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Argatroban | CAS No: 74863-84-6 | GMP-certified suppliers
A medication that prevents and treats thrombosis in patients with heparin-induced thrombocytopenia (HIT) and supports safe anticoagulation during percutaneous coronary interventions.
Therapeutic categories
Primary indications
- Argatroban is indicated for prevention and treatment of thrombosis caused by heparin-induced thrombocytopenia (HIT)
- It is also indicated for use in patients with, or at risk for, HIT who are undergoing percutaneous coronary intervention
Product Snapshot
- Argatroban is an injectable small molecule formulation supplied as an intravenous injection or solution concentrate
- It is primarily used for prevention and treatment of thrombosis associated with heparin-induced thrombocytopenia and for patients undergoing percutaneous coronary intervention at risk for HIT
- Argatroban is approved for use in the US and Canada, with both approved and investigational designations
Clinical Overview
Pharmacologically, argatroban acts by reversibly binding to the active site of thrombin, inhibiting both free and clot-associated thrombin activity. This blockade interrupts thrombin-mediated processes including fibrin formation, activation of coagulation factors V, VIII, and XIII, protein C activation, and platelet aggregation. Unlike indirect anticoagulants, argatroban does not require antithrombin III as a co-factor. It exhibits high selectivity with an inhibitory constant (Ki) of approximately 0.04 µM and shows minimal activity against related serine proteases such as factor Xa, plasmin, trypsin, and kallikrein at therapeutic levels.
Key pharmacokinetic parameters of argatroban include hepatic metabolism primarily via the cytochrome P450 CYP3A4/5 enzyme system, necessitating caution in patients with liver impairment or those receiving CYP3A4 inhibitors or inducers. Its elimination half-life is short, allowing for rapid adjustments in anticoagulant effect and reversibility. Given its narrow therapeutic index, careful dosing and monitoring of coagulation parameters, particularly activated partial thromboplastin time (aPTT), are essential during therapy.
Safety considerations involve bleeding risk typical of anticoagulants, requiring baseline coagulation assessment and discontinuation of prior parenteral anticoagulants before initiating argatroban. Due to its metabolism through CYP3A pathways, potential drug interactions must be evaluated to avoid adverse events or subtherapeutic exposure.
Argatroban is marketed under various brand names globally and is primarily utilized in hospital settings for managing HIT-related thrombotic complications, especially during invasive cardiovascular procedures.
For API procurement, quality assurance should focus on stringent control of purity, stereochemistry, and absence of impurities that could compromise safety. Suppliers must comply with international pharmacopeial standards and regulatory requirements to ensure consistent clinical performance.
Identification & chemistry
| Generic name | Argatroban |
|---|---|
| Molecule type | Small molecule |
| CAS | 74863-84-6 |
| UNII | OCY3U280Y3 |
| DrugBank ID | DB00278 |
Pharmacology
| Summary | Argatroban is a synthetic direct thrombin inhibitor that binds reversibly to the active site of thrombin, blocking both free and clot-bound enzyme activity. It inhibits thrombin-mediated processes including fibrin formation, activation of coagulation factors V, VIII, and XIII, and platelet aggregation, without requiring antithrombin III. This selective inhibition of thrombin underlies its therapeutic use in preventing and treating thrombosis associated with heparin-induced thrombocytopenia. |
|---|---|
| Mechanism of action | Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; protein C; and platelet aggregation. |
| Pharmacodynamics | Argatroban is a synthetic direct thrombin inhibitor derived from L-arginine indicated as an anticoagulant for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia. Argatroban is a direct thrombin inhibitor that reversibly binds to the thrombin active site. Argatroban does not require the co-factor antithrombin III for antithrombotic activity. Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; protein C; and platelet aggregation. Argatroban is highly selective for thrombin with an inhibitory constant (K<sub>i</sub>) of 0.04 µM. At therapeutic concentrations, Argatroban has little or no effect on related serine proteases (trypsin, factor Xa, plasmin, and kallikrein). Argatroban is capable of inhibiting the action of both free and clot-associated thrombin. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Prothrombin | Humans | inhibitor |
ADME / PK
| Absorption | Bioavailability is 100% (intravenous). |
|---|---|
| Half-life | 39 and 51 minutes |
| Protein binding | 54% |
| Metabolism | Liver via hydroxylation and aromatization of the 3-methyltetrahydroquinoline ring. Age and gender do not substantially affect the pharmacodynamic or pharmacokinetic profile of argatroban. |
| Route of elimination | Argatroban is excreted primarily in the feces (65%), presumably through biliary secretion; 22% is eliminated via urine. |
| Volume of distribution | * 174 mL/kg * 12.18 L [70-kg adult] |
| Clearance | * 5.1 L/kg/hr [infusion doses up to 40 mcg/kg/min] |
Formulation & handling
- Argatroban is a small molecule dipeptide administered exclusively via intravenous or parenteral injection.
- Formulation requires consideration of low water solubility and stability in solution at various concentrations for injectable use.
- Precautions should be taken regarding potential drug and herbal interactions affecting metabolism, including CYP3A4 modulators.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient has primary patent protection in the United States that expired in June 2014, with additional patents extending exclusivity until September 2027. It is marketed in the US and Canada, indicating a mature market with ongoing patent protection in the US. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Argatroban is manufactured by a single originator company, with packaging managed by another established firm. Its branded products are primarily marketed in the US and Canadian markets. Existing patents extending through 2027 indicate ongoing brand protection, suggesting limited generic competition at present. |
|---|
Safety
| Toxicity | Excessive bleeding |
|---|
- Argatroban may increase risk of excessive bleeding
- Monitor coagulation parameters during handling and formulation
- Implement appropriate containment measures to minimize exposure and prevent cross-contamination
Argatroban is a type of Anticoagulant proteins
Anticoagulant proteins are a crucial subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a vital role in preventing the formation of blood clots. These proteins are naturally occurring substances that interfere with the clotting cascade, a complex series of reactions that lead to blood coagulation.
One of the well-known anticoagulant proteins is hirudin, derived from leeches. Hirudin acts by inhibiting thrombin, a key enzyme involved in blood clot formation. Another notable anticoagulant protein is antithrombin III, which blocks several clotting factors, including thrombin and factors IXa, Xa, XIa, and XIIa. These proteins are widely used in the pharmaceutical industry to develop medications for conditions such as deep vein thrombosis, pulmonary embolism, and stroke prevention.
The production of anticoagulant proteins involves advanced biotechnological processes. Recombinant DNA technology and genetic engineering techniques are employed to produce these proteins in large quantities. The proteins are expressed in host organisms such as bacteria, yeast, or mammalian cells, and then purified through various chromatographic and filtration steps to obtain a highly pure and active form.
The development of anticoagulant proteins has significantly improved the treatment and management of thrombotic disorders. These APIs have proven to be effective in preventing clot formation, reducing the risk of life-threatening complications. However, it is crucial to administer anticoagulant proteins under medical supervision due to their potential side effects and the need for precise dosing.
In conclusion, anticoagulant proteins are a vital subcategory of pharmaceutical APIs that act by inhibiting key components of the clotting cascade. Their production involves advanced biotechnological processes, and they have greatly enhanced the management of thrombotic disorders. Proper medical guidance is essential for their safe and effective use.
Argatroban (Anticoagulant proteins), 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.
Argatroban API manufacturers & distributors
Compare qualified Argatroban API suppliers worldwide. We currently have 9 companies offering Argatroban API, with manufacturing taking place in 6 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 |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, ISO9001, MSDS, USDMF | 229 products |
| BrightGene | Producer | China | China | CoA, JDMF | 11 products |
| Curia | Producer | United States | Italy | CoA, EDMF/ASMF, GMP, MSDS, USDMF | 106 products |
| Emcure Pharma | Producer | India | India | CoA, USDMF | 80 products |
| Euticals | Producer | Italy | Unknown | CoA, USDMF | 48 products |
| Kolon Life Science | Producer | South Korea | South Korea | CoA | 32 products |
| Lundbeck Pharma | Producer | Italy | Italy | CoA, GMP, JDMF, USDMF | 15 products |
| Mitsubishi Tanabe | Producer | Japan | Japan | CoA, JDMF | 2 products |
| Weijie Pharmaceuticals | Producer | China | China | CoA, FDA, GMP, JDMF | 15 products |
When sending a request, specify which Argatroban 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.).
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