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AzTrials

Healthy VolunteersPhase 1NCT02236988

Study to Evaluate Pharmacokinetics of Prototype Modified-Release Formulations Of Apremilast in Healthy Men

A Phase 1 study testing Apremilast Immediate Release, Apremilast Modified Release 1 and Apremilast Modified Release 2 in people with Healthy Volunteers, run by Amgen at 1 site in United States.

Completed

Finished. The study has ended and is not enrolling. Results may be posted on the official record.

Official record
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Trial summary

This study will assess up to 12 different oral formulations of apremilast to determine how much apremilast is absorbed by the body compared to a reference formulation. Read more about this study

Who is it for?
Ages 18 to 55 years, men onlyHealthy volunteers can take part
Conditions the study is for
Healthy Volunteers
What is being tested?
Apremilast Immediate Release, Apremilast Modified Release 1 and Apremilast Modified Release 2
Type of treatment
Pill or oral medicine
Could I receive a placebo?
No, everyone receives an active treatment
How many people
80 participants
Where
1 siteUnited States
Study dates
7 Jan 2014to 11 Sep 2014
Phase
Phase 1
Are there results?
Yes, posted in the registrySummary in the doctors' view

Key requirements

Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.

  • Ages 18 to 55 years
  • Men only
  • Healthy volunteers accepted
  • Adult

Who may be able to join

  • Subjects must satisfy ALL of the following criteria to be eligible for enrollment into the study:
  • Must understand and voluntarily sign a written informed consent form prior to any study-related procedures being performed.
  • Must be able to communicate with the investigator, understand and comply with the requirements of the study, and agree to adhere to restrictions and examination schedules.
  • Male subjects of any race between 18 to 55 years of age (inclusive), and in good health as determined by the Investigator.
  • Has a body mass index between 18 and 33 kg/m^2 (inclusive).
  • No clinically significant laboratory tests as determined by the investigator.
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  • Must not have a fever, with systolic blood pressure: 90 to 140 mmHg and diastolic blood pressure: 60 to 90 mmHg, and pulse rate: 40 to 110 bpm (measurements taken while lying down).
  • Must have a normal or clinically acceptable 12-lead electrocardiogram (ECG).
  • Subjects (including those who have had a vasectomy) who engage in activity in which conception is possible must use barrier contraception (male latex condom or non-latex condom not made out of natural [animal] membrane [eg, polyurethane]) while on study medication, and for 28 days after the last dose of study medication.
  • Must agree to refrain from donating sperm, blood or plasma (other than for this study) while participating in this study and for at least 28 days after the last dose of study drug.

Who cannot join

  • The presence of ANY of the following will exclude any healthy subject from enrollment into the study:
  • History of any clinically significant and relevant neurological, gastrointestinal, renal, hepatic, cardiovascular, psychological, pulmonary, metabolic, endocrine, hematological, allergic disease, drug allergies, or other major disorders.
  • Any condition which places the subject at unacceptable risk if he were to participate in the study, or confounds the ability to interpret data from the study.
  • Use of any prescribed systemic or topical medication within 30 days of the first dose administration, unless Sponsor agreement is obtained.
  • Use of any non-prescribed systemic or topical medication (including vitamin/mineral supplements, and herbal medicines) within 14 days of the first dose administration, unless Sponsor agreement is obtained.
  • Any surgical or medical condition possibly affecting drug absorption, distribution, metabolism and excretion, eg, bariatric procedure, colon resection, irritable bowel syndrome, Crohn's disease, etc. Subjects with cholecytectomy and appendectomy may be included.
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  • 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).
  • Donated blood or plasma within 8 weeks before the first dose administration to a blood bank or blood donation center.
  • History of drug abuse (as defined by the current version of the Diagnostic and Statistical Manual (DSM) within 2 years before dosing, or a positive drug screen reflecting consumption of illicit drugs.
  • History of alcohol abuse (as defined by the current version of the DSM) within 2 years before dosing, or a positive alcohol screen.
  • Known to have serum hepatitis, or known to be a carrier of the hepatitis B surface antigen (HBsAg), or hepatitis C virus (HCV) antibody, or have a positive result to the test for human immunodeficiency virus (HIV) antibodies at Screening.

Trial locations and contacts

1 site in 1 country.

United States1 site

  • Covance Clinical Research Unit Inc.

    Madison, Wisconsin, 53704-2526

Other trials in United States

About this study

Official title: A Phase 1, Open-Label, Single Center Study to Evaluate the Pharmacokinetics of Prototype Modified-Release Formulations Of Apremilast (CC-10004) in Healthy Male Subjects

This study will assess up to 12 different oral formulations of apremilast to determine how much apremilast is absorbed by the body compared to a reference formulation.

Read the detailed description

This will be a single-center, open-label, crossover, single modified-release-dose study in adult males to evaluate the pharmacokinetics (PK) of prototype modified-release (MR) formulations compared to the reference immediate-release (IR) apremilast formulation. Within 4 separate groups, participants will be randomly assigned to a treatment sequence. A total of up to 12 test MR formulations may be evaluated.

Group 1: A 4-sequence, 4-period design to compare three modified-release prototypes with the reference immediate-release formulation. A total of 16 participants will be enrolled to obtain at least 12 participants who complete all 4 periods.

Group 2: A 4-sequence, 4-period design to compare three MR prototypes with the reference IR formulation. Sixteen participants will be enrolled to obtain at least 12 participants who complete all four periods.

Group 3: A six-sequence, three-period design to compare two MR prototypes with the reference IR formulation. Eighteen participants will be enrolled to obtain at least 12 participants who complete all three periods.

Group 4: A 10-sequence, 5-period design to compare four MR prototypes with the reference IR formulation. Thirty participants will be enrolled to obtain at least 20 participants who complete all five periods.

Being tested
Apremilast Immediate Release, Apremilast Modified Release 1, Apremilast Modified Release 2, Apremilast Modified Release 3, Apremilast Modified Release 4
Keywords
Apremilast, Healthy male subjects, Pharmacokinetics

What participants receive

What participants receive. In a randomised study each person is assigned to one group by chance.

  • Apremilast Immediate ReleaseDrug

    Also called Otezla, CC-10004

    30 mg immediate release tablets

  • Apremilast Modified Release 1Drug

    75 mg oral tablet of prototype modified release (MR) 1

  • Apremilast Modified Release 2Drug

    75 mg oral tablet of prototype MR 2

  • Apremilast Modified Release 3Drug

    75 mg oral capsule of prototype MR 3

  • Apremilast Modified Release 4Drug

    75 mg oral capsule of prototype MR 4

  • Apremilast Modified Release 5Drug

    75 mg oral capsule of prototype MR 5

  • Apremilast Modified Release 6Drug

    75 mg oral capsule of prototype MR 6

  • Apremilast Modified Release 8Drug

    80 mg oral capsule of prototype MR 8

  • Apremilast Modified Release 9Drug

    80 mg oral capsule of prototype MR 9

  • Apremilast Modified Release 11Drug

    80 mg oral capsule of prototype MR 11

  • Apremilast Modified Release 12Drug

    80 mg oral capsule of prototype MR 12

  • Apremilast Modified Release 13Drug

    80 mg oral capsule of prototype MR 13

  • Apremilast Modified Release 14Drug

    80 mg oral capsule of prototype MR 14

Study groups in NCT02236988
Study groupRoleWhat they receive
Group 1ExperimentalParticipants received the following 4 treatments, given in 4 possible sequences (ADBC, BACD, CBDA, and DCAB) with 7 to 10 days between each treatment: A) Two oral doses of 30 mg apremilast immediate release tablets 12 hours apart (reference formulation) B) A single oral dose 75 mg apremilast tablet prototype MR 1 C) A single oral dose 75 mg apremilast tablet prototype MR 2 D) A single oral dose 75 mg apremilast capsule prototype MR 3
Receives: Drug: Apremilast Immediate Release; Drug: Apremilast Modified Release 1; Drug: Apremilast Modified Release 2; Drug: Apremilast Modified Release 3
Group 2ExperimentalParticipants received the following 4 treatments, given in 4 possible sequences (AGEF, EAFG, FEGA, and GFAE) with 7 to 10 days between each treatment: A) Two oral doses of 30 mg apremilast immediate release tablets 12 hours apart (reference formulation) E) A single oral dose 75 mg apremilast capsule prototype MR 4 F) A single oral dose 75 mg apremilast capsule prototype MR 5 G) A single oral dose 75 mg apremilast capsule prototype MR 6
Receives: Drug: Apremilast Immediate Release; Drug: Apremilast Modified Release 4; Drug: Apremilast Modified Release 5; Drug: Apremilast Modified Release 6
Group 3ExperimentalParticipants received the following 3 treatments, given in 6 possible sequences (AIJ, IJA, JAI, AJI, IAJ, or JIA) with 7 to 10 days between each treatment: A) Two oral doses of 30 mg apremilast immediate release tablets 12 hours apart (reference formulation) I) A single oral dose 80 mg apremilast capsule prototype MR 8 J) A single oral dose 80 mg apremilast capsule prototype MR 9
Receives: Drug: Apremilast Immediate Release; Drug: Apremilast Modified Release 8; Drug: Apremilast Modified Release 9
Group 4ExperimentalParticipants received the following 5 treatments, given in 10 possible sequences (ALOMN, LMANO, MNLOA, NOMAL, OANLM, NMOLA, ONAML, AOLNM, LAMON, or MLNAO) with 7 to 10 days between each treatment: A) Two oral doses of 30 mg apremilast immediate release tablets 12 hours apart (reference formulation) L) A single oral dose 80 mg apremilast capsule prototype MR 11 M) A single oral dose 80 mg apremilast capsule prototype MR 12 N) A single oral dose 80 mg apremilast capsule prototype MR 13 O) A single oral dose 80 mg apremilast capsule prototype MR 14
Receives: Drug: Apremilast Immediate Release; Drug: Apremilast Modified Release 11; Drug: Apremilast Modified Release 12; Drug: Apremilast Modified Release 13; Drug: Apremilast Modified Release 14

What is being measured

The primary outcome is the main question the study is designed to answer.

  1. Group 1: Observed Maximum Plasma Concentration (Cmax) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  2. Group 1: Area Under the Plasma Concentration-time Curve From Time Zero to the Last Measured Time Point (AUC0-t) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  3. Group 1: Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC0-∞) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  4. Group 1: Time to Observed Maximum Plasma Concentration (Tmax) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  5. Group 1: Half-life of Apremilast in Terminal Phase (T1/2)

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  6. Group 1: Apparent Total Plasma Clearance (CL/F) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  7. Group 1: Apparent Total Volume of Distribution (Vz/F) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  8. Group 1: Relative Bioavailability of Apremilast Test Formulations Relative to Reference Corrected by Dose

    Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as:

    (AUC0-∞/Dose[test]) / (AUC0-∞/Dose[reference]) * 100%.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  9. Group 1: Relative Bioavailability of Apremilast Test Formulations Relative to Reference

    Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as:

    (AUC0-∞[test]) / (AUC0-∞[reference]) * 100%.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  10. Group 2: Observed Maximum Plasma Concentration (Cmax) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  11. Group 2: Area Under the Plasma Concentration-time Curve From Time Zero to the Last Measured Time Point (AUC0-t) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  12. Group 2: Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC0-∞) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

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

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  14. Group 2: Half-life of Apremilast in Terminal Phase (T1/2)

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  15. Group 2: Apparent Total Plasma Clearance (CL/F) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  16. Group 2: Apparent Total Volume of Distribution (Vz/F) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  17. Group 2: Relative Bioavailability of Apremilast Test Formulations Relative to Reference Corrected by Dose

    Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as:

    (AUC0-∞/Dose[test]) / (AUC0-∞/Dose[reference]) * 100%.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  18. Group 2: Relative Bioavailability of Apremilast Test Formulations Relative to Reference

    Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as:

    (AUC0-∞[test]) / (AUC0-∞[reference]) * 100%.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  19. Group 3: Observed Maximum Plasma Concentration (Cmax) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  20. Group 3: Area Under the Plasma Concentration-time Curve From Time Zero to the Last Measured Time Point (AUC0-t) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  21. Group 3: Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC0-∞) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  22. Group 3: Time to Observed Maximum Plasma Concentration (Tmax) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  23. Group 3: Half-life of Apremilast in Terminal Phase (T1/2)

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  24. Group 3: Apparent Total Plasma Clearance (CL/F) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  25. Group 3: Relative Bioavailability of Apremilast Test Formulations Relative to Reference Corrected by Dose

    Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as:

    (AUC0-∞/Dose[test]) / (AUC0-∞/Dose[reference]) * 100%.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  26. Group 3: Relative Bioavailability of Apremilast Test Formulations Relative to Reference

    Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as:

    (AUC0-∞[test]) / (AUC0-∞[reference]) * 100%.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  27. Group 4: Observed Maximum Plasma Concentration (Cmax) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  28. Group 4: Area Under the Plasma Concentration-time Curve From Time Zero to the Last Measured Time Point (AUC0-t) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

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

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  30. Group 4: Time to Observed Maximum Plasma Concentration (Tmax) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  31. Group 4: Half-life of Apremilast in Terminal Phase (T1/2)

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  32. Group 4: Apparent Total Plasma Clearance (CL/F) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  33. Group 4: Apparent Total Volume of Distribution (Vz/F) of Apremilast

    Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  34. Group 4: Relative Bioavailability of Apremilast Test Formulations Relative to Reference Corrected by Dose

    Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as:

    (AUC0-∞/Dose[test]) / (AUC0-∞/Dose[reference]) * 100%.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

  35. Group 4: Relative Bioavailability of Apremilast Test Formulations Relative to Reference

    Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as:

    (AUC0-∞[test]) / (AUC0-∞[reference]) * 100%.

    Measured: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.

Secondary outcomes (4)

  1. Group 1: Number of Participants With Treatment-emergent Adverse Events

    An adverse event (AE) is any noxious, unintended, or untoward medical occurrence that may appear or worsen in a participant during the course of a study. It may be 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.

    A treatment-emergent AE (TEAE) was defined as any AE that occurred after dosing of the study drug.

    A serious adverse event (SAE) is any AE occurring at any dose that:

    • Resulted in death;
    • Was life-threatening;
    • Required inpatient hospitalization or prolongation of existing hospitalization;
    • Resulted in persistent or significant disability/incapacity;
    • Was a congenital anomaly/birth defect;
    • Constituted an important medical event.

    Measured: Adverse events were collected for 7 to 10 days after each treatment.

  2. Group 2: Number of Participants With Treatment-emergent Adverse Events

    An adverse event (AE) is any noxious, unintended, or untoward medical occurrence that may appear or worsen in a participant during the course of a study. It may be 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.

    A treatment-emergent AE (TEAE) was defined as any AE that occurred after dosing of the study drug.

    A serious adverse event (SAE) is any AE occurring at any dose that:

    • Resulted in death;
    • Was life-threatening;
    • Required inpatient hospitalization or prolongation of existing hospitalization;
    • Resulted in persistent or significant disability/incapacity;
    • Was a congenital anomaly/birth defect;
    • Constituted an important medical event.

    Measured: Adverse events were collected for 7 to 10 days after each treatment.

  3. Group 3: Number of Participants With Treatment-emergent Adverse Events

    An adverse event (AE) is any noxious, unintended, or untoward medical occurrence that may appear or worsen in a participant during the course of a study. It may be 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.

    A treatment-emergent AE (TEAE) was defined as any AE that occurred after dosing of the study drug.

    A serious adverse event (SAE) is any AE occurring at any dose that:

    • Resulted in death;
    • Was life-threatening;
    • Required inpatient hospitalization or prolongation of existing hospitalization;
    • Resulted in persistent or significant disability/incapacity;
    • Was a congenital anomaly/birth defect;
    • Constituted an important medical event.

    Measured: Adverse events were collected for 7 to 10 days after each treatment.

  4. Group 4: Number of Participants With Treatment-emergent Adverse Events

    An adverse event (AE) is any noxious, unintended, or untoward medical occurrence that may appear or worsen in a participant during the course of a study. It may be 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.

    A treatment-emergent AE (TEAE) was defined as any AE that occurred after dosing of the study drug.

    A serious adverse event (SAE) is any AE occurring at any dose that:

    • Resulted in death;
    • Was life-threatening;
    • Required inpatient hospitalization or prolongation of existing hospitalization;
    • Resulted in persistent or significant disability/incapacity;
    • Was a congenital anomaly/birth defect;
    • Constituted an important medical event.

    Measured: Adverse events were collected for 7 to 10 days after each treatment.

Timeline

From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.

  1. First posted11 Sep 2014 (estimated)
  2. Study start7 Jan 2014
  3. Primary completion11 Sep 2014
  4. Study completion11 Sep 2014

Resources

More details

For doctors and researchers: how the study is designed, who runs it, and its registry IDs.

Study design
Study type
Interventional
Phase
Phase 1
Primary purpose
Other
Allocation
Randomised
Intervention model
Crossover
Masking
None (open label)
Enrolment
80 participants (actual)
IDs, dates and publications
ClinicalTrials.gov ID
NCT02236988
Sponsor's protocol ID
CC-10004-CP-027
Status last verified
Mar 2021
First submitted
9 Sep 2014
Last updated
1 Jun 2021
Data monitoring committee
No
Individual data sharing
Yes: De-identified individual patient data for variables necessary to address the specific research question in an approved data sharing request
Expanded access
Available

Questions about this trial

What is this clinical trial studying?

A Phase 1 study testing Apremilast Immediate Release, Apremilast Modified Release 1 and Apremilast Modified Release 2 in people with Healthy Volunteers, run by Amgen at 1 site in United States.

The full registered description is in the About this study section and the official record.

Who may be eligible to take part?

The sponsor lists 10 inclusion and 11 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.

Is this clinical trial currently recruiting?

The record says: finished, as of the sponsor's last update on 1 Jun 2021. Status can change between updates, so confirm with the study contact before making plans.

Where is the study taking place?

The record lists 1 site in United States. Whether a site is taking part right now should be confirmed with that site. See every site.

What are the possible benefits and risks?

They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.

What does this phase mean?

Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.

Not every study follows the same path, and some studies (observational studies, device studies) have no phase.

Are results available for this study?

Yes. Results are posted in the registry (first posted 1 Jun 2021). A summary is in the For doctors view, and the full results are on ClinicalTrials.gov.

How can a doctor refer a patient or contact the research team?

The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.

What does the primary outcome measure?

Group 1: Observed Maximum Plasma Concentration (Cmax) of Apremilast (time frame: IR reference formulation: predose and at 0.5, 1, 2, 3, 5, 8, 12, 12.5, 13, 14, 15, 17, 20, 24, 36, 48, 60, and 72 hours after the first dose; MR formulations: predose and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, 20, 24, 30, 36, 48, and 72 hours postdose.). The study lists 35 primary outcomes in all. It is what the study was designed to measure, not a finding.

Where can I read the original study information?

On the ClinicalTrials.gov record for NCT02236988.

Does a listing mean the treatment is approved or proven to work?

No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.

How often is this information updated?

AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 1 Jun 2021.

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