Eliquis (Apixaban) API Manufacturers & Suppliers
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Apixaban | CAS No: 503612-47-3 | GMP-certified suppliers
A medication that helps reduce stroke and systemic embolism risk in nonvalvular atrial fibrillation and supports prevention and treatment of deep vein thrombosis and pulmonary embolism.
Therapeutic categories
Primary indications
- Apixaban is indicated for reducing the risk of stroke and systemic embolism in patients who have nonvalvular atrial fibrillation, prophylaxis of deep vein thrombosis(DVT) leading to pulmonary embolism(PE) in patients after a hip or knee replacement surgery, and treatment of DVT and PE to reduce the risk of recurrence[Label,A177565,A6897]
Product Snapshot
- Oral small‑molecule formulation supplied primarily as coated or film‑coated tablets
- Used for prevention of stroke and systemic embolism in nonvalvular atrial fibrillation and for prophylaxis and treatment of DVT and PE
- Approved in the US, EU, and Canada for these indications
Clinical Overview
Apixaban acts by selectively inhibiting factor Xa in both its free and prothrombinase‑bound forms, independent of antithrombin III. Inhibition of factor Xa decreases thrombin generation and suppresses fibrin clot formation. This targeted interruption of the coagulation cascade produces a predictable anticoagulant effect that is not dependent on vitamin K pathways.
Oral absorption is rapid, and the compound is a substrate for CYP3A4/5, several additional CYP isoforms, P‑glycoprotein, and BCRP. These pathways contribute to metabolic clearance and influence drug–drug interaction potential. Distribution is moderate, with partial protein binding reported in the literature. Elimination involves both metabolic and biliary‑fecal routes, with renal pathways contributing to a lesser extent.
Safety considerations center on bleeding risk, which may increase with advancing age, impaired renal function, or coadministration of strong inhibitors or inducers of CYP3A4 or P‑glycoprotein. There is no requirement for routine coagulation monitoring in standard clinical use, but clinicians may assess exposure in special circumstances. Use should be avoided in active pathological bleeding, and caution is warranted around neuraxial procedures due to risk of hematoma.
Apixaban is widely used in chronic cardiovascular disease management and perioperative thromboprophylaxis. Its predictable pharmacology has made it a preferred option in settings where direct factor Xa inhibition is desired.
For API procurement, sourcing should prioritize manufacturers with demonstrated control of stereochemistry, impurity profiles, and particle‑size specifications, alongside full regulatory documentation to support global dossier development and qualification activities.
Identification & chemistry
| Generic name | Apixaban |
|---|---|
| Molecule type | Small molecule |
| CAS | 503612-47-3 |
| UNII | 3Z9Y7UWC1J |
| DrugBank ID | DB06605 |
Pharmacology
| Summary | Apixaban is an oral anticoagulant that selectively inhibits factor Xa, blocking its activity in both free and complexed forms without requiring antithrombin III. By also inhibiting the prothrombinase complex, it reduces thrombin generation and suppresses clot formation. These actions support its use in conditions where prevention or treatment of pathological thrombosis is required. |
|---|---|
| Mechanism of action | Apixaban selectively inhibits factor Xa in its free and bound forms, independant of antithrombin III[Label]. Apixaban also inhibits prothrominase[Label]. These effects prevent the formation of a thrombus[Label]. |
| Pharmacodynamics | Apixaban selectively inhibits factor Xa in its free and bound forms, independant of antithrombin III[Label]. Apixaban also inhibits prothrominase[Label]. These effects prevent the formation of a thrombus[Label]. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Coagulation factor X | Humans | inhibitor |
ADME / PK
| Absorption | Apixaban is approximately 50% bioavailable[Label] though other studies report 43-46% oral bioavailability. |
|---|---|
| Half-life | 12.7±8.55h[Label,A177565,A6897]. |
| Protein binding | 92-94%[Label]. |
| Metabolism | 50% of the orally administered dose is excreted as the unchanged parent compound, however 25% of the dose is excreted as O-demethyl apixaban sulfate[Label,A177565]. All apixaban metabolites account for approximately 32% of the excreted dose though the structure of all metabolites are not well defined. Apixaban is mainly metabolized by cytochrome p450(CYP)3A4 and to a lesser extent by CYP1A2, CYP2C8, CYP2C9, CYP2C19, and CYP2J2[Label]. |
| Route of elimination | 56% of an orally administered dose is recovered in the feces and 24.5-28.8% of the dose is recovered in the urine[label,A177565,A6897]. 83-88% of the dose recovered in the urine was the unchanged parent compound. |
| Volume of distribution | Approximately 21L[Label]. |
| Clearance | 3.3L/h[Label] though other studies report 4876mL/h. |
Formulation & handling
- Oral small‑molecule anticoagulant formulated as solid tablets; low aqueous solubility may necessitate solubility‑enhancing excipients for consistent dissolution.
- Stable as a solid; standard moisture protection is generally adequate due to moderate lipophilicity and limited hygroscopicity.
- Food has minimal impact on absorption, allowing flexible administration conditions in formulation design.
Regulatory status
| Lifecycle | Most patent protection for the API has lapsed in Canada, the EU, and the United States, with the exception of a U.S. patent expiring in 2031. As a result, the API is largely in a mature market phase, with some remaining exclusivity only in the U.S. until that final expiry. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Apixaban is supplied globally by a single originator partnership, with branded products established across the US, EU, and Canada. Multiple Canadian and several US patents have already expired, enabling generic entry in many markets, while a remaining US patent extending to 2031 preserves some originator protection there. As a result, the manufacturing landscape includes both established branded supply and growing generic participation outside the still‑protected segments of the US market. |
|---|
Safety
| Toxicity | Animal studies have shown an increased risk of maternal bleeding during pregnancy but no increase in fetal malformations or fetal or maternal deaths[Label]. It is unknown if this animal data also translates to humans so apixaban should only be used in pregnancy if the benefits outweigh the risks[Label]. It is not know whether apixaban is safe and effective in labor and during birth, though animal studies have shown an increased rate of maternal bleeding[Label]. Animal studies in rats show apixaban excreted in milk, though it is not know if this also applies to humans[Label]. Nursing mothers should either stop breastfeeding or stop taking apixaban depending on the risk and benefit of each option[Label]. Studies to determine safety and effectiveness in pediatric patients have yet to be performed[Label]. Studies that involved geriatric patients (at least 75 years old) saw no difference in safety or effectiveness compared to younger patients, though geriatric patients at an especially advanced age may be more susceptible to adverse effects[Label]. Dosage adjustments for patients with end stage renal disease(ESRD) are based on estimates of pharmacokinetic principles and not clinical study[Label]. Patients with ESRD may experience pharmacodynamics similar to those seen in well controlled studies but it may not lead to the same clinical effects[Label]. Dosage adjustments are not necessary in mild hepatic impairment[Label]. In moderate hepatic impairment patients may already experience abnormalities in coagulation and so no dose recommendations are possible[Label]. Apixaban is not recommended for patients with severe hepatic impairment[Label]. |
|---|
- Animal data indicate increased maternal bleeding and milk excretion in rats, underscoring reproductive‑toxicity considerations and the need for controlled handling in studies involving gestating or lactating models
- Moderate to severe hepatic impairment and ESRD may alter apixaban pharmacokinetics and coagulation parameters, reflecting higher uncertainty in exposure profiles in these populations
- Geriatric subjects show generally comparable safety to younger adults, though very advanced age may correlate with greater susceptibility to anticoagulation‑related adverse effects
Apixaban is a type of Antithrombotics
Antithrombotics, a subcategory of pharmaceutical active pharmaceutical ingredients (APIs), play a crucial role in preventing and treating thrombotic disorders, which are characterized by the formation of blood clots within blood vessels. These medications are essential in reducing the risk of thrombosis, such as deep vein thrombosis (DVT), pulmonary embolism (PE), and stroke, which can lead to severe health complications.
Antithrombotics exert their therapeutic effects through various mechanisms. One commonly used class of antithrombotics is anticoagulants, which inhibit the clotting process by interfering with the formation of blood clots. These drugs include heparin, warfarin, and direct oral anticoagulants (DOACs). They are administered to patients with conditions like atrial fibrillation, venous thromboembolism, or mechanical heart valves to prevent clot formation.
Another class of antithrombotics is antiplatelet agents, which prevent platelet aggregation, an essential step in blood clot formation. Aspirin, clopidogrel, and ticagrelor are well-known antiplatelet drugs used to prevent thrombosis in patients with coronary artery disease, ischemic stroke, or peripheral artery disease.
Antithrombotics are typically prescribed based on the individual patient's risk factors, medical history, and the specific thrombotic condition being treated. Dosage and administration instructions may vary depending on the drug's pharmacokinetic profile and desired therapeutic outcomes.
As with any medication, antithrombotics may have potential side effects, such as increased bleeding risk. Therefore, healthcare professionals carefully assess the patient's overall health status, including any underlying conditions, before prescribing these medications.
In conclusion, antithrombotics are a crucial subcategory of pharmaceutical APIs that play a vital role in preventing and treating thrombotic disorders. By inhibiting clot formation through various mechanisms, these medications significantly contribute to reducing the risk of serious complications associated with blood clots.
Apixaban (Antithrombotics), 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.
Apixaban API manufacturers & distributors
Compare qualified Apixaban API suppliers worldwide. We currently have 35 companies offering Apixaban API, with manufacturing taking place in 13 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 |
|---|---|---|---|---|---|
| ACE Japan | Producer | Japan | Japan | CoA | 76 products |
| Amino Chemicals | Producer | Malta | Malta | CoA, GMP | 20 products |
| Apollo Healthcare Resourc... | Distributor | Singapore | Singapore | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC | 200 products |
| Arshine Pharmaceutical Co... | Distributor | China | China | CoA | 176 products |
| Aurora Industry Co., Ltd | Distributor | China | China | BSE/TSE, CEP, CoA, FDA, GMP, ISO9001, MSDS, USDMF, WC | 250 products |
| AXXO GmbH | Distributor | Germany | World | CoA, GMP, GDP, KDMF, MSDS, USDMF | 243 products |
| Chongqing Jooe Co., Ltd. | Producer | China | China | CoA, GMP, MSDS | 10 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CoA, FDA, GMP, KDMF, MSDS, USDMF, WC | 170 products |
| Dr. Sahu's Laboratories | Producer | India | India | CoA, GMP | 70 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CEP, CoA, FDA, GMP, ISO9001, MSDS, USDMF | 484 products |
| HEC Pharm | Producer | Germany | Unknown | CoA, USDMF | 31 products |
| Hikal | Producer | India | India | CoA, USDMF | 26 products |
| Honour Lab | Producer | India | India | CoA, GMP, USDMF, WC | 30 products |
| Indoco Remedies | Producer | India | India | CoA, USDMF | 19 products |
| Jubilant Pharmova | Producer | India | India | BSE/TSE, CoA, GMP, ISO9001, MSDS, USDMF | 52 products |
| Medichem | Producer | Spain | Malta | CoA, GMP | 39 products |
| Micro Labs | Producer | India | India | CoA, USDMF | 38 products |
| Minakem | Producer | France | Canada | BSE/TSE, CoA, FDA, GMP, MSDS, USDMF | 31 products |
| Morepen Laboratories Ltd. | Producer | India | India | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, ISO9001, MSDS, USDMF, WC | 22 products |
| MSN Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 119 products |
| Mylan | Producer | India | India | CoA, USDMF | 201 products |
| Natco Pharma | Producer | India | India | CoA, USDMF | 40 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, MSDS, USDMF | 64 products |
| Rochem International, Inc... | Distributor | United States | United States | BSE/TSE, CEP, CoA, GMP, ISO9001, MSDS, USDMF | 144 products |
| Senova Technology Co., Lt... | Producer | China | China | BSE/TSE, CoA, ISO9001, MSDS | 157 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, GMP, ISO9001, MSDS, USDMF | 762 products |
| Sintenovo | Producer | Spain | Spain | CoA, USDMF | 7 products |
| Solfyn International LLP | Distributor | India | India | BSE/TSE, CoA, GMP, ISO9001, MSDS, USDMF, WHO-GMP | 24 products |
| Srini Pharma | Producer | India | India | CoA, GMP | 12 products |
| Sun Pharma | Producer | India | India | CoA, USDMF | 219 products |
| Unichem Labs. | Producer | India | India | CoA, USDMF | 62 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 136 products |
| Vonage Pharma (Former Plu... | Producer | Turkey | Turkey | CoA, GMP, MSDS, USDMF, WC | 28 products |
| Zhejiang Hisun Pharma | Producer | China | China | CoA, USDMF | 69 products |
When sending a request, specify which Apixaban 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 Apixaban 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.
