General Information

Apixaban Impurities and Apixaban  

Daicel Pharma synthesizes high-quality Apixaban impurities, including N-Formyl-1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo(3,4-c)pyridine-3-carboxamide, ethyl 6-(4-(5-chloropentanamido)phenyl-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo(3,4-c)pyridine-3-carboxylate, ethyl 1-(4-methoxyphenyl)-7a-morpholino-6-(4-nitrophenyl)-7-oxo3a,4,5,6,7,7a-hexahydro-1H-pyrazolo(3,4-c)pyridine-3-carboxylate, and so on. These impurities are essential for evaluating the quality, stability, and safety of Apixaban, which is an active pharmaceutical ingredient. Additionally, Daicel Pharma offers a customized synthesis of Apixaban impurities for global delivery to meet the specific needs of our customers.

Apixaban [CAS: 503612-47-3] is an oral anticoagulant that selectively inhibits factor Xa. Apixaban blocks the conversion of prothrombin to thrombin, and prevents the formation of cross-linked fibrin clots.

Apixaban: Use and Commercial Availability  

Apixaban is a medication and belongs to the class of novel oral anticoagulants (NOACs). It is available under the brand name Eliquis. This medication has multiple approved indications, including reducing the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation. It also treats deep vein thrombosis (DVT) and pulmonary embolism (PE) and prevents DVT in patients undergoing knee or hip replacement surgery. Additionally, Apixaban helps reduce the risk of recurrent DVT and PE. Overall, Apixaban is a versatile medication that inhibits blood clotting factors, reducing the risk of potentially serious complications associated with various medical conditions.

Apixaban Structure and Mechanism of Action

The chemical name of Apixaban is 4,5,6,7-Tetrahydro-1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-1H-pyrazolo[3,4-c]pyridine-3-carboxamide. Its chemical formula is C₂₅H₂₅N₅O₄, and its molecular weight is approximately 459.5 g/mol.

Apixaban inhibits prothrombinase activity and clot-bound Fxa. It decreases thrombin generation and thrombus development.

Apixaban Impurities and Synthesis

As with any medication, Apixaban may contain impurities that affect its safety and efficacy. Impurities can be generated during the synthesis¹ and storage of the drug. Apixaban impurities can include related compounds that may have similar chemical and physical properties as the active pharmaceutical ingredient (API) and degradation products that result from chemical or external changes in the drug over time. Apixaban impurities may also include residual solvents, reagents, or other substances used during the manufacturing process. It is essential to synthesize and analyze Apixaban impurities in the API to ensure the medication is safe and effective for patients.

Daicel Pharma provides a Certificate of Analysis (CoA) for Apixaban impurity standards, including N-Formyl-1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo(3,4-c)pyridine-3-carboxamide, ethyl 6-(4-(5-chloropentanamido)phenyl-1-(4-methoxyphenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo(3,4-c)pyridine-3-carboxylate, ethyl 1-(4-methoxyphenyl)-7a-morpholino-6-(4-nitrophenyl)-7-oxo3a,4,5,6,7,7a-hexahydro-1H-pyrazolo(3,4-c)pyridine-3-carboxylate, and so on. The CoA is generated from a cGMP-compliant analytical facility and includes comprehensive characterization data such as 1H NMR, 13C NMR, IR, MASS, and HPLC purity². We can also give additional characterization data like 13C-DEPT and CHN on request. Daicel Pharma is capable of preparing unknown Apixaban impurities or degradation products. Each delivery has a complete characterization report.