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Roflumilast | CAS No: 162401-32-3 | GMP-certified suppliers
A medication that supports severe COPD management by reducing exacerbation risk and treats plaque psoriasis and seborrheic dermatitis across key dermatologic patient populations.
Therapeutic categories
Primary indications
- 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 cream roflumilast is indicated to treat plaque psoriasis, including intertriginous areas, in patients 12 years of age and older, while topical foam roflumilast is indicated to treat seborrheic dermatitis in adult and pediatric patients 9 years of age and older
Product Snapshot
- Roflumilast is available as an oral small‑molecule tablet and as topical cream or foam formulations
- It is used for COPD exacerbation risk reduction as well as plaque psoriasis and seborrheic dermatitis
- It holds approved status in major regulated markets including the US, EU, and Canada
Clinical Overview
Roflumilast is a benzamide derivative that selectively inhibits PDE4, a major cAMP‑metabolizing enzyme expressed in immune, pro‑inflammatory, epithelial, and smooth muscle cells. By inhibiting PDE4, roflumilast and its active metabolite, roflumilast N‑oxide, increase intracellular cAMP levels. Although this activity is linked to anti‑inflammatory effects, the precise therapeutic mechanism in COPD, psoriasis, or seborrheic dermatitis remains incompletely defined. Both parent drug and metabolite show high selectivity for PDE4 with minimal activity against other PDE isoforms.
Oral administration results in formation of the N‑oxide metabolite, which contributes substantially to systemic activity. Roflumilast is metabolized primarily via CYP1A2 and CYP3A pathways, with subsequent renal elimination of metabolites. Key pharmacokinetic parameters, including absorption rate and half‑life, vary across formulations, and the topical products are designed to limit systemic exposure.
Safety considerations include gastrointestinal effects, weight decrease, and neuropsychiatric symptoms reported with oral therapy. Topical products generally demonstrate lower systemic involvement, though local reactions can occur. Roflumilast interacts with strong CYP3A or CYP1A2 modulators, which may alter exposure to the oral formulation.
Brand usage varies by region, with multiple oral and topical products approved in major regulatory markets since 2010.
For API sourcing, procurement teams should confirm compliance with regional GMP requirements, control of enantiomeric and impurity profiles, and robust documentation of residual solvent and polymorph characteristics to support formulation development and regulatory submissions.
Identification & chemistry
| Generic name | Roflumilast |
|---|---|
| Molecule type | Small molecule |
| CAS | 162401-32-3 |
| UNII | 0P6C6ZOP5U |
| DrugBank ID | DB01656 |
Pharmacology
| Summary | Roflumilast and its active metabolite inhibit PDE4, leading to increased intracellular cAMP and modulation of inflammatory signaling pathways. The therapeutic effect is associated with selective PDE4 blockade, though the precise mechanisms underlying clinical benefit are not fully defined. |
|---|---|
| Mechanism of action | Roflumilast and its active metabolite (roflumilast N-oxide) are inhibitors of PDE4. Roflumilast and roflumilast N-oxide inhibition of PDE4 (a major cyclic 3′,5′-adenosine monophosphate (cyclic AMP) metabolizing enzyme) activity leads to accumulation of intracellular cyclic AMP. The specific mechanism(s) by which roflumilast exerts its therapeutic action is not well defined. |
| Pharmacodynamics | Roflumilast and its active metabolite, roflumilast N-oxide, increase cyclic adenosine-3′, 5′-monophosphate (cAMP) in affected cells by inhibiting PDE4. They are highly selective for PDE4 and are effectively inactive against PDEs 1, 2, 3, 5, and 7. |
Targets
| Target | Organism | Actions |
|---|---|---|
| cAMP-specific 3',5'-cyclic phosphodiesterase 4 (PDE4) | Humans | inhibitor |
ADME / PK
| Absorption | After a 500mcg dose, the bioavailability of roflumilast is about 80%.In the fasted state, maximum plasma concentrations are reached in 0.5 to 2 hours, while in the fed state, Cmax is reduced by 40%, Tmax is increased by one hour, and total absorption is unchanged. Applied topically, the mean systemic exposure for roflumilast and its N-oxide metabolite in adults was 72.7 ± 53.1 and 628 ± 648 h∙ng/mL, respectively.The mean systemic exposure for roflumilast and its N-oxide metabolite in adolescents was 25.1 ± 24.0 and 140 ± 179 h∙ng/mL, respectively. |
|---|---|
| Half-life | Following oral administration, the plasma half-lives of roflumilast and roflumilast N-oxide are 17 hours and 30 hours, respectively. |
| Protein binding | Plasma protein binding of roflumilast and its N-oxide metabolite is approximately 99% and 97%, respectively. |
| Metabolism | Roflumilast is metabolized to roflumilast N-oxide, the active metabolite of roflumilast in humans, by CYP3A4 and CYP1A2.The N-oxide metabolite is less potent than its parent drug in regards to PDE4 inhibition, but its plasma AUC is approximately 10-fold greater. |
| Route of elimination | Roflumilast is excreted 70% in the urine as roflumilast N-oxide. |
| Volume of distribution | Following a single oral dose of 500 mcg, the volume of distribution of roflumilast is approximately 2.9 L/kg. |
| Clearance | Plasma clearance of roflumilast following short-term intravenous infusion is approximately 9.6 L/h. |
Formulation & handling
- Oral formulations require solubility‑enhancing approaches due to very low aqueous solubility and moderate lipophilicity.
- High‑fat meals may reduce and delay peak levels, but overall exposure is unchanged, so food effects are not typically formulation‑limiting.
- Topical products should account for the lipophilic small‑molecule profile to ensure adequate dermal penetration and stable dispersion in semi‑solid bases.
Regulatory status
| Lifecycle | Most U.S. patents have recently expired or will conclude in early 2024, indicating the API is entering a late‑lifecycle phase. With established presence in the US, EU, and Canada, the markets are mature and positioned for expanding generic competition. |
|---|
| Markets | US, EU, Canada |
|---|
Supply Chain
| Supply chain summary | Roflumilast is supplied by a single originator group marketing the product under the Daliresp and Daxas brands across the US, EU, and Canada, indicating a consolidated source of branded material with broad international distribution. With multiple key US patents already expired or expiring in 2023–2024, the molecule is positioned for existing or imminent generic entry. This shift suggests the manufacturing landscape may transition from originator‑led supply to a more diversified set of API producers. |
|---|
Safety
| Toxicity | There are no data regarding overdosage with orally administered roflumilast. Phase I studies in which roflumilast was administered at single doses up to 5000 mcg showed an increase in the incidence of headache, gastrointestinal disorders, dizziness, palpitations, lightheadedness, clamminess, and arterial hypotension.In the event of an overdose, administer support medical care as soon as possible. Hemodialysis is unlikely to be of benefit given the extensive protein binding of roflumilast. |
|---|
- High-dose exposure has been associated with increased incidence of headache, gastrointestinal disturbances, dizziness, palpitations, vasomotor symptoms, and arterial hypotension in Phase I studies up to 5000 mcg
- Extensive plasma protein binding suggests limited removal by hemodialysis in overdose scenarios
- Monitor for autonomic or cardiovascular perturbations when handling concentrated research materials due to documented dose-related systemic effects
Roflumilast is a type of Phosphodiesterase-4 Inhibitors
Phosphodiesterase-4 (PDE-4) inhibitors belong to the subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that are widely used in the treatment of various inflammatory and respiratory conditions. These inhibitors work by blocking the enzyme phosphodiesterase-4, which is responsible for breaking down cyclic adenosine monophosphate (cAMP) in cells. By inhibiting PDE-4, the levels of cAMP are increased, leading to reduced inflammation and bronchoconstriction.
PDE-4 inhibitors have shown significant therapeutic potential in the management of chronic obstructive pulmonary disease (COPD), asthma, and psoriasis. The most commonly prescribed PDE-4 inhibitor is roflumilast, which is available in oral tablet form. Roflumilast specifically targets lung tissue and effectively reduces airway inflammation and hyperresponsiveness, improving lung function and reducing exacerbations in COPD patients.
Apart from their anti-inflammatory properties, PDE-4 inhibitors have also shown promise in the treatment of other conditions such as depression, cognitive disorders, and autoimmune diseases. Ongoing research and clinical trials aim to explore the full potential of PDE-4 inhibitors in these therapeutic areas.
As with any medication, PDE-4 inhibitors may have certain side effects, including gastrointestinal disturbances (such as diarrhea and nausea), weight loss, and psychiatric effects. Therefore, careful consideration of the risks and benefits is essential before initiating treatment with PDE-4 inhibitors.
In conclusion, PDE-4 inhibitors are a subcategory of pharmaceutical APIs that hold great potential in the treatment of inflammatory and respiratory conditions. With ongoing research and development, these inhibitors may find expanded applications in various therapeutic areas, benefiting patients worldwide.
Roflumilast (Phosphodiesterase-4 Inhibitors), classified under Respiratory Tract Agents
Respiratory Tract Agents are a vital category of pharmaceutical APIs (Active Pharmaceutical Ingredients) designed to treat respiratory conditions and diseases. These agents are specifically formulated to target the respiratory system, which includes the lungs, airways, and nasal passages. They play a crucial role in managing various respiratory disorders, such as asthma, chronic obstructive pulmonary disease (COPD), and allergic rhinitis.
Respiratory Tract Agents encompass a wide range of medications, including bronchodilators, corticosteroids, antihistamines, and mucolytics. Bronchodilators are commonly used to relieve airway constriction and facilitate smooth breathing by relaxing the muscles in the airways. Corticosteroids help reduce inflammation in the respiratory system, alleviating symptoms and preventing exacerbations. Antihistamines work by blocking histamine receptors, thus mitigating allergic reactions that often impact the respiratory tract. Mucolytics aid in loosening and thinning mucus, making it easier to expel from the airways.
These APIs are developed through rigorous research and development processes, ensuring their efficacy, safety, and compliance with regulatory standards. Pharmaceutical manufacturers rely on advanced technologies and stringent quality control measures to produce high-quality Respiratory Tract Agents. These APIs are subsequently incorporated into various dosage forms, including inhalers, nasal sprays, nebulizers, and oral medications.
Respiratory Tract Agents are essential in the management of respiratory conditions, providing relief from symptoms, improving lung function, and enhancing the overall quality of life for patients. They are prescribed by healthcare professionals and often used in combination therapies to achieve optimal results. As respiratory disorders continue to affect a significant portion of the global population, the development and availability of effective Respiratory Tract Agents play a vital role in addressing these health challenges and improving patient outcomes.
Roflumilast API manufacturers & distributors
Compare qualified Roflumilast API suppliers worldwide. We currently have 8 companies offering Roflumilast API, with manufacturing taking place in 3 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| ALP PHARM | Producer | China | China | CoA, USDMF | 33 products |
| Apino Pharma Co., Ltd. | Producer | China | China | cDMF, CoA, GMP, MSDS | 229 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Hetero Drugs | Producer | India | India | CoA, USDMF | 98 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| MSN Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 119 products |
| Mylan | Producer | India | India | CoA, USDMF | 201 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
When sending a request, specify which Roflumilast API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Roflumilast API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
Frequently asked questions about Roflumilast API
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Technical
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Regulatory
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