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®
Apremilast IR · 1 trial · 1 indication
| Arm | Type | Description |
|---|---|---|
| Part 1: Apremilast 30 mg IR BID / Apremilast 75 mg XL QD | EXPERIMENTAL | Participants received apremilast 30 mg immediate release (IR) tablet twice a day (BID) for 7 days in treatment period 1 then apremilast 75 mg extended release (XL) formulation once a day (QD) for 7 days in treatment period 2. |
| Part 1: Apremilast 75 mg XL QD / Apremilast 30 mg IR BID | EXPERIMENTAL | Participants received apremilast 75 mg XL formulation once a day for 7 days in treatment period 1 then apremilast 30 mg IR tablet twice a day for 7 days in treatment period 2. |
| Part 2: Sequence 1 | EXPERIMENTAL | Participants received a single dose of apremilast in each of 4 treatment periods according to the following: Treatment period 1: Apremilast 30 mg IR tablet under fasted conditions; Treatment period 2: Apremilast 75 mg XL formulation after a high-fat meal; Treatment period 3: Apremilast 75 mg XL formulation under fasted conditions; Treatment period 4: Apremilast 75 mg XL formulation after a standard meal. |
| Part 2: Sequence 2 | EXPERIMENTAL | Participants received a single dose of apremilast in each of 4 treatment periods according to the following: Treatment period 1: Apremilast 75 mg XL formulation under fasted conditions; Treatment period 2: Apremilast 30 mg IR tablet under fasted conditions; Treatment period 3: Apremilast 75 mg XL formulation after a standard meal; Treatment period 4: Apremilast 75 mg XL formulation after a high-fat meal. |
| Part 2: Sequence 3 | EXPERIMENTAL | Participants received a single dose of apremilast in each of 4 treatment periods according to the following: Treatment period 1: Apremilast 75 mg XL formulation after a standard meal; Treatment period 2: Apremilast 75 mg XL formulation under fasted conditions; Treatment period 3: Apremilast 75 mg XL formulation after a high-fat meal; Treatment period 4: Apremilast 30 mg IR tablet under fasted conditions. |
| Part 2: Sequence 4 | EXPERIMENTAL | Participants received a single dose of apremilast in each of 4 treatment periods according to the following: Treatment period 1: Apremilast 75 mg XL formulation after a high-fat meal; Treatment period 2: Apremilast 75 mg XL formulation after a standard meal; Treatment period 3: Apremilast 30 mg IR tablet under fasted conditions; Treatment period 4: Apremilast 75 mg XL formulation under fasted conditions. |
| Name | Type | Description |
|---|---|---|
| Apremilast IR | DRUG | Apremilast immediate release tablet |
| Apremilast XL | DRUG | Apremilast extended release formulation tablet |
Inclusion Criteria: Subjects must satisfy the following criteria to be enrolled in the study (Part 1 and Part 2): 1. Must understand and voluntarily sign a written Informed consent form (ICF) prior to any study-related procedures being performed. 2. Must be able to communicate with the investigato...
Apremilast IR is an immediate-release small molecule formulation of apremilast, a PDE4 inhibitor. It is being developed by Amgen Inc. (ticker AMGN) and has been studied in a Phase 1 clinical trial in healthy adult volunteers. The specific therapeutic indication for this formulation has not been disclosed.
Apremilast IR targets phosphodiesterase 4 (PDE4), specifically the PDE4A, PDE4B, PDE4C, and PDE4D subtypes. It acts as a PDE4 inhibitor. By inhibiting these enzymes, the drug modulates intracellular signaling pathways, though the precise clinical consequences of this inhibition for the immediate-release formulation are still under early investigation.
Apremilast IR is being developed by Amgen Inc., which trades under the ticker symbol AMGN. Amgen is the sponsor responsible for the clinical development of this immediate-release formulation of apremilast.
Apremilast IR is in Phase 1 clinical development. It is an investigational formulation and has not been approved by the FDA. The Phase 1 program has completed one trial, and no active trials are currently listed for this specific immediate-release formulation.
Apremilast IR has been evaluated in one completed Phase 1 trial, NCT02777554, titled A Study to Evaluate the Pharmacokinetic Exposure of 2 Formulations of Apremilast in Healthy Adults. The trial enrolled 144 healthy adult volunteers in the United States, was randomized and controlled, and did not use double blinding.
Apremilast IR is an immediate-release formulation of apremilast, the active drug substance. The IR designation refers to the formulation's release characteristics rather than a different molecule. This distinguishes it from other formulation approaches that may be under development for the same active ingredient.