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Roflumilast

Generic Name
Roflumilast
Brand Names
Daliresp, Zoryve, Daxas
Drug Type
Small Molecule
Chemical Formula
C17H14Cl2F2N2O3
CAS Number
162401-32-3
Unique Ingredient Identifier
0P6C6ZOP5U

Overview

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 the 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. It was first approved by FDA in July 2022 and by Health Canada in April 2023.

Background

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 the 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. It was first approved by FDA in July 2022 and by Health Canada in April 2023.

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. Topical roflumilast is indicated to treat plaque psoriasis, including intertriginous areas, in patients 12 years of age and older.

Associated Conditions

  • Exacerbation of COPD
  • Psoriasis Vulgaris (Plaque Psoriasis)

FDA Approved Products

ZORYVE
Manufacturer:Arcutis Biotherapeutics, Inc.
Route:TOPICAL
Strength:3 mg in 1 g
Approved: 2024/01/19
NDC:80610-130
roflumilast
Manufacturer:Strides Pharma Science Limited
Route:ORAL
Strength:500 ug in 1 1
Approved: 2023/03/21
NDC:64380-786
Daliresp
Manufacturer:AstraZeneca Pharmaceuticals LP
Route:ORAL
Strength:500 ug in 1 1
Approved: 2020/03/12
NDC:0310-0095
Roflumilast
Manufacturer:Zydus Pharmaceuticals USA Inc.
Route:ORAL
Strength:250 ug in 1 1
Approved: 2023/05/18
NDC:68382-624
ROFLUMILAST
Manufacturer:Micro Labs Limited
Route:ORAL
Strength:500 ug in 1 1
Approved: 2023/04/24
NDC:42571-259

Singapore Approved Products

No Singapore products found for this drug

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