Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Label indication OTEZLA/OTEZLA XR, an inhibitor of phosphodiesterase 4 (PDE4), is indicated for the treatment of: Adult patients with: Active psoriatic arthritis ( 1.1 ) Plaque psoriasis who are candidates for phototherapy or systemic therapy ( 1.2 ) Oral ulcers associated with Behçet's Disease ( 1.3 ) Pediatric patients 6 years of age and older with: Active psoriatic arthritis ( 1.1 ) Moderate to severe plaque psoriasis who are… FDA label
Also known as Otezla, CC-10004
Apremilast Immediate Release · 1 trial · 1 indication
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as: (AUC0-∞/Dose\[test\]) / (AUC0-∞/Dose\[reference\]) \* 100%.
Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as: (AUC0-∞\[test\]) / (AUC0-∞\[reference\]) \* 100%.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as: (AUC0-∞/Dose\[test\]) / (AUC0-∞/Dose\[reference\]) \* 100%.
Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as: (AUC0-∞\[test\]) / (AUC0-∞\[reference\]) \* 100%.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as: (AUC0-∞/Dose\[test\]) / (AUC0-∞/Dose\[reference\]) \* 100%.
Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as: (AUC0-∞\[test\]) / (AUC0-∞\[reference\]) \* 100%.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Concentrations of apremilast in plasma were measured using a validated liquid chromatography tandem mass spectrometry assay.
Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as: (AUC0-∞/Dose\[test\]) / (AUC0-∞/Dose\[reference\]) \* 100%.
Relative bioavailability of each test formulation compared to the reference formulation corrected by dose, calculated as: (AUC0-∞\[test\]) / (AUC0-∞\[reference\]) \* 100%.
| Arm | Type | Description |
|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 |
| Name | Type | Description |
|---|---|---|
| Apremilast Immediate Release | DRUG | 30 mg immediate release tablets |
| Apremilast Modified Release 1 | DRUG | 75 mg oral tablet of prototype modified release (MR) 1 |
| Apremilast Modified Release 2 | DRUG | 75 mg oral tablet of prototype MR 2 |
| Apremilast Modified Release 3 | DRUG | 75 mg oral capsule of prototype MR 3 |
| Apremilast Modified Release 4 | DRUG | 75 mg oral capsule of prototype MR 4 |
| Apremilast Modified Release 5 | DRUG | 75 mg oral capsule of prototype MR 5 |
| Apremilast Modified Release 6 | DRUG | 75 mg oral capsule of prototype MR 6 |
| Apremilast Modified Release 8 | DRUG | 80 mg oral capsule of prototype MR 8 |
| Apremilast Modified Release 9 | DRUG | 80 mg oral capsule of prototype MR 9 |
| Apremilast Modified Release 11 | DRUG | 80 mg oral capsule of prototype MR 11 |
| Apremilast Modified Release 12 | DRUG | 80 mg oral capsule of prototype MR 12 |
| Apremilast Modified Release 13 | DRUG | 80 mg oral capsule of prototype MR 13 |
| Apremilast Modified Release 14 | DRUG | 80 mg oral capsule of prototype MR 14 |
Inclusion Criteria: Subjects must satisfy ALL of the following criteria to be eligible for enrollment into the study: 1. Must understand and voluntarily sign a written informed consent form prior to any study-related procedures being performed. 2. Must be able to communicate with the investigator,...
Apremilast Immediate Release is an immediate-release small molecule formulation of apremilast being developed by Amgen Inc. (ticker AMGN). It is in Phase 1 clinical development, with the disclosed clinical activity conducted in healthy adult male volunteers rather than in a patient population with a named disease.
Apremilast Immediate Release targets the phosphodiesterase 4 (PDE4) enzymes, specifically the PDE4A, PDE4D, PDE4B, and PDE4C subtypes. It acts as an inhibitor of these PDE4 enzymes, which are the molecular targets named for this small molecule asset.
Apremilast Immediate Release is being developed by Amgen Inc., which trades under the ticker AMGN. Amgen is the developer listed for this immediate-release apremilast formulation.
Apremilast Immediate Release is in Phase 1 clinical development. It is an investigational formulation and is not approved. One Phase 1 trial has been completed, and no trials are currently active, so the disclosed clinical work to date has been early-stage pharmacokinetic evaluation.
Apremilast Immediate Release has been studied in one completed Phase 1 trial, NCT02236988, titled a study to evaluate the pharmacokinetics of prototype modified-release formulations of apremilast in healthy men. That trial enrolled 80 participants in the United States, was randomized and controlled, and used healthy male volunteers aged 18 years and older.