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.
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)
Research Report
Comprehensive Monograph: Roflumilast (DB01656)
Section 1: Molecular Profile and Physicochemical Characteristics
Roflumilast is a small molecule drug that represents a significant therapeutic advancement in the management of specific inflammatory diseases. Its development and application are rooted in its precise chemical structure and distinct physicochemical properties, which dictate its interaction with its biological target and its behavior within the human body. This section provides a foundational overview of the molecule's chemical identity, nomenclature, and key physical characteristics.
1.1 Chemical Identity and Nomenclature
Roflumilast is chemically classified as a benzamide derivative. Its structure is the result of the formal condensation of the carboxy group of 3-(cyclopropylmethoxy)-4-(difluoromethoxy)benzoic acid with the amino group of 3,5-dichloropyridin-4-amine.[1] This specific arrangement of functional groups, including an aromatic ether, a chloropyridine, an organofluorine compound, and a cyclopropane member, is critical to its pharmacological activity.[1]
The molecule is identified across scientific and regulatory domains by a set of standardized names and codes:
- Systematic (IUPAC) Name: 3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide.[1]
- Generic Name: Roflumilast.
- CAS Number: 162401-32-3, its unique registry number assigned by the Chemical Abstracts Service.[1]
- DrugBank ID: DB01656, its accession number in the comprehensive DrugBank database.[1]
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/05/18 | Phase 1 | Recruiting | |||
2025/03/06 | Phase 3 | Recruiting | |||
2024/11/07 | Phase 2 | Completed | |||
2024/10/18 | Phase 3 | Recruiting | |||
2024/10/16 | Early Phase 1 | Recruiting | |||
2024/10/08 | Phase 3 | Recruiting | |||
2024/06/13 | Phase 1 | Active, not recruiting | |||
2024/06/03 | Phase 4 | Recruiting | |||
2023/06/01 | Phase 1 | Not yet recruiting | |||
2023/03/10 | Phase 3 | Completed |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| AstraZeneca Pharmaceuticals LP | 0310-0095 | ORAL | 500 ug in 1 1 | 3/12/2020 | |
| Golden State Medical Supply, Inc. | 51407-975 | ORAL | 500 ug in 1 1 | 3/21/2025 | |
| Zydus Lifesciences Limited | 70771-1673 | ORAL | 250 ug in 1 1 | 9/27/2023 | |
| Arcutis Biotherapeutics, Inc. | 80610-130 | TOPICAL | 3 mg in 1 g | 1/19/2024 | |
| American Health Packaging | 60687-786 | ORAL | 500 ug in 1 1 | 10/30/2023 | |
| Novadoz Pharmaceuticals LLC | 72205-201 | ORAL | 250 ug in 1 1 | 10/28/2019 | |
| Camber Pharmaceuticals, Inc. | 31722-623 | ORAL | 500 ug in 1 1 | 4/28/2023 | |
| AstraZeneca Pharmaceuticals LP | 0310-0088 | ORAL | 250 ug in 1 1 | 3/12/2020 | |
| Novadoz Pharmaceuticals LLC | 72205-200 | ORAL | 500 ug in 1 1 | 10/28/2019 | |
| Camber Pharmaceuticals, Inc. | 31722-676 | ORAL | 250 ug in 1 1 | 4/28/2023 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 7/5/2010 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No HSA approvals found for this drug. | |||||
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| ROFMILAS TABLETS 500MCG | N/A | N/A | N/A | 1/8/2025 |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| No TGA approvals found for this drug. | |||||
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
|---|---|---|---|---|---|
| ROFLUMILAST AUROVITAS 250 MICROGRAMOS COMPRIMIDOS EFG | Aurovitas Spain, S.A.U. | 89830 | COMPRIMIDO | Medicamento Sujeto A Prescripción Médica | Not Commercialized |
| ROFLUMILAST AUROVITAS 500 MICROGRAMOS COMPRIMIDOS EFG | Aurovitas Spain, S.A.U. | 85529 | COMPRIMIDO | Medicamento Sujeto A Prescripción Médica | Commercialized |
| ROFLUMILAST FERRER 250 MICROGRAMOS COMPRIMIDOS EFG | 84761 | COMPRIMIDO | Medicamento Sujeto A Prescripción Médica | Not Commercialized | |
| ROFLUMILAST FERRER 500 MICROGRAMOS COMPRIMIDOS EFG | 84760 | COMPRIMIDO | Medicamento Sujeto A Prescripción Médica | Not Commercialized | |
| ROFLUMILAST ABDI 500 MICROGRAMOS COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | Abdi Farma Unipessoal Lda. | 86766 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Medicamento Sujeto A Prescripción Médica | Not Commercialized |
| ROFLUMILAST ACCORD 500 MICROGRAMOS COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | 84968 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Medicamento Sujeto A Prescripción Médica | Not Commercialized | |
| DAXAS 500 MICROGRAMOS COMPRIMIDOS RECUBIERTOS CON PELICULA | 10636002 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Medicamento Sujeto A Prescripción Médica | Commercialized |
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
|---|---|---|---|---|---|
| No UK EMC drug information found for this drug. | |||||
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