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
- 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)
- Associated Therapies
- -
Roflumilast in Chronic Obstructive Pulmonary Disease (COPD) Patients Treated With Fixed Dose Combinations of Long-acting β2-agonist (LABA) and Inhaled Corticosteroid (ICS)
- Conditions
- COPDRespiratory DisordersPulmonary DiseaseLung DiseasesChronic Obstructive Lung DiseasesCOPD ExacerbationChronic Obstructive Airway Disease
- Interventions
- Drug: RoflumilastDrug: Placebo
- First Posted Date
- 2011-09-30
- Last Posted Date
- 2017-04-13
- Lead Sponsor
- AstraZeneca
- Target Recruit Count
- 2354
- Registration Number
- NCT01443845
- Locations
- 🇷🇺
Forest Investigative Site 612, St. Petersburg, Russian Federation
🇷🇺Forest Investigative Site 600, St Petersburg, Russian Federation
🇺🇸Forest Investigative Site 248, Baltimore, Maryland, United States
Roflumilast and Cognition
- First Posted Date
- 2011-09-14
- Last Posted Date
- 2020-01-02
- Lead Sponsor
- Maastricht University Medical Center
- Target Recruit Count
- 22
- Registration Number
- NCT01433666
- Locations
- 🇳🇱
Maastricht University, Faculty of Psychology and Neuroscience, Maastricht, Limburg, Netherlands
A Study to Evaluate the Effect of Roflumilast on Airway Inflammation and Function Following Allergen Challenge in Subjects With Allergic Asthma
- First Posted Date
- 2011-06-03
- Last Posted Date
- 2016-10-25
- Lead Sponsor
- AstraZeneca
- Target Recruit Count
- 48
- Registration Number
- NCT01365533
- Locations
- 🇨🇦
Nycomed investigational site, Quebec, Canada
Pharmacokinetic Study of Single and Repeated Dose of Roflumilast 500 µg , in Healthy Chinese Subjects
- First Posted Date
- 2011-05-17
- Last Posted Date
- 2016-10-26
- Lead Sponsor
- AstraZeneca
- Target Recruit Count
- 32
- Registration Number
- NCT01354782
- Locations
- 🇨🇳
Nycomed Investigational Site, Beijing, China
Roflumilast in Chronic Obstructive Pulmonary Disease (COPD) Patients Treated With Fixed Combinations of Long-acting β2-agonists (LABA) and Inhaled Glucocorticosteroid (ICS)
- Conditions
- Chronic Obstructive Pulmonary Disease
- Interventions
- Drug: PlaceboDrug: Roflumilast
- First Posted Date
- 2011-04-05
- Last Posted Date
- 2016-12-13
- Lead Sponsor
- AstraZeneca
- Target Recruit Count
- 1945
- Registration Number
- NCT01329029
- Locations
- 🇦🇺
Nycomed Investigational site, Daws Park, Australia
🇬🇧Nycomed Investigational Site, Norwich, United Kingdom
A Chronic Obstructive Pulmonary Disease (COPD) Trial Investigating Roflumilast on Safety and Effectiveness in China, Hong Kong and Singapore:
- First Posted Date
- 2011-03-11
- Last Posted Date
- 2017-02-01
- Lead Sponsor
- AstraZeneca
- Target Recruit Count
- 626
- Registration Number
- NCT01313494
Efficacy of 500µg Roflumilast Once Daily Versus Placebo Over 12 Weeks in Patients With Diabetes Mellitus Type 2. A Double Blind, Parallel Group, Proof of Concept Clinical Study
- First Posted Date
- 2010-06-09
- Last Posted Date
- 2016-10-26
- Lead Sponsor
- AstraZeneca
- Target Recruit Count
- 487
- Registration Number
- NCT01140542
Pharmacodynamic/Pharmacokinetic Interactions Between Oral Roflumilast and Inhaled Formoterol
- First Posted Date
- 2009-07-16
- Last Posted Date
- 2016-12-02
- Lead Sponsor
- AstraZeneca
- Target Recruit Count
- 27
- Registration Number
- NCT00940329
- Locations
- 🇩🇪
Nycomed, Konstanz, Germany
Effect of Roflumilast on Exacerbation Rate in Patients With Chronic Obstructive Pulmonary Disease. Ratio-Study. (BY217/M2-112)
- Conditions
- Chronic Obstructive Pulmonary DiseaseCOPD
- First Posted Date
- 2007-02-02
- Last Posted Date
- 2016-11-30
- Lead Sponsor
- AstraZeneca
- Target Recruit Count
- 1100
- Registration Number
- NCT00430729
- Locations
- 🇬🇧
ALTANA Pharma, Cities in the United Kingdom, United Kingdom
Effect of Roflumilast in Chronic Obstructive Pulmonary Disease (COPD) Patients Treated With Tiotropium: The HELIOS Study (BY217/M2-128)
- Conditions
- Chronic Obstructive Pulmonary Disease
- Interventions
- Drug: PlaceboDrug: Roflumilast
- First Posted Date
- 2007-01-19
- Last Posted Date
- 2016-12-05
- Lead Sponsor
- AstraZeneca
- Target Recruit Count
- 743
- Registration Number
- NCT00424268
- Locations
- 🇬🇧
Altana Pharma/Nycomed Investigational Site, Yaxley, United Kingdom
Drug Development Updates
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