Apremilast (Otezla): Uses, Dose, MOA, Side effects

Apremilast is a prescription medication available as an oral pill for treating certain inflammatory conditions, including psoriasis, psoriatic arthritis, and oral ulcers associated with Behçet’s syndrome.

It is a type of drug called a phosphodiesterase 4 (PDE4) inhibitor, which works by blocking the activity of an enzyme called PDE4.

This enzyme is involved in the inflammation process, and blocking it helps to reduce inflammation and its associated symptoms.

Apremilast was first approved by the US Food and Drug Administration (FDA) in 2014 for the treatment of psoriatic arthritis, and in 2015 for the treatment of moderate-to-severe plaque psoriasis. Since then, it has also been approved for the treatment of oral ulcers associated with Behçet’s syndrome.

Apremilast is marketed by Celgene Corporation, which is now a subsidiary of Bristol Myers Squibb following a merger in 2019.

Celgene initially developed Apremilast and obtained FDA approval for its use. After the merger, Bristol Myers Squibb took over the marketing of the drug. Apremilast is sold under the brand name Otezla.

Apremilast Class: Phosphodiesterase Inhibitor

Apremilast Category: immunomodulatory drug

Apremilast (Otezla) FDA-approved indications:

The FDA has approved Apremilast (Otezla) for the following indications:

1. Moderate to severe plaque psoriasis in adult patients who are candidates for phototherapy or systemic therapy.
2. Active psoriatic arthritis in adult patients, alone or in combination with DMARDs (disease-modifying antirheumatic drugs), such as methotrexate.
3. Oral ulcers associated with Behçet’s syndrome in adults.

Apremilast (Otezla) Dose:

The usual daily maintenance dose of Apremilast (Otezla) for the treatment of plaque psoriasis, psoriatic arthritis, and oral ulcers due to Behcet’s syndrome is 60 mg in two equally divided doses.

Treatment is usually initiated in a low dose and titrated upwards as mentioned in the table below [Ref]:

The maximum recommended dose in patients with severe renal impairment is 30 mg orally once a day.

Apremilast (Otezla) Contraindications:

There are a few contraindications to the use of Apremilast (Otezla). These include:

• Hypersensitivity:

Apremilast is contraindicated in patients with a known hypersensitivity to the drug or any of its components.

• PDE4 inhibitors:

Apremilast is a PDE4 inhibitor, and its use is contraindicated in patients who are taking other PDE4 inhibitors, such as roflumilast.

• Pregnancy:

Apremilast may cause fetal harm if taken during pregnancy. It is contraindicated in pregnant women and women who are planning to become pregnant.

Apremilast (Otezla) Side effects:

Some of the important side effects of Apremilast are mentioned in the table below:

Apremilast and Depression:

Depression is a possible side effect of Apremilast, although it is not a common side effect. In clinical trials, depression was reported in a small percentage of patients taking Apremilast, and it was generally mild to moderate in severity.

Patients taking Apremilast should be aware of the potential for depression and should promptly report any symptoms of depression to their healthcare provider, such as feelings of sadness, hopelessness, loss of interest in activities, changes in sleep patterns, or thoughts of self-harm.

In some cases, Apremilast may not be the best treatment option for patients with a history of depression or other mood disorders.

Apremilast (Otezla) Drug Interactions:

Apremilast (Otezla) Mechanism of action (MOA):

Apremilast is a medication that works by inhibiting the activity of an enzyme called phosphodiesterase 4 (PDE4).

PDE4 is involved in the regulation of inflammation and immune response. By inhibiting PDE4, it reduces the production of certain pro-inflammatory cytokines and increases the production of anti-inflammatory cytokines.

This helps to reduce inflammation and modify the immune response, which can lead to improvement in certain inflammatory conditions.

Apremilast cost:

According to GoodRx, as of February 2023, the average retail price for:

• 10mg (30 tablets): $2,800,
• 30 mg (30 tablets): $3,600.

Apremilast Vs Roflumilast: Are they the same:

Roflumilast is also a phosphodiesterase inhibitor, however, it is indicated only for the treatment of COPD.

Here is a table comparing Apremilast vs Roflumiast: