Apremilast

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Apremilast
Apremilast.svg
Systematic (IUPAC) name
N-{2-[(1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide
Clinical data
Trade names Otezla
Pregnancy cat. C (US)
Legal status -only (US)
Pharmacokinetic data
Bioavailability 73%[1]
Protein binding 68%[1]
Metabolism Hepatic (CYP3A4, with minor contributions from CYP2A6, CYP1A2)[1]
Half-life 6-9 hours[1]
Excretion Urine (58%), faeces (39%)[1]
Identifiers
ATC code L04AA32
PubChem CID 11561674
ChemSpider 9736448
ChEBI CHEBI:78540
ChEMBL CHEMBL514800
Chemical data
Formula C22H24N2O7S 
Mol. mass 460.500 g/mol

Apremilast (brand name Otezla[2]) 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.[3] It has anti-inflammatory activity.

Medical use[edit]

Apremilast was approved by the USFDA in March 2014 for treatment of adults with active psoriatic arthritis.[4] It is also being tested for its efficacy in treating other chronic inflammatory diseases such as ankylosing spondylitis, Behcet's disease, and rheumatoid arthritis.

See also[edit]

References[edit]