Roflumilast is a selective phosphodiesterase-4 inhibitor indicated to decrease the risk of exacerbations in patients with severe chronic obstructive pulmonary disease (COPD) and to treat skin conditions such as plaque psoriasis and atopic dermatitis. PDE4 is a major cyclic-3',5′-adenosinemonophosphate (cyclic AMP, cAMP)-metabolizing enzyme expressed on nearly all immune and pro-inflammatory cells, in addition to structural cells like those of the smooth muscle or epithelium.
- Mechanism
- Curator reviewed · 1 reference
Roflumilast and its active metabolite (roflumilast N-oxide) are inhibitors of PDE4. Roflumilast and roflumilast N-oxide inhibition of PDE4 (a major cyclic 3′,5′-adenosine monophosphate (cyclic AMP) metabolizing enzyme) activity leads to accumulation of intracellular cyclic AMP. The specific mechanism(s) by which roflumilast exerts its therapeutic action is not well defined.
- Primary indication
- Oral roflumilast is indicated to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations.Curator reviewed · 16 structured indications
- Formula / weight
- C17H14Cl2F2N2O3 · 403.207 g/mol (avg)
- First approval
- Canada, 2017 · United States, 2011 · European Union, 2016
- Code names
- ARQ-154 · B-9302-107 · BY-217 · BYK-20869
- Brand names
Resolves to
MNDBXUUTURYVHR-UHFFFAOYSA-NSMILESFC(F)OC1=C(OCC2CC2)C=C(C=C1)C(=O)NC1=C(Cl)C=NC=C1ClWhat you can answer from here — as of September 23, 2026
Which other approved drugs treat the same conditions as Roflumilast, and which companies have late-stage candidates in those indications?
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