Roflumilast is a highly selective phosphodiesterase-4 (PDE4) inhibitor.[A251385] PDE4 is a major cyclic-3',5′-adenosinemonophosphate (cyclic AMP, cAMP)-metabolizing enzyme [L37564] expressed on nearly all immune and pro-inflammatory cells, in addition to structural cells like those of the smooth muscle or epithelium.[A251385] 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.[L37564,A251385] The oral formulation of roflumilast is indicated to manage chronic obstructive pulmonary disease.[L46546] It was first approved by the EMA in July 2010, and by the FDA in January 2018.[L37564] Roflumilast topical cream is indicated to treat plaque psoriasis. The cream formulation was first approved by the FDA in July 2022 [L42580] and by Health Canada in April 2023.[L46541] 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.[L49281]
Synonyms
Roflumilast
Roflumilastum
Brand Names
Libertek
Daliresp
Zoryve
Daxas
Roflumilast
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.[L37564, L46541, L46546] Topical cream roflumilast is indicated to treat plaque psoriasis, including intertriginous areas, in patients 12 years of age and older, while topical foam roflumilast is indicated to treat seborrheic dermatitis in adult and pediatric patients 9 years of age and older..[L42580, L46541, L49276]
Drug Info/Drug Targets: DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Knox C, Law V, Jewison
T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS.
Nucleic Acids Res. 2011 Jan; 39 (Database issue):D1035-41. | PMID:21059682
