|Systematic (IUPAC) name|
|Metabolism||Hepatic (CYP3A4, with minor contributions from CYP2A6, CYP1A2)|
|Excretion||Urine (58%), faeces (39%)|
Apremilast (brand name Otezla) is an orally available small molecule inhibitor of phosphodiesterase 4 (PDE4). Apremilast specifically inhibits PDE4 and inhibits spontaneous production of TNF-alpha from human rheumatoid synovial cells. It has anti-inflammatory activity.
Apremilast was approved by the USFDA in March 2014 for treatment of adults with active psoriatic arthritis. Apremilast is the first oral agent that is FDA-approved for the treatment of psoriatic arthritis and offers the convenience of oral dosing compared to treatment with biopharmaceuticals. In September 2014, the USFDA approved Otezla (apremilast) for the treatment of moderate to severe plaque psoriasis. It is also being tested for its efficacy in treating other chronic inflammatory diseases such as ankylosing spondylitis, Behcet's disease, and rheumatoid arthritis.Celgene reported seven kinds of crystal form A,B,C,D,E,F and G and thought the crystal form B was the most thermodynamically stable anhydrous form.However,Utopharm company reported another more thermodynamically stable anhydrous form II than the crystal form B,.
Common mild to moderate adverse effects associated with apremilast include:
Depression: Worsening depression, suicidal thoughts, and other mood changes may occur with apremilast. Risks and benefits of therapy must be carefully evaluated by a health professional before apremilast is prescribed in patients with a history of depression and/or suicidal thoughts.
Weight loss: Weight loss has been associated with apremilast and should be frequently monitored during treatment. Reports from clinical studies indicated a 5-10% decrease in body weight in 10% of patients taking Otezla (compared to 3.3% of patients taking placebo).
Concurrent use of strong cytochrome P450 enzyme inducers has been shown to decrease exposure of apremilast and can result in reduced or loss of efficacy of apremilast. It is not recommended to use simultaneously with strong P450 enzyme inducers, including:
- St. John's Wort (drug-herb interaction)
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