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
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Title | Posted | Study ID | Phase | Status | Sponsor |
---|---|---|---|---|---|
2019/04/16 | Phase 2 | Completed | |||
2018/12/05 | Phase 2 | Completed | |||
2018/08/20 | Phase 2 | Completed | |||
2018/05/22 | Phase 2 | Completed | |||
2018/03/08 | Phase 1 | Completed | |||
2018/02/09 | Phase 2 | Completed | |||
2017/12/22 | N/A | Completed | |||
2017/03/08 | Phase 4 | Completed | |||
2016/07/18 | N/A | UNKNOWN | Millennium Magnetic Technologies, LLC | ||
2016/02/02 | Phase 2 | Terminated |
FDA Drug Approvals
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Health Canada Drug Approvals
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Philippines FDA Drug Approvals
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UK EMC Drug Information
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