Roflumilast

Roflumilast is a highly selective phosphodiesterase-4 (PDE4) inhibitor. 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. The resultant increase in intracellular cAMP induced by roflumilast’s inhibition of PDE4 is thought to mediate its disease-modifying effects, although its precise mechanism of action has yet to be elucidated. The oral formulation of roflumilast is indicated to manage chronic obstructive pulmonary disease. It was first approved by the EMA in July 2010, and by the FDA in January 2018. Roflumilast topical cream is indicated to treat plaque psoriasis. The cream formulation was first approved by the FDA in July 2022 and by Health Canada in April 2023. On December 15, 2023, the FDA approved a new topical foam formulation of roflumilast for the treatment of seborrheic dermatitis in patients aged 9 years and older. It is grouped under the following drug class(es): PDE4 inhibitors. Its therapeutic use is listed as anti-asthmatic agents, anti-inflammatories, anti-psoriatic agents and dermatologicals. The directory classifies it as a commercial API with a synthetic source/manufacturing origin. Other names for this substance include Daliresp, BY-217, ZORYVE, DAXAS and roflumilastum. Its PubChem CID is 449193.