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Specifications
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Appearance: |
White or off-white powder |
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Purity: |
99.0% min |
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Assay: |
98-102% |
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Melting point: |
153-158℃ |
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Water: |
0.5% max |
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Single impurity: |
0.3% max |
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Total impurities: |
1.0% max |
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Residue on ignition: |
0.5% max |
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THF: |
0.072% max |
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Ethyl acetate: |
0.5% max |
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Methanol: |
0.3% max |
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Ethanol: |
0.5% max |
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Toluene: |
0.089% max |
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DMF: |
0.088% max |
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Identification: |
Complies |
Transport Information
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Parameter |
Specification |
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UN Number |
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Class |
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Packing Group |
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H.S. Code |
2933399099306 |
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Stability & Reactivity |
The product is chemically stable under standard ambient conditions. |
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Storage |
-20℃ |
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Condition to Avoid |
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Package |
Overview
Roflumilast丨CAS 162401-32-3 is a highly selective inhibitor of phosphodiesterase-4 (PDE4), an enzyme that breaks down cyclic adenosine monophosphate (cAMP) in inflammatory cells. By elevating intracellular cAMP levels, roflumilast reduces inflammation-particularly in the airways-and is approved for the treatment of chronic obstructive pulmonary disease (COPD).
As an oral anti-inflammatory drug, roflumilast provides a novel, non-steroidal treatment option that complements bronchodilators and other COPD medications.
Applications
1. Chronic Obstructive Pulmonary Disease (COPD)
Primary indication for reducing the risk of COPD exacerbations in patients with:
Severe COPD (FEV1 < 50%)
Chronic bronchitis phenotype
History of frequent exacerbations
Mechanism: PDE4 inhibition leads to increased cAMP in neutrophils, eosinophils, macrophages, and T cells, suppressing pro-inflammatory cytokine release and reducing airway inflammation.
2. Asthma (Investigational)
Studied for use in severe asthma, especially phenotypes with eosinophilic or neutrophilic inflammation.
Shows promise in combination therapy with corticosteroids.
3. Other Inflammatory Disorders (Preclinical/Research)
Being investigated for potential roles in:
Psoriasis
Pulmonary fibrosis
Inflammatory bowel disease (IBD)
Neuroinflammatory conditions such as multiple sclerosis or Alzheimer's disease
Benefits
1. Selective PDE4 Inhibition
Roflumilast丨CAS 162401-32-3 provides targeted anti-inflammatory activity in the lungs without affecting PDE1–3 or PDE5 pathways.
Reduces airway neutrophilic inflammation, complementing bronchodilators.
2. Oral Once-Daily Dosing
Convenient oral tablet, usually 500 µg once daily, improves patient adherence compared to inhaled therapies.
3. Steroid-Sparing Potential
Non-corticosteroid anti-inflammatory action reduces reliance on inhaled or systemic corticosteroids, which have more side effects.
4. Exacerbation Risk Reduction
Demonstrated efficacy in reducing moderate-to-severe COPD exacerbations, especially in high-risk patients with chronic bronchitis.
Pharmacokinetics
High oral bioavailability (~80%)
Half-life: ~17 hours (supports once-daily dosing)
Active metabolite: Roflumilast N-oxide (responsible for ~90% of PDE4 inhibition)
Metabolized by CYP3A4 and CYP1A2
Summary
Roflumilast丨CAS 162401-32-3 is a selective PDE4 inhibitor used primarily to prevent COPD exacerbations in patients with chronic bronchitis. With its non-steroidal, anti-inflammatory mechanism, it offers a unique and effective therapeutic strategy for severe, frequent-exacerbator COPD patients. Ongoing research into asthma and inflammatory diseases may expand its clinical utility.
