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

NCT02236988 | Completed Phase 1 Results

• 1 other identifier: CC-10004-CP-027
• Study Type: interventional
• Target: 80
• Locations: 1 country
• Sites: 1

Brief 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.

Conditions

Healthy Volunteers

Keywords

Apremilast; Healthy male subjects; Pharmacokinetics

Outcome Measures

Primary Outcomes (35)

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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%.

  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.

• 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%.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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%.

  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.

• 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%.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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%.

  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.

• 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%.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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.

  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.

• 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%.

  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.

• 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%.

  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)

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

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

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

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

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

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

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

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

Study Arms (4)

Group 1

EXPERIMENTAL

Participants 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

Drug: Apremilast Immediate Release; Drug: Apremilast Modified Release 1; Drug: Apremilast Modified Release 2; Drug: Apremilast Modified Release 3

Group 2

EXPERIMENTAL

Participants 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

Drug: Apremilast Immediate Release; Drug: Apremilast Modified Release 4; Drug: Apremilast Modified Release 5; Drug: Apremilast Modified Release 6

Group 3

EXPERIMENTAL

Participants 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

Drug: Apremilast Immediate Release; Drug: Apremilast Modified Release 8; Drug: Apremilast Modified Release 9

Group 4

EXPERIMENTAL

Participants 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

Drug: Apremilast Immediate Release; Drug: Apremilast Modified Release 11; Drug: Apremilast Modified Release 12; Drug: Apremilast Modified Release 13; Drug: Apremilast Modified Release 14

Interventions

Apremilast Immediate Release DRUG

30 mg immediate release tablets

Also known as: Otezla, CC-10004

Group 1; Group 2; Group 3; Group 4

Apremilast Modified Release 1 DRUG

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

Group 1

Apremilast Modified Release 2 DRUG

75 mg oral tablet of prototype MR 2

Group 1

Apremilast Modified Release 3 DRUG

75 mg oral capsule of prototype MR 3

Group 1

Apremilast Modified Release 4 DRUG

75 mg oral capsule of prototype MR 4

Group 2

Apremilast Modified Release 5 DRUG

75 mg oral capsule of prototype MR 5

Group 2

Apremilast Modified Release 6 DRUG

75 mg oral capsule of prototype MR 6

Group 2

Apremilast Modified Release 8 DRUG

80 mg oral capsule of prototype MR 8

Group 3

Apremilast Modified Release 9 DRUG

80 mg oral capsule of prototype MR 9

Group 3

Apremilast Modified Release 11 DRUG

80 mg oral capsule of prototype MR 11

Group 4

Apremilast Modified Release 12 DRUG

80 mg oral capsule of prototype MR 12

Group 4

Apremilast Modified Release 13 DRUG

80 mg oral capsule of prototype MR 13

Group 4

Apremilast Modified Release 14 DRUG

80 mg oral capsule of prototype MR 14

Group 4

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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.
• 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.

You may not qualify if:

• 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.
• 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.

Sponsors & Collaborators

• Amgen: lead

Study Sites (1)

Covance Clinical Research Unit Inc.

Madison, Wisconsin, 53704-2526, United States

Location

MeSH Terms

Interventions

apremilast

Results Point of Contact

• Title: Study Director
• Organization: Amgen Inc.

medinfo@amgen.com

866-572-6436

Study Officials

• MD

  Amgen

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: OTHER
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR
• Expanded Access: Yes

Study Record Dates

• First Submitted: September 9, 2014
• First Posted: September 11, 2014
• Study Start: January 7, 2014
• Primary Completion: September 11, 2014
• Study Completion: September 11, 2014
• Last Updated: June 1, 2021
• Results First Posted: June 1, 2021

Record last verified: 2021-03

Data Sharing

• IPD Sharing: Will share
• Shared Documents: STUDY PROTOCOL, SAP, ICF, CSR
• Time Frame: Data sharing requests relating to this study will be considered beginning 18 months after the study has ended and either 1) the product and indication have been granted marketing authorization in both the US and Europe or 2) clinical development for the product and/or indication discontinues and the data will not be submitted to regulatory authorities. There is no end date for eligibility to submit a data sharing request for this study.
• Access Criteria: Qualified researchers may submit a request containing the research objectives, the Amgen product(s) and Amgen study/studies in scope, endpoints/outcomes of interest, statistical analysis plan, data requirements, publication plan, and qualifications of the researcher(s). In general, Amgen does not grant external requests for individual patient data for the purpose of re-evaluating safety and efficacy issues already addressed in the product labelling. Requests are reviewed by a committee of internal advisors. If not approved, a Data Sharing Independent Review Panel will arbitrate and make the final decision. Upon approval, information necessary to address the research question will be provided under the terms of a data sharing agreement. This may include anonymized individual patient data and/or available supporting documents, containing fragments of analysis code where provided in analysis specifications. Further details are available at the URL below.

Locations

US (1)