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

Published: Jul 31, 2025

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]

Continue reading the full research report

Clinical Trials

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Title	Posted	Study ID	Phase	Status	Sponsor
Safety and Efficacy of ARQ-151 Cream in Adolescents and Adults With Atopic Dermatitis	2019/04/16	NCT03916081	Phase 2	Completed	Arcutis Biotherapeutics, Inc.
Long-Term Safety of ARQ-151 Cream in Adult Subjects With Chronic Plaque Psoriasis	2018/12/05	NCT03764475	Phase 2	Completed	Arcutis Biotherapeutics, Inc.
The Safety, Efficacy and Pharmacokinetics of ARQ-151 Cream in Subjects With Chronic Plaque Psoriasis	2018/08/20	NCT03638258	Phase 2	Completed	Arcutis Biotherapeutics, Inc.
Trial of Roflumilast in Asthma Management (TRIM)	2018/05/22	NCT03532490	Phase 2	Completed	Johns Hopkins University
Study of Roflumilast in Combination With Standard Chemotherapy for High-risk Diffuse Large B-cell Lymphoma	2018/03/08	NCT03458546	Phase 1	Completed	The University of Texas Health Science Center at San Antonio
Roflumilast in Non-CF Bronchiectasis Study	2018/02/09	NCT03428334	Phase 2	Completed	The University of Hong Kong
Long-term Observational Study of the Safety of Roflumilast	2017/12/22	NCT03381573	N/A	Completed	AstraZeneca
The Effectiveness of Roflumilast in Improving Mucociliary Clearance in Patients With COPD and Chronic Bronchitis	2017/03/08	NCT03073798	Phase 4	Completed	Johns Hopkins University
Pre-Clinical (Alzheimers) Diagnosis PCD = Optimum Outcomes OO	2016/07/18	NCT02835716	N/A	UNKNOWN	Millennium Magnetic Technologies, LLC
A Multicenter Randomized Double-blind Clinical Study Evaluated the Safety, Pharmacokinetic and Pharmacodynamic Characteristics of Roflumilast in COPD Patients	2016/02/02	NCT02671942	Phase 2	Terminated	Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

FDA Drug Approvals

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Approved Product	Manufacturer	NDC Code	Route	Strength	Effective Date
No FDA approvals found for this drug.

EMA Drug Approvals

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Approved Product	Authorization Holder	Status	Issued Date
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HSA Drug Approvals

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NMPA Drug Approvals

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PPB Drug Approvals

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TGA Drug Approvals

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Health Canada Drug Approvals

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CIMA AEMPS Drug Approvals

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Approved Product	Company	Registration Number	Pharmaceutical Form	Prescription Type	Status
No CIMA AEMPS (Spain) approvals found for this drug.

Philippines FDA Drug Approvals

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Approved Product	Company	License Number	Dosage Form	Strength	Approval Date
No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

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Approved Product	Company	License Number	Dosage Form	Strength	Approval Date
No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

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No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

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Medicine Name	MA Holder	MA Number	Pharmaceutical Form	Active Ingredient	Authorization Date
No UK EMC drug information found for this drug.

Related News

FDA Approves Arcutis' Zoryve (Roflumilast) Cream 0.15% for Atopic Dermatitis in Children and Adults

a year ago

• The FDA has approved Arcutis Biotherapeutics' Zoryve (roflumilast) cream 0.15% for treating mild to moderate atopic dermatitis in patients aged six and older. • Clinical trials demonstrated that Zoryve significantly improved atopic dermatitis symptoms, with approximately 40% of patients achieving clear or almost clear skin at Week 4. • Zoryve showed rapid itch reduction within 24 hours of application and was well-tolerated, offering a steroid-free alternative for long-term disease control. • Arcutis plans to launch Zoryve cream 0.15% by the end of July, ensuring patient access through various support programs and pharmacy channels.

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