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Epoprostenol | CAS No: 35121-78-9 | GMP-certified suppliers
A medication that provides long-term intravenous treatment for severe primary and scleroderma-associated pulmonary hypertension in patients unresponsive to conventional therapies.
Therapeutic categories
Primary indications
- For the long-term intravenous treatment of primary pulmonary hypertension and pulmonary hypertension associated with the scleroderma spectrum of disease in NYHA Class III and Class IV patients who do not respond adequately to conventional therapy
Product Snapshot
- Epoprostenol is supplied as a lyophilized powder for solution intended for intravenous parenteral administration
- It is primarily used for the long-term treatment of primary pulmonary hypertension and pulmonary hypertension related to scleroderma spectrum diseases
- The product is approved for sale in key regulatory markets including the United States and Canada
Clinical Overview
Pharmacodynamically, epoprostenol exerts two main effects: it causes direct vasodilation of pulmonary and systemic arterial vascular beds and inhibits platelet aggregation. In preclinical studies, vasodilation reduces ventricular afterload and improves cardiac output and stroke volume. The effect on heart rate is dose-dependent, with low doses inducing vagally mediated bradycardia and higher doses eliciting reflex tachycardia due to vasodilation-induced hypotension. Other observed effects include bronchodilation and modulation of gastric functions such as acid secretion and emptying. In humans, sensitive and specific assays for in vivo pharmacokinetic profiling are currently unavailable, limiting direct assessment of ADME parameters.
The mechanism of action involves activation of prostacyclin (PGI2) receptors, which are G protein-coupled receptors on platelets and endothelial cells. This activation stimulates adenylate cyclase to increase intracellular cyclic AMP levels, leading to inhibition of platelet activation and aggregation. Cyclic AMP also inhibits calcium mobilization triggered by thromboxane A2, thereby attenuating coagulation. Subsequent activation of protein kinase A phosphorylates myosin light-chain kinase, facilitating smooth muscle relaxation and vasodilation. The physiological roles of PGI2 and thromboxane A2 act in opposition, maintaining vascular homeostasis.
From a safety perspective, epoprostenol's administration requires careful monitoring due to its potent vasodilatory effects, risk of hypotension, and bleeding potential from platelet inhibition. The drug is classified among anticoagulants, antiplatelet agents, prostacyclin analogues, and vasodilators, emphasizing its multifaceted pharmacologic profile.
Notable clinical usage contexts include management of severe pulmonary hypertension unresponsive to standard therapy, often necessitating continuous intravenous infusion due to epoprostenol’s short half-life. The sodium salt form is commonly utilized for therapeutic applications.
For API sourcing, stringent quality control is essential given the compound’s sensitivity and instability. Maintaining cold chain logistics and verifying compliance with pharmacopeial standards ensure appropriate purity, potency, and safety profiles required for pharmaceutical manufacturing and regulatory approval globally.
Identification & chemistry
| Generic name | Epoprostenol |
|---|---|
| Molecule type | Small molecule |
| CAS | 35121-78-9 |
| UNII | DCR9Z582X0 |
| DrugBank ID | DB01240 |
Pharmacology
| Summary | Epoprostenol is a prostacyclin analog that primarily targets prostacyclin receptors to induce vasodilation and inhibit platelet aggregation. Its mechanism involves activation of adenylate cyclase, increasing cyclic AMP levels, which leads to smooth muscle relaxation and reduced platelet activation. These pharmacodynamic effects contribute to decreased vascular resistance and improved hemodynamics in pulmonary hypertension. |
|---|---|
| Mechanism of action | Prostaglandins are present in most body tissues and fluids and mediate many biological functions. Epoprostenol (PGI2) is a member of the family of prostaglandins that is derived from arachidonic acid. The major pharmacological actions of epoprostenol is ultimately inhibition of platelet aggregation. Prostacycline (PGI2) from endothelial cells activate G protein-coupled receptors on platelets and endothelial cells. This activation causes adenylate cyclase to produce cyclic AMP which inhibits further platelet activation and activates protein kinase A. Cyclic AMP also prevents coagulation by preventing an increase in intracellular calcium from thromboxane A2 binding. PKA then continues the cascade by phosphorylating and inhibiting myosin light-chain kinase which leads to smooth muscle relaxation and vasodilation. Notably, PGI2 and TXA2 work as physiological antagonists. |
| Pharmacodynamics | Epoprostenol has two major pharmacological actions: (1) direct vasodilation of pulmonary and systemic arterial vascular beds, and (2) inhibition of platelet aggregation. In animals, the vasodilatory effects reduce right and left ventricular afterload and increase cardiac output and stroke volume. The effect of epoprostenol on heart rate in animals varies with dose. At low doses, there is vagally mediated brudycardia, but at higher doses, epoprostenol causes reflex tachycardia in response to direct vasodilation and hypotension. No major effects on cardiac conduction have been observed. Additional pharmacologic effects of epoprostenol in animals include bronchodilation, inhibition of gastric acid secretion, and decreased gastric emptying. No available chemical assay is sufficiently sensitive and specific to assess the in vivo human pharmacokinetics of epoprostenol. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Prostacyclin synthase | Humans | inducer |
| P2Y purinoceptor 12 | Humans | agonist |
| Prostacyclin receptor | Humans | agonist |
ADME / PK
| Half-life | The in vitro half-life of epoprostenol in human blood at 37°C and pH 7.4 is approximately 6 minutes; the in vivo half-life of epoprostenol in humans is therefore expected to be no greater than 6 minutes. |
|---|---|
| Metabolism | Epoprostenol is metabolized to 2 primary metabolites: 6-keto-PGF1α (formed by spontaneous degradation) and 6,15-diketo-13,14-dihydro-PGF1α (enzymatically formed), both of which have pharmacological activity orders of magnitude less than epoprostenol in animal test systems. Fourteen additional minor metabolites have been isolated from urine, indicating that epoprostenol is extensively metabolized in humans. |
| Route of elimination | Epoprostenol is metabolized to 2 primary metabolites: 6-keto-PGF1α (formed by spontaneous degradation) and 6,15-diketo-13,14-dihydro-PGF1α (enzymatically formed), both of which have pharmacological activity orders of magnitude less than epoprostenol in animal test systems. Fourteen additional minor metabolites have been isolated from urine, indicating that epoprostenol is extensively metabolized in humans. |
| Volume of distribution | * 357 mL/kg |
Formulation & handling
- Epoprostenol is a small molecule API supplied as a powder for parenteral and intravenous administration, requiring reconstitution prior to use.
- The API exhibits low water solubility, necessitating careful consideration of solvent systems and formulation for injectable solutions.
- Concurrent use with herbal or dietary supplements that have anticoagulant or antiplatelet effects should be avoided due to potential interaction risks.
Regulatory status
| Lifecycle | The API is currently protected by patents in the United States expiring in early 2027, with marketed products available in both the US and Canada. Following patent expiry, the API is expected to enter a more mature phase with potential for generic competition. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Epoprostenol is represented by multiple packagers predominantly active in the Canadian and US markets, indicating a focus on North American distribution. The branded products exist primarily under similar names, reflecting a consolidated product identity within these regions. Existing patents are set to expire in early 2027, suggesting that generic competition could emerge in the near term. |
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Safety
| Toxicity | Symptoms of overdose are extensions of its dose-limiting pharmacologic effects and include flushing, headache, hypotension, nausea, vomiting, and diarrhea. Most events were self-limiting and resolved with reduction or withholding of epoprostenol. Single intravenous doses at 10 and 50 mg/kg (2703 and 27,027 times the recommended acute phase human dose based on body surface area) were lethal to mice and rats, respectively. Symptoms of acute toxicity were hypoactivity, ataxia, loss of righting reflex, deep slow breathing, and hypothermia. |
|---|
- Overdose symptoms may include flushing, headache, hypotension, nausea, vomiting, and diarrhea
- Effects are dose-dependent and potentially reversible upon dose adjustment
- Acute toxicity observed in animal studies includes hypoactivity, ataxia, respiratory depression, and hypothermia, with lethality at high intravenous doses
Epoprostenol is a type of Vasodilators
Vasodilators are a crucial subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) that play a significant role in the management of various cardiovascular conditions. These medications work by widening the blood vessels, promoting increased blood flow and reducing peripheral resistance.
Vasodilators are commonly prescribed to treat hypertension (high blood pressure), angina (chest pain), and heart failure. They are designed to relax and dilate the smooth muscle cells in the walls of blood vessels, leading to improved circulation and reduced strain on the heart.
One widely used class of vasodilators is calcium channel blockers, which prevent calcium from entering the muscle cells of blood vessels. This action inhibits muscle contraction, resulting in widened arteries and enhanced blood flow. Another class is nitric oxide (NO) donors, which release NO, a potent vasodilator, to promote relaxation of vascular smooth muscles.
The therapeutic benefits of vasodilators extend beyond cardiovascular disorders. Some vasodilators, such as minoxidil, have been repurposed for treating male pattern baldness. These medications stimulate hair growth by dilating blood vessels around hair follicles, enhancing nutrient and oxygen delivery.
As with any pharmaceutical API, vasodilators must meet strict quality standards and regulatory guidelines to ensure safety and efficacy. Manufacturers employ sophisticated production processes and stringent quality control measures to guarantee the purity, potency, and stability of these APIs.
In conclusion, vasodilators are a vital subcategory of pharmaceutical APIs used to manage cardiovascular conditions. By expanding blood vessels and enhancing blood flow, vasodilators contribute to improved patient outcomes and play a critical role in the treatment of hypertension, angina, heart failure, and even hair loss.
Epoprostenol (Vasodilators), classified under Antihypertensive agents
Antihypertensive agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat high blood pressure, also known as hypertension. These medications are designed to lower blood pressure and reduce the risk of associated cardiovascular complications.
Antihypertensive agents function by targeting various mechanisms involved in blood pressure regulation. Some common classes of antihypertensive agents include angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor blockers (ARBs), beta-blockers, calcium channel blockers (CCBs), and diuretics.
ACE inhibitors work by inhibiting the enzyme responsible for converting angiotensin I to angiotensin II, a hormone that constricts blood vessels. ARBs, on the other hand, block the receptors to which angiotensin II binds, thereby preventing its vasoconstrictive effects.
Beta-blockers reduce blood pressure by blocking the effects of adrenaline and noradrenaline, which are responsible for increasing heart rate and constricting blood vessels. CCBs inhibit calcium from entering the smooth muscles of blood vessels, resulting in relaxation and vasodilation. Diuretics promote the elimination of excess fluid and sodium from the body, reducing blood volume and thereby lowering blood pressure.
Antihypertensive agents are typically prescribed based on the individual patient's condition and specific needs. They can be used alone or in combination to achieve optimal blood pressure control. It is important to note that antihypertensive agents should be taken regularly as prescribed by a healthcare professional and may require periodic monitoring to ensure their effectiveness and manage any potential side effects.
In summary, antihypertensive agents play a vital role in the management of hypertension by targeting various mechanisms involved in blood pressure regulation. These medications offer significant benefits in reducing the risk of cardiovascular complications associated with high blood pressure.
Epoprostenol API manufacturers & distributors
Compare qualified Epoprostenol API suppliers worldwide. We currently have 6 companies offering Epoprostenol API, with manufacturing taking place in 5 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 |
|---|---|---|---|---|---|
| Chirogate International | Producer | Taiwan | Taiwan | CoA | 17 products |
| Flavine | Distributor | Germany | Unknown | CoA | 83 products |
| MSN Labs. | Producer | India | India | CoA, USDMF | 119 products |
| Pharmacia & Upjohn | Producer | United States | United States | CoA, JDMF, USDMF | 30 products |
| Sun Pharma | Producer | India | India | CoA, USDMF | 219 products |
| Yonsung Fine Chem. | Producer | South Korea | South Korea | CoA, JDMF | 13 products |
When sending a request, specify which Epoprostenol 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 Epoprostenol 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.
