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Acemetacin | CAS No: 53164-05-9 | GMP-certified suppliers
A medication that provides symptomatic relief of pain and inflammation in rheumatic joint disorders, ankylosing spondylitis, degenerative spinal conditions, and post-surgical soft-tissue inflammation.
Therapeutic categories
Primary indications
- Acemetacin is not FDA, Canada or EMA approved, but in the countries where it is marketed it is indicated for the symptomatic treatment of pain and swelling in acute inflammation of the joints in rheumathoid arthritis, osteoarthritis, low back pain and post-surgical pain
- It is also indicated for the treatment of chronic inflammation of the joints in presence of rheumatoid arthritis, treatment of ankylosing spondylitis, treatment of irritation in the joints and spinal column caused by degenerative disorders, treatment of inflammatory soft-tissue rheumatism syndrome and painful swelling and inflammation caused by injury
- [L1044, L1046]
Product Snapshot
- Acemetacin is an oral small molecule formulated primarily as capsules, including extended and delayed-release forms
- It is used for the symptomatic treatment of acute and chronic inflammation-related pain in conditions such as rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, and soft tissue rheumatism
- Acemetacin is approved in certain international markets but lacks FDA, Health Canada, and EMA approval
Clinical Overview
Clinically, acemetacin is utilized in several countries outside of the United States and European Union for the symptomatic management of pain and inflammation associated with rheumatic conditions. Indications include acute and chronic joint inflammation in rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, degenerative spinal disorders, soft-tissue rheumatisms, and pain resulting from injury or surgery. It has not been approved by the FDA, Health Canada, or EMA.
The mechanism of action of acemetacin involves non-selective inhibition of cyclooxygenase (COX) enzymes, which are responsible for the synthesis of pro-inflammatory prostaglandins E2 and F2 derived from fatty acids in cell membranes. This inhibition reduces the production of prostaglandins, thereby decreasing inflammation and pain. Notably, acemetacin’s weaker inhibition of prostaglandin synthesis compared to indometacin translates into relatively better gastrointestinal tolerability. Additionally, acemetacin inhibits histamine release from mast cells, reduces hyperthermia, modulates blood pressure parameters, and inhibits platelet aggregation. Its metabolite, indometacin, further exhibits inhibition of polymorphonuclear leukocyte motility and cerebral blood flow alterations through nitric oxide pathway modulation and vasoconstriction.
Pharmacokinetic data identifies acemetacin as a substrate of UGT2B7 enzymes involved in its metabolism. Safety concerns align with those of non-selective NSAIDs, including risks of gastrointestinal irritation, nephrotoxicity, hypertension, and hyperkalemia. The potential for adverse effects linked to indometacin metabolism underscores the need for monitoring during clinical use.
For API sourcing and quality assurance, attention should be given to adherence to current Good Manufacturing Practices (cGMP), impurity profiles including residual solvents, and batch-to-batch consistency. Analytical verification of acemetacin purity and confirmation of inactive impurities such as the parent compound indometacin is essential to ensure compliance with pharmacopeial standards and regulatory guidelines in relevant markets.
Identification & chemistry
| Generic name | Acemetacin |
|---|---|
| Molecule type | Small molecule |
| CAS | 53164-05-9 |
| UNII | 5V141XK28X |
| DrugBank ID | DB13783 |
Pharmacology
| Summary | Acemetacin is a non-selective inhibitor of cyclooxygenase enzymes (COX-1 and COX-2), reducing the synthesis of prostaglandins involved in inflammation and pain signaling. Its metabolite indometacin contributes additional anti-inflammatory effects by inhibiting leukocyte motility and modulating vascular responses. The pharmacodynamic profile includes anti-inflammatory, analgesic, antipyretic activities, and inhibition of platelet aggregation. |
|---|---|
| Mechanism of action | Acemetacin is a non-selective inhibitor of the production of pro-inflammatory mediators derived from the action of the enzyme COX. COX is essential for the synthesis of prostaglandin E2 and F2 which are molecules derived from fatty acids and stored in the cell membrane. Acetometacine is metabolized and forms its major metabolite indometacin which is also a non-selective inhibitor of COX and exhibits the capacity to inhibit the motility of polymorphonuclear leukocytes and decreased cerebral flow by modulating the nitric oxide pathway and vasoconstriction. |
| Pharmacodynamics | The effect of acemetacin causes a weak reduction of prostaglandin synthesis which generates an anti-inflammatory and analgesic effect. The weak inhibition of prostaglandin reduces significantly the damage caused in the mucous membrane of the gastrointestinal tract. Studies have shown that acemetacin strongly inhibits the release of histamine from mast cells and the generation of hyperthermia. Acemetacin effect also causes changes in systolic and diastolic blood pressure as well as inhibition of platelet aggregation. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Prostaglandin G/H synthase 1 | Humans | antagonist |
| Prostaglandin G/H synthase 2 | Humans | antagonist |
ADME / PK
| Absorption | After 8 days of oral administration twice daily of acemetacin there was an age-dependant Cmax of 276.8 ng/ml in elderly compared to 187 ng/ml for younger individuals. There was also a Tmax of 2.5 h and AUC in a range of 483-712 ng h/ml. The bioavailability of acemetacin after repeated doses is aproximately 66% in plasma and 64% in urine. |
|---|---|
| Half-life | The elimination half-life of acemetacin after steady-state is 4.5 hours. |
| Protein binding | Acemetacin is found highly bound to plasma proteins, reaching a percentage higher than 90% of the administered dose. |
| Metabolism | Acemetacin is highly metabolized and degraded by esterolytic cleavage to form its major and active metabolite indometacin. It presents other inactive metabolites made by reaction of O-demethylation, N-desacylation and part of them are also transformed by conjugation with glucuronic acid. |
| Route of elimination | The elimination of acemetacin is divided in renal elimination that covers 40% of the complete administered dose and the restant 60% is excreted in feces. |
| Volume of distribution | The apparent volume of distribution of acemetacin is in a range of 0.5-0.7 L/kg. |
| Clearance | Intravenous administration of acemetacin in healthy subjects reported a clearance rate of 4.59 ml min/kg. |
Formulation & handling
- Acemetacin is a small molecule suitable for oral administration, primarily formulated as capsules in immediate, extended, and delayed-release forms.
- Due to low water solubility (2.29 mg/L) and moderate lipophilicity (LogP 3.15), formulation strategies should address dissolution and bioavailability enhancement.
- Stability considerations should focus on protecting the solid form from moisture and light to maintain compound integrity during storage and handling.
Regulatory status
Safety
| Toxicity | The pharmacological activity of acemetacin causes blockage of prostaglandin synthesis. Prostaglandin is one of the mediators of renal blood flow and glomerular filtration thus, acemetacin causes a decreased renal function, transient renal insufficiency, interstitial nephritis and papillary necrosis especially in elderly patients, patients with congestive heart failure, hepatic cirrhosis and impaired renal function. |
|---|
- Acemetacin inhibits prostaglandin synthesis, which may lead to decreased renal function and potential renal toxicity
- Risk of renal adverse effects, including transient renal insufficiency, interstitial nephritis, and papillary necrosis, is increased in patients with pre-existing renal impairment, heart failure, or hepatic cirrhosis
- Handling should consider the compound's nephrotoxic potential
Acemetacin is a type of 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.
Acemetacin API manufacturers & distributors
Compare qualified Acemetacin API suppliers worldwide. We currently have 1 companies offering Acemetacin API, with manufacturing taking place in 1 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 |
|---|---|---|---|---|---|
| Zhejiang Hengkang Pharmac... | Producer | China | China | BSE/TSE, CEP, CoA, EDMF/ASMF, MSDS, USDMF, WC | 31 products |
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