursApremilast - FastedApremilast - Fed
Estimate of Terminal Elimination Half-life of Apremilast in Plasma (t1/2)8.88 ± 21.27.99 ± 18.9
PrimaryApparent Total Plasma Clearance When Dosed Orally (CL/F) of Apremilast

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

Time frame:
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.
Reported as:
Geometric mean · mL/hr
Apparent Total Plasma Clearance When Dosed Orally (CL/F) of Apremilast
mL/hrApremilast - FastedApremilast - Fed
Apparent Total Plasma Clearance When Dosed Orally (CL/F) of Apremilast9499.80 ± 34.68556.28 ± 33.9
PrimaryApparent Total Volume of Distribution When Dosed Orally (Vz/F) of Apremilast

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

Time frame:
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.
Reported as:
Geometric mean · mL
Apparent Total Volume of Distribution When Dosed Orally (Vz/F) of Apremilast
mLApremilast - FastedApremilast - Fed
Apparent Total Volume of Distribution When Dosed Orally (Vz/F) of Apremilast121735.96 ± 38.298582.15 ± 28.0

Adverse events

Collected over From first dose of study drug in Period 1 up to 5 to 10 days after dosing in Period 2, approximately 20 days.. Non-serious events are listed at a 5% frequency threshold.

Adverse event summary by group
GroupDeathsSeriousOther
Apremilast - Fasted—0/45 (0%)5/45 (11.1%)
Apremilast - Fed—0/46 (0%)3/46 (6.5%)
Total—0/46 (0%)7/46 (15.2%)
Most frequent other events
Most frequent other events
EventApremilast - FastedApremilast - FedTotal
NauseaGastrointestinal disorders3/452/465/46
HeadacheNervous system disorders3/451/463/46

Baseline characteristics

Age, Continuous
Age, Continuous(years)Apremilast
Mean38.5 ± 13.45
Sex: Female, Male
Sex: Female, Male(Participants)Apremilast
Female25
Male21
Ethnicity (NIH/OMB)
Ethnicity (NIH/OMB)(Participants)Apremilast
Hispanic or Latino17
Not Hispanic or Latino29
Unknown or Not Reported0
Race/Ethnicity, Customized
Race/Ethnicity, Customized(Participants)Apremilast
White31
Black or African American13
Asian1
American Indian or Alaska Native1
08

Study locations

1 site
  • PPD Development
    Austin, Texas 787844, United States
09

References and documents

Individual participant data

Plan to share: Yes — De-identified individual patient data for variables necessary to address the specific research question in an approved data sharing request

Supporting information: Study protocol, Sap, Icf, Csr

10

Updates

Tracking since Sep 25, 2026
No changes since tracking began. The registry record was last updated on Apr 21, 2021, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
11

Registry details

Key details

Study ID
NCT01634178
Lead sponsor
Amgen
Responsible party
Sponsor
First posted
Jul 6, 2012
Start date
Feb 1, 2012
Primary completion
Mar 1, 2012
Completion
Mar 1, 2012
Results posted
Apr 21, 2021
Last update
Apr 21, 2021

Study contacts

MD
study director · Amgen

Oversight

Data monitoring committee
No
View the source record on ClinicalTrials.gov ↗

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