Apremilast
CAS No.
608141-41-9
Reference product
OTEZLA/CELGENE
Polymorphic form
Form B
Therapeutic Area
Musculo-skeletal system
Status
pipeline
EU DMF readiness
✓
US DMF readiness
031141
Drug description:
Apremilast belongs to selective immunosuppressants.
Apremilast, alone or in combination with Disease Modifying Antirheumatic Drugs (DMARDs), is indicated for the treatment of active psoriatic arthritis (PsA) in adult patients who have had an inadequate response or who have been intolerant to a prior DMARD therapy. Apremilast is indicated for the treatment of moderate to severe chronic plaque psoriasis in adult patients who failed to respond to or who have a contraindication to, or are intolerant to other systemic therapy including cyclosporine, methotrexate or psoralen and ultraviolet-A light (PUVA).
It is formulated as film coated tablet for oral administration.
Mechanism of action:
Apremilast is an inhibitor of phosphodiesterase 4 (PDE4), works intracellularly to modulate a network of pro-inflammatory and anti-inflammatory mediators. PDE4 is a cyclic adenosine monophosphate (cAMP)-specific PDE and the dominant PDE in inflammatory cells. PDE4 inhibition elevates intracellular cAMP levels, which in turn down-regulates the inflammatory response by modulating the expression of TNF-α, IL-23, IL-17 and other inflammatory cytokines. Cyclic AMP also modulates levels of anti-inflammatory cytokines such as IL-10.These pro- and anti-inflammatory mediators have been implicated in psoriatic arthritis and psoriasis.
The above product is presented solely for informational purposes and does not constitute an offer in any sense. Products with PIPELINE & EARLY DEVELOPMENT STATUS under patent (SPC) protection in Poland and/or other countries are not offered until expiration of the corresponding IP right.