Roflumilast Powder is a phosphodiesterase-4 (PDE4) inhibitor, mainly used for severe chronic obstructive pulmonary disease and cough with excessive mucus bronchitis, wheezing bronchitis, bronchial asthma, acute and chronic bronchitis with abnormal respiratory secretions, and airbag inflammation. Traditional drugs for the treatment of COPD mainly include bronchodilators and inhaled glucocorticoids. Still, their effects primarily focus on relieving symptoms and improving lung function while controlling chronic airway inflammation is relatively limited. As a systemic anti-inflammatory drug, roflumilast fills this gap and provides a new option for the comprehensive treatment of COPD. Its treatment goal is to reduce the frequency and severity of acute exacerbations of COPD rather than for immediate relief of symptoms. Compared with traditional COPD treatment drugs (such as LABA, LAMA and ICS), daxas emphasizes systemic anti-inflammatory effects, can effectively reduce the frequency of acute exacerbations, and has unique efficacy for patients with chronic bronchitis phenotype. The anti-inflammatory mechanism of action of daxas makes it potentially suitable for other inflammatory diseases such as asthma, idiopathic pulmonary fibrosis (IPF) and inflammatory bowel disease (IBD).
Shaanxi Medibridge Biotech Co., Ltd. focuses on the supply of pharmaceutical raw materials and research-use compounds. We support customers with stable quality, clear specification communication, flexible packaging options, and document-related support for different project stages.
COA
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Product Name |
CAS Number |
Batch Number |
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Roflumilast Powder |
162401-32-3 |
MB2607150128 |
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Manufacturer Date |
Analysis Date |
Expiry Date |
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2026/7/15 |
2026/7/16 |
2028/7/15 |
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Sample Qty Base |
Packing |
Test Method |
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100KGS |
25KG/drum |
HPLC |
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Item |
Standard |
Results |
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Appearance |
White to off white powder |
Complies |
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Identification |
By IR |
Complies |
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Identification |
By HPLC |
Complies |
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Solubility |
DMSO: soluble20mg/mL, clear |
Complies |
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Melting point |
158°C |
94-95°C |
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Residual solvents |
Dichloromethane: ≤ 100ppm |
Complies |
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Residual solvents |
Hexame≤ 200 ppm |
Not detectable |
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Residual solvents |
Ethyl acetate≤500 ppm |
Complies |
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Residual solvents |
Terahy drofuran≤ 100 ppm |
Not detectable |
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Related substances |
Impurity A: ≤ 0.10% |
Complies |
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Related substances |
Impurity B: ≤ 0.10% |
Complies |
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Related substances |
Any other single impurity≤ 0.10% |
Not detectable |
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Related substances |
Total impuritied≤ 0.50% |
99.34% |
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Assay |
98.0-102.0% |
99.45% |
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Conclusion |
The batch conforms to the IN-HOUSE standard |
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PDE4 Inhibition and cAMP Signaling
Phosphodiesterase 4 (PDE4) hydrolyzes intracellular cyclic adenosine monophosphate (cAMP). Roflumilast and its active metabolite inhibit PDE4, allowing cAMP to accumulate and influencing signaling and function in inflammation-related cells. However, the complete mechanisms connecting these molecular effects to clinical outcomes remain incompletely defined.
Inflammatory and Immune Cell Research
Roflumilast's experimental evidence extends beyond changes in a single inflammatory mediator. An early primary study investigated multiple human leukocyte functions, including leukotriene B₄ and reactive oxygen species production in neutrophils, TNF-α release from monocytes and macrophages, and proliferation and cytokine release in CD4⁺ T cells.
In that study, half-maximal inhibitory concentrations for the measured cellular responses were approximately 2–21 nM for roflumilast and 3–40 nM for roflumilast N-oxide. These values apply to the specific cells, stimuli, and assay conditions investigated; they should not be treated as universal working concentrations.
NF-κB and MAPK: Interpreting Downstream Changes
In an experimental study using LPS-stimulated RAW264.7 murine macrophages, roflumilast reduced NO production and TNF-α and IL-1β expression. These effects were accompanied by reduced IκBα phosphorylation and degradation, decreased NF-κB DNA-binding activity, and inhibition of p38 and JNK phosphorylation.
These findings support modulation of inflammatory signaling networks. However, they do not establish roflumilast as a direct inhibitor of NF-κB, p38, or JNK. The observed changes may represent downstream consequences of altered PDE4–cAMP signaling.
A stronger mechanistic study should connect PDE4 inhibition, intracellular cAMP changes, signaling time courses, and functional outcomes. Knockdown, knockout, or complementary pathway interventions can help establish dependence on the proposed mechanism. A change in a single Western blot band is insufficient to demonstrate the complete signaling pathway.
Translating Cellular Findings to Tissue Responses
Airway inflammation is one of roflumilast's most established research areas. Beyond isolated cells, investigators have used human lung tissue to examine its effects on LPS-induced TNF-α and chemokine production, providing evidence at the tissue level.
Relevant research questions include:
- Whether changes in inflammatory cell recruitment correspond to altered cAMP signaling;
- How epithelial cells and immune cells interact during inflammatory responses;
- Whether responses differ across inflammatory stimuli;
- Whether molecular changes translate into improvements in tissue or whole-organ function.
Skin Research and Local Delivery
Roflumilast has formulation-specific clinical evidence in dermatology. The DERMIS-1 and DERMIS-2 trials evaluated 0.3% roflumilast cream in plaque psoriasis, while INTEGUMENT-1 and INTEGUMENT-2 evaluated 0.15% cream in atopic dermatitis. These findings apply to the tested formulations and study populations; they cannot be directly extrapolated to unformulated powder or an arbitrary topical preparation.
For raw-material and formulation research, the central challenge is to evaluate local concentration, skin retention, and systemic exposure together.
Increasing solubility does not necessarily increase the effective drug concentration within skin. Release from the formulation, partitioning into skin layers, and tissue binding also influence delivery performance.
Application Fields and Formulation Development
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Application Direction |
Primary Indications |
Dosage Forms & Routes of Administration |
Therapeutic Advantages |
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Respiratory System |
Chronic Obstructive Pulmonary Disease (COPD) |
Oral tablets |
Reduces the frequency of exacerbations in severe COPD patients and improves pulmonary function. |
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Dermatology |
Psoriasis, Atopic Dermatitis (Eczema) |
Topical creams / foams |
Steroid-free profile, making it suitable for long-term use and sensitive areas (such as the face and intertriginous regions). |
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Other Research Explorations |
Alopecia areata, asthma, arthritis, neuroinflammation models |
In vitro and in vivo research reagents |
Investigating the role of the PDE4 pathway in neuroprotection, anti-fibrosis, and autoimmune disease mechanisms. |
FAQ
How safe is roflumilast?
Roflumilast is generally safe and effective when used as prescribed, though its safety profile depends heavily on whether you take it as an oral pill or use it as a topical cream or foam.
Is roflumilast good for psoriasis?
Yes, roflumilast is an effective and safe treatment for plaque psoriasis.
What is roflumilast used for in dermatology?
Roflumilast is a selective, non-steroidal phosphodiesterase-4 (PDE4) inhibitor used in dermatology to suppress inflammatory pathways in chronic skin conditions.
Is roflumilast used for eczema?
Yes, topical roflumilast (brand name Zoryve) is used to treat mild to moderate eczema, specifically the most common form called atopic dermatitis.
If you are looking for a high-quality Roflumilast Powder manufacturer with whom you can establish a long-term, stable partnership, then Shaanxi Medibridge Biotech Co., Ltd. would be your best business partner. Don't hesitate to contact us at hi@medibridgeapi.com.
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