Conditions: Healthy Volunteers
Keywords: Apremilast Healthy male subjects Pharmacokinetics
Allocation: RANDOMIZED | Intervention model: CROSSOVER
Enrollment: 80
Healthy volunteers: yes

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.

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.

Arms:
arm 1: 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 arm 2: 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 arm 3: 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 arm 4: 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

Interventions: intervention 1: Apremilast Immediate Release intervention 2: Apremilast Modified Release 1 intervention 3: Apremilast Modified Release 2 intervention 4: Apremilast Modified Release 3 intervention 5: Apremilast Modified Release 4 intervention 6: Apremilast Modified Release 5 intervention 7: Apremilast Modified Release 6 intervention 8: Apremilast Modified Release 8 intervention 9: Apremilast Modified Release 9 intervention 10: Apremilast Modified Release 11 intervention 11: Apremilast Modified Release 12 intervention 12: Apremilast Modified Release 13 intervention 13: Apremilast Modified Release 14
Intervention descriptions: intervention 1: 30 mg immediate release tablets intervention 2: 75 mg oral tablet of prototype modified release (MR) 1 intervention 3: 75 mg oral tablet of prototype MR 2 intervention 4: 75 mg oral capsule of prototype MR 3 intervention 5: 75 mg oral capsule of prototype MR 4 intervention 6: 75 mg oral capsule of prototype MR 5 intervention 7: 75 mg oral capsule of prototype MR 6 intervention 8: 80 mg oral capsule of prototype MR 8 intervention 9: 80 mg oral capsule of prototype MR 9 intervention 10: 80 mg oral capsule of prototype MR 11 intervention 11: 80 mg oral capsule of prototype MR 12 intervention 12: 80 mg oral capsule of prototype MR 13 intervention 13: 80 mg oral capsule of prototype MR 14

Protocol document: