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Acenocoumarol | CAS No: 152-72-7 | GMP-certified suppliers
A medication that supports treatment and prevention of thromboembolic conditions, including deep vein thrombosis, pulmonary embolism, cerebral embolism, and infarction‑related clotting events.
Therapeutic categories
Primary indications
- For the treatment and prevention of thromboembolic diseases
- More specifically, it is indicated for the prevention of cerebral embolism, deep vein thrombosis, pulmonary embolism, thromboembolism in infarction and transient ischemic attacks
- It is used for the treatment of deep vein thrombosis and myocardial infarction
Product Snapshot
- Oral small‑molecule anticoagulant supplied as tablet formulations
- Used for prevention and management of thromboembolic events such as cerebral embolism, deep vein thrombosis, pulmonary embolism, and related cardiovascular thromboses
- Approved in Canada and the US with mixed approved and investigational status depending on jurisdiction
Clinical Overview
The pharmacological action of acenocoumarol is based on selective inhibition of vitamin K reductase. By limiting regeneration of reduced vitamin K, it restricts gamma‑carboxylation of glutamate residues on clotting factors II, VII, IX, and X, as well as proteins C and S. Insufficient carboxylation impairs calcium‑dependent activation of these factors, reducing thrombin generation and lowering the thrombogenic potential of circulating clots. Both the intrinsic and extrinsic coagulation pathways are affected.
Acenocoumarol exhibits a narrow therapeutic index. Its anticoagulant effect generally correlates with international normalized ratio values, which require regular monitoring. Hemoglobin, hematocrit, and liver function tests are also monitored in clinical use. Patients receiving therapy are not permitted to donate blood due to bleeding risk.
Absorption, distribution, and elimination parameters vary, and dosing is individualized based on coagulation response rather than fixed pharmacokinetic targets. Acenocoumarol undergoes hepatic metabolism and is a substrate of several cytochrome P450 enzymes, including CYP1A2, CYP2C9, CYP2C19, and CYP3A4, indicating potential sensitivity to drug interactions. Its classification as a P‑glycoprotein substrate further supports attention to interaction risk. Toxicity is primarily related to excessive anticoagulation, with bleeding as the principal clinical concern.
Acenocoumarol is marketed in various regions under established brands for chronic oral anticoagulation, though local product names vary.
For API procurement, sourcing should prioritize manufacturers with documented control of stereochemical purity and impurity profiles, as variability can influence potency in a drug with a narrow therapeutic index. Robust regulatory documentation and consistent batch‑to‑batch quality are essential for formulation development and continual supply assurance.
Identification & chemistry
| Generic name | Acenocoumarol |
|---|---|
| Molecule type | Small molecule |
| CAS | 152-72-7 |
| UNII | I6WP63U32H |
| DrugBank ID | DB01418 |
Pharmacology
| Summary | Acenocoumarol acts as a vitamin K antagonist by inhibiting vitamin K epoxide reductase, reducing the availability of reduced vitamin K required for activating vitamin K‑dependent coagulation factors. This limits gamma‑carboxylation of factors II, VII, IX, and X, along with proteins C and S, leading to decreased thrombin generation. The resulting reduction in functional clotting factors underpins its use in preventing and treating thromboembolic disorders. |
|---|---|
| Mechanism of action | Acenocoumarol inhibits vitamin K reductase, resulting in depletion of the reduced form of vitamin K (vitamin KH2). As vitamin K is a cofactor for the carboxylation of glutamate residues on the N-terminal regions of vitamin K-dependent clotting factors, this limits the gamma-carboxylation and subsequent activation of the vitamin K-dependent coagulant proteins. The synthesis of vitamin K-dependent coagulation factors II, VII, IX, and X and anticoagulant proteins C and S is inhibited resulting in decreased prothrombin levels and a decrease in the amount of thrombin generated and bound to fibrin. This reduces the thrombogenicity of clots. |
| Pharmacodynamics | Acenocoumarol inhibits the reduction of vitamin K by vitamin K reductase. This prevents carboxylation of certain glutamic acid residues near the N-terminals of clotting factors II, VII, IX and X, the vitamin K-dependent clotting factors. Glutamic acid carboxylation is important for the interaction between these clotting factors and calcium. Without this interaction, clotting cannot occur. Both the extrinsic (via factors VII, X and II) and intrinsic (via factors IX, X and II) are affected by acenocoumarol. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Vitamin K epoxide reductase complex subunit 1 | Humans | inhibitor |
ADME / PK
| Absorption | Rapidly absorbed orally with greater than 60% bioavailability. Peak plasma levels are attained 1 to 3 hours following oral administration. |
|---|---|
| Half-life | 8 to 11 hours. |
| Protein binding | 98.7% protein bound, mainly to albumin |
| Metabolism | Extensively metabolized in the liver via oxidation forming two hydroxy metabolites and keto reduction producing two alcohol metabolites. Reduction of the nitro group produces an amino metabolite which is further transformed to an acetoamido metabolite. Metabolites do not appear to be pharmacologically active. |
| Route of elimination | Mostly via the kidney as metabolites |
| Volume of distribution | The volume of distribution at steady-state appeared to be significantly dose dependent: 78 ml/kg for doses < or = 20 microg/kg and 88 ml/kg for doses > 20 microg/kg respectively |
Formulation & handling
- Low aqueous solubility solid oral small molecule; may require solubility or dissolution enhancement for robust tablet performance.
- Chemically stable 4‑hydroxycoumarin derivative suitable for standard solid‑dose processing with attention to light protection if needed for coumarins.
- Oral use with known sensitivity to dietary vitamin K variability, which may necessitate controlled excipient selection to avoid nutrient interactions.
Regulatory status
| Lifecycle | The API is marketed in the United States and Canada, where patent protections have expired or are nearing expiry, indicating a mature competitive landscape. These markets generally reflect stable generic participation and limited prospects for further exclusivity-driven growth. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Acenocoumarol is an established anticoagulant originally introduced by a single originator manufacturer, with subsequent production now supported by multiple generic producers. Branded formulations such as Sintrom have long-standing availability in several regions, including Canada and other international markets, though distribution in the United States is limited. Patents expired decades ago, and widespread generic competition is already well established in global supply chains. |
|---|
Safety
| Toxicity | The onset and severity of the symptoms are dependent on the individual's sensitivity to oral anticoagulants, the severity of the overdosage, and the duration of treatment. Bleeding is the major sign of toxicity with oral anticoagulant drugs. The most frequent symptoms observed are: cutaneous bleeding (80%), haematuria (with renal colic) (52%), haematomas, gastrointestinal bleeding, haematemesis, uterine bleeding, epistaxis, gingival bleeding and bleeding into the joints. Further symptoms include tachycardia, hypotension, peripheral circulatory disorders due to loss of blood, nausea, vomiting, diarrhoea and abdominal pains. |
|---|
- Principal hazard is anticoagulant‑related bleeding
- Material handling should account for potential cutaneous, gastrointestinal, and urogenital hemorrhagic effects upon exposure
- Systemic exposure may provoke hemodynamic instability (tachycardia, hypotension) secondary to blood loss, indicating a need for controls that limit inhalation or ingestion
Acenocoumarol is a type of Other antithrombin
The Other Antithrombin subcategory in pharmaceutical active pharmaceutical ingredients (APIs) refers to a class of compounds that exhibit antithrombin activity but do not fall under the traditional anticoagulant or antiplatelet categories. These APIs play a crucial role in preventing blood clot formation and reducing the risk of thrombotic events.
One notable API in this subcategory is [Name of the API], which demonstrates potent antithrombin properties by inhibiting specific clotting factors in the blood. By targeting these factors, [Name of the API] helps regulate the coagulation cascade, a complex process involved in blood clot formation.
The unique mechanism of action of [Name of the API] distinguishes it from other antithrombin APIs, making it a valuable option for treating thrombotic disorders. This API exhibits high selectivity, effectively inhibiting clotting factors without significantly impacting other blood components or processes.
[Name of the API] is carefully developed and rigorously tested to ensure its safety, efficacy, and reliability. It undergoes stringent quality control measures to meet regulatory standards and ensure consistency in its performance.
Pharmaceutical companies incorporate [Name of the API] into various formulations, such as oral tablets, injections, or topical preparations, enabling healthcare providers to administer it in the most suitable form for patients.
The Other Antithrombin subcategory in pharmaceutical APIs, with [Name of the API] as a prominent member, provides an innovative therapeutic approach to managing thrombotic disorders and contributes to enhancing patient care and outcomes in the field of hematology.
Acenocoumarol (Other antithrombin), classified under Anticoagulants
Anticoagulants are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) used to prevent and treat blood clotting disorders. These medications play a crucial role in various medical conditions, including deep vein thrombosis (DVT), pulmonary embolism (PE), and atrial fibrillation (AF). Anticoagulants work by inhibiting the formation of blood clots or by preventing existing clots from getting larger.
There are different types of anticoagulants available, including direct thrombin inhibitors, vitamin K antagonists, and factor Xa inhibitors. Direct thrombin inhibitors, such as dabigatran, directly target the enzyme thrombin to hinder clot formation. Vitamin K antagonists, like warfarin, interfere with the production of clotting factors that rely on vitamin K. Factor Xa inhibitors, such as rivaroxaban and apixaban, inhibit the activity of factor Xa, a crucial component in the clotting cascade.
Anticoagulants are commonly prescribed to patients at risk of developing blood clots or those with existing clotting disorders. They are often used during surgeries, such as hip or knee replacements, to minimize the risk of post-operative clot formation. Patients with AF, a condition characterized by irregular heart rhythm, may also be prescribed anticoagulants to prevent stroke caused by blood clots.
While anticoagulants offer significant benefits in preventing and treating clot-related conditions, they also carry potential risks, including bleeding complications. Patients taking anticoagulants require careful monitoring to ensure the right dosage is administered, as excessive anticoagulation can lead to hemorrhage. Regular blood tests and close medical supervision are essential to manage the delicate balance between preventing clots and avoiding excessive bleeding.
In conclusion, anticoagulants are a crucial category of pharmaceutical APIs used to prevent and treat blood clotting disorders. They function by inhibiting clot formation or preventing existing clots from enlarging. While highly beneficial, their use requires careful monitoring to minimize the risk of bleeding complications.
Acenocoumarol API manufacturers & distributors
Compare qualified Acenocoumarol API suppliers worldwide. We currently have 4 companies offering Acenocoumarol 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 |
|---|---|---|---|---|---|
| Alkaloida Chemical | Producer | Hungary | Hungary | CoA, GMP | 6 products |
| Asence Pharma | Producer | India | India | CoA, WC | 6 products |
| Ipochem | Producer | Poland | Poland | CoA, GMP | 3 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, MSDS | 64 products |
When sending a request, specify which Acenocoumarol 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 Acenocoumarol 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.
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