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Limaprost | CAS No: 74397-12-9 | GMP-certified suppliers
A medication that improves ischemic symptoms related to thromboangiitis obliterans and enhances pain, numbness, and gait ability in acquired lumbar spinal canal stenosis.
Therapeutic categories
Primary indications
- Limaprost is used for the improvement of various ischemic symptoms such as ulcer, pain and feeling of coldness associated with thromboangiitis obliterans as well as improvement of subjective symptoms (pain and numbness of lower legs) and gait ability associated with acquired lumbar spinal canal stenosis (in patients with bilateral intermittent claudication showing normal SLR test result)
Product Snapshot
- Limaprost is available as an oral small molecule tablet
- The compound is primarily indicated for the management of ischemic symptoms related to thromboangiitis obliterans and lumbar spinal canal stenosis
- It currently holds investigational status and lacks approval from major regulatory agencies
Clinical Overview
Clinically, limaprost is indicated for the treatment of ischemic symptoms such as ulcers, pain, and coldness associated with thromboangiitis obliterans. It also addresses subjective symptoms including pain, numbness, and impaired gait in patients with acquired lumbar spinal canal stenosis, particularly in cases exhibiting bilateral intermittent claudication and normal straight leg raise test results.
Pharmacodynamically, limaprost improves peripheral circulation by dilating vascular smooth muscle and exerts antithrombotic effects by modulating platelet aggregation. It may also enhance nerve function by improving blood flow within nerve tissue, as observed in conditions like cervical spondylosis, although clinical efficacy in this indication has not been conclusively demonstrated.
Absorption, distribution, metabolism, and excretion (ADME) parameters specific to limaprost are not extensively documented in publicly available sources. Safety and toxicity considerations highlight the need for careful monitoring for adverse effects consistent with prostaglandin analogs, such as gastrointestinal disturbances and hypotension, but comprehensive toxicity profiles remain limited.
Limaprost has been marketed under trade names such as Opalmon® by Ono Pharmaceutical and Prorenal® by Dainippon Sumitomo Pharma. While approved for certain ischemic and neurological conditions primarily in Japan, some investigational uses, including treatment for carpal tunnel syndrome and cervical spondylosis, were discontinued due to insufficient clinical efficacy.
For API sourcing, it is advisable to verify the chemical identity and purity of limaprost according to pharmacopeial standards and regulatory requirements. Sourcing should ensure robust characterization of the fatty acid analog structure and consistent quality to support formulation and regulatory compliance globally.
Identification & chemistry
| Generic name | Limaprost |
|---|---|
| Molecule type | Small molecule |
| CAS | 74397-12-9 |
| UNII | L02U804092 |
| DrugBank ID | DB09211 |
Pharmacology
| Summary | Limaprost is a prostaglandin E1 analog that acts as an agonist at prostaglandin E2 receptors, primarily stimulating the EP2 subtype to activate adenylate cyclase and induce smooth muscle relaxation. This vasodilatory effect enhances blood flow to peripheral tissues, improving ischemic symptoms. Its pharmacodynamic action targets multiple EP receptor subtypes to modulate vascular tone and microcirculation. |
|---|---|
| Mechanism of action | As a prostglandin E1 analog, limaprost acts as an agonist at prostraglandin E2 receptors. It likely stimulates the adenylate cyclase coupled E2 subtype of these receptors to produce smooth muscle relaxation . |
| Pharmacodynamics | Limaprost produces vasodilation to improve blood flow to the extremities and increase cutaneous temperature. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Prostaglandin E2 receptor EP2 subtype | Humans | agonist |
| Prostaglandin E2 receptor EP1 subtype | Humans | agonist |
| Prostaglandin E2 receptor EP3 subtype | Humans | agonist |
ADME / PK
| Absorption | Limaprost reaches peak plasma concentration in about 30 minutes . |
|---|---|
| Half-life | The mean half life of elimination is 1.64 hours . |
| Clearance | Mean total clearance is 1.77 liters per hour . |
Formulation & handling
- Limaprost is a small molecule suitable for oral administration in solid dosage forms such as tablets. Due to its low water solubility and high LogP, formulation strategies should address bioavailability challenges related to lipophilicity. Handling considerations include protection from moisture to maintain stability given its solid state.
Regulatory status
Safety
| Toxicity | The most common adverse effects seen with limaprost are diarrhea, nausea/vomiting, flushing, abdominal discomfort, and headache. |
|---|
- Handle limaprost with appropriate protective equipment to minimize exposure risk due to potential gastrointestinal irritation
- Ensure proper ventilation during manufacturing to reduce inhalation of dust or vapors associated with flushing and headache adverse effects
- Store in a controlled environment to maintain compound stability and reduce degradation that may increase toxicity potential
Limaprost is a type of Prostaglandin Analogues
Prostaglandin analogues are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in the field of medicine. These synthetic compounds mimic the effects of natural prostaglandins, which are hormone-like substances found in the body.
Prostaglandin analogues have gained significant attention in medical research due to their diverse therapeutic applications. They exhibit a wide range of physiological activities, such as regulating inflammation, blood flow, and hormone levels. These compounds are commonly used in the treatment of various conditions, including glaucoma, ocular hypertension, and certain types of cancer.
One notable application of prostaglandin analogues is in ophthalmology. These compounds effectively reduce intraocular pressure by increasing the outflow of aqueous humor, providing an effective treatment for glaucoma patients. Moreover, prostaglandin analogues offer the advantage of once-daily dosing, enhancing patient compliance and convenience.
In the field of oncology, prostaglandin analogues have shown promise as anticancer agents. They exert anti-proliferative effects on cancer cells and can induce apoptosis, making them valuable in the treatment of certain malignancies.
Overall, prostaglandin analogues represent a significant class of pharmaceutical APIs with diverse therapeutic applications. Continued research and development in this area hold great potential for the advancement of medicine and the improvement of patient care.
Limaprost (Prostaglandin Analogues), classified under Anti-inflammatory Agents
Anti-inflammatory agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat various inflammatory conditions. These agents play a vital role in alleviating pain, reducing swelling, and controlling inflammation in the body. They are widely employed in the management of diverse medical conditions, including arthritis, autoimmune disorders, asthma, and skin conditions like dermatitis.
Anti-inflammatory APIs primarily function by inhibiting the production of specific enzymes called cyclooxygenases (COX) and lipoxygenases (LOX). These enzymes are responsible for the synthesis of pro-inflammatory molecules known as prostaglandins and leukotrienes, respectively. By suppressing the activity of COX and LOX, anti-inflammatory agents effectively curtail the production of these inflammatory mediators, thereby mitigating inflammation.
Common examples of anti-inflammatory APIs include non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen, aspirin, and naproxen. These agents exhibit analgesic, antipyretic, and anti-inflammatory properties. Another group of anti-inflammatory APIs includes corticosteroids, such as prednisone and dexamethasone, which are synthetic hormones that modulate the body's immune response to control inflammation.
In conclusion, anti-inflammatory agents are a vital category of pharmaceutical APIs widely used to manage inflammation-related disorders. They target enzymes involved in the synthesis of pro-inflammatory molecules, effectively reducing pain and swelling. NSAIDs and corticosteroids are commonly prescribed anti-inflammatory APIs due to their efficacy in controlling inflammation.
Limaprost API manufacturers & distributors
Compare qualified Limaprost API suppliers worldwide. We currently have 4 companies offering Limaprost API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| Chinoin | Producer | Hungary | Unknown | CoA, JDMF | 21 products |
| Chirogate International | Producer | Taiwan | Taiwan | CoA | 17 products |
| Kanto Chemical | Producer | Japan | Japan | CoA, JDMF | 3 products |
| Yonsung Fine Chem. | Producer | South Korea | South Korea | CoA, JDMF | 13 products |
When sending a request, specify which Limaprost 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 Limaprost 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.
