Roflumilast

Generic Name: Roflumilast

Brand Names: Daliresp, Zoryve, Daxas

Drug Type: Small Molecule

Chemical Formula: C_₁₇H_₁₄Cl_₂F_₂N_₂O_₃

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: -

Clinical Trials

Safety, Tolerability and Efficacy of 28-day Inhaled CHF 6001 DPI in COPD Patients

Phase 2

Completed

Conditions: COPD

Interventions: Drug: CHF6001 DPI
Drug: Placebo
Drug: Roflumilast

First Posted Date: 2012-11-21

Last Posted Date: 2017-03-29

Lead Sponsor: Chiesi Farmaceutici S.p.A.

Target Recruit Count: 55

Registration Number: NCT01730404

Locations: 🇮🇪
Celerion, Belfast, Ireland
🇬🇧
Medicines Evaluation Unit Ltd, Manchester, United Kingdom
🇬🇧
Nottingham University Hospitals NHS Trust, Nottingham, United Kingdom

and more 2 locations

Safety and Efficacy of Roflumilast and Pioglitazone in Treating Adults With Nonalcoholic SteatoHepatitis

Phase 2

Terminated

Conditions: Nonalcoholic Steatohapatitis

Interventions: Drug: Roflumilast
Drug: Placebo
Drug: Pioglitazone

First Posted Date: 2012-10-10

Last Posted Date: 2017-02-01

Lead Sponsor: AstraZeneca

Target Recruit Count: 20

Registration Number: NCT01703260

Impact of Roflumilast on Visceral Adiposity and Metabolic Profile in Chronic Obstructive Pulmonary Disease

Phase 2

Terminated

Conditions: Metabolic Syndrome
Chronic Obstructive Pulmonary Disease

Interventions: Drug: Placebo
Drug: Roflumilast

First Posted Date: 2012-10-05

Last Posted Date: 2014-11-11

Lead Sponsor: Laval University

Target Recruit Count: 14

Registration Number: NCT01701934

Locations: 🇨🇦
Centre hospitalier de l'Université de Montréal, Montréal, Quebec, Canada
🇨🇦
Institut universitaire de cardiologie et de pneumologie de Québec, Québec, Quebec, Canada
🇨🇦
St. Paul's Hospital, Vancouver, British Columbia, Canada

and more 2 locations

Roflumilast Plus Alogliptin Proof-of-Mechanism Study in Type2 Diabetes

Phase 1

Completed

Conditions: Type 2 Diabetes

Interventions: Drug: Roflumilast
Drug: Exenatide
Drug: Alogliptin
Drug: Placebo to alogliptin
Drug: Placebo to roflumilast

First Posted Date: 2012-08-14

Last Posted Date: 2017-02-01

Lead Sponsor: AstraZeneca

Target Recruit Count: 40

Registration Number: NCT01664624

Effects of ROFLUMILAST on Subclinical Atherosclerosis in Chronic Obstructive Pulmonary Disease (COPD)

Phase 4

Completed

Conditions: Chronic Obstructive Pulmonary Disease and Allied Conditions

Interventions: Drug: Placebo
Drug: Roflumilast

First Posted Date: 2012-06-28

Last Posted Date: 2019-04-12

Lead Sponsor: LudwLudwig Boltzmann Institute for COPD and Respiratory Epidemiology

Target Recruit Count: 80

Registration Number: NCT01630200

Locations: 🇦🇹
Deparment for Respiratory and Critical Care Medicine, Otto Wangner Hospital, Vienna, Austria

Phase2, Single Group, Open Clinical Trial to Evaluate the Efficacy and Safety of Roflumilast in Symptomatic Bronchiectasis Patients

Phase 2

Conditions: Symptomatic Bronchiectasis

Interventions: Drug: Roflumilast

First Posted Date: 2012-04-19

Last Posted Date: 2012-04-19

Lead Sponsor: Seoul National University Bundang Hospital

Target Recruit Count: 25

Registration Number: NCT01580748

Locations: 🇰🇷
Seoul National University Bundang Hospital, Seongnam, Gyeongi-do, Korea, Republic of

A Placebo-controlled Trial of Daliresp on Chronic Obstructive Pulmonary Disease (COPD)

Not Applicable

Completed

Conditions: COPD

Interventions: Drug: placebo
Drug: roflumilast

First Posted Date: 2012-04-06

Last Posted Date: 2015-10-19

Lead Sponsor: University of Alabama at Birmingham

Target Recruit Count: 27

Registration Number: NCT01572948

Locations: 🇺🇸
UAB Lung Health Center, Birmingham, Alabama, United States

Trial to Assess the Anti-inflammatory Effects of Roflumilast in Chronic Obstructive Pulmonary Disease

Phase 3

Completed

Conditions: COPD
Chronic Obstructive Pulmonary Disease

Interventions: Drug: Placebo
Drug: Roflumilast

First Posted Date: 2012-01-13

Last Posted Date: 2019-11-29

Lead Sponsor: AstraZeneca

Target Recruit Count: 158

Registration Number: NCT01509677

Evaluation With CT Scan of Possible Changes in Airways After Treatment With Daxas® in Severe Chronic Obstructive Pulmonary Disease Patients

Phase 4

Completed

Conditions: Pulmonary Disease, Chronic Obstructive

Interventions: Drug: Placebo of Roflumilast
Drug: Roflumilast
Radiation: Functional Respiratory Imaging

First Posted Date: 2011-11-29

Last Posted Date: 2013-09-19

Lead Sponsor: FLUIDDA nv

Target Recruit Count: 41

Registration Number: NCT01480661

Locations: 🇧🇪
ZNA Middelheim, Antwerp, Belgium
🇧🇪
Antwerp University Hospital, Edegem, Antwerp, Belgium

Effect of Roflumilast at Acute Exacerbations of Chronic Obstructive Pulmonary Disease

Phase 2

Terminated

Conditions: Chronic Obstructive Pulmonary Disease With (Acute) Exacerbation

Interventions: Drug: Roflumilast
Drug: Placebo

First Posted Date: 2011-11-17

Last Posted Date: 2017-02-14

Lead Sponsor: AstraZeneca

Target Recruit Count: 81

Registration Number: NCT01473758

Locations: 🇬🇧
Academic Unit of Respiratory Medicine, Royal Free Hospital, Jadwiga A. Wedzicha, London, United Kingdom

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