Products
Apremilast is commercially available in the form of film-coated tablets (Otezla). It was approved in the United States in 2014 and in many countries and the EU in 2015.
Structure and properties
Apremilast (C22H24N2O7S, Mr = 460.5 g/mol) is a dioxoisoindole acetamide derivative.
Effects
Apremilast (ATC L04AA32) has immunomodulatory and anti-inflammatory properties. The effects are due to inhibition of phosphodiesterase-4 (PDE-4) in inflammatory cells, resulting in an increase in intracellular cAMP. This results in decreased formation of inflammatory mediators, such as TNF-alpha, IL-17, and IL-13, and increased formation of anti-inflammatory mediators, such as IL-10.
Indications
- Moderate to severe plaque psoriasis (2nd-line agent).
- Active psoriatic arthritis (2nd choice agent).
Dosage
According to the professional information. Treatment is started cautiously. Subsequently, one tablet twice daily is taken independently of meals. In patients with severe renal insufficiency, the dose must be reduced to one tablet once daily.
Contraindications
- Hypersensitivity
- Pregnancy
Full precautions can be found in the drug label.
Interactions
Apremilast is extensively metabolized by both CYP-mediated and non-CYP-mediated pathways. Drug-drug interactions are possible with CYP inducers. There are no clinically relevant interactions with CYP inhibitors, oral contraceptives, and methotrexate.
Adverse effects
The most common potential adverse effects include diarrhea, nausea, and headache. Apremilast use may be associated with depressed mood and weight loss.