Product 

[Generic name] [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 
[Product name] apixaban
[Pharmacological classification] selective inhibitor of activated Factor Ⅹ
[category] chemical drug 6 new drug class
[Indications] for non-valvular atrial fibrillation (AF) of stroke and systemic embolism prophylaxis (US) patients; for the prevention undergoing elective hip joint or knee replacement surgery in adult patients with venous thromboembolism (EU) 
[Specifications] formulation and tablet; 2.5mg, 5mg 
Dosage The recommended dose is 5 mg, 2 times a day; for patients meet at least two of the following characteristics, it is recommended to use a small dose of 2.5 mg, 2 times a day: age ≥80 years old, weighing ≤60 kg, or serum creatinine ≥1.5 mg / dl. In addition, when the cytochrome P450 3A4 (CYP3A4) and P- glycoprotein (P-gp) potent dual inhibitor, such as ketoconazole and clarithromycin combination therapy is also recommended to use small doses. 
Pharmacological and clinical characteristics of competitive advantages: 
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 is a selective inhibitor of the activation of factor Ⅹ oral administration. 1- (4-Methoxyphenyl) -7-oxo-6- [4- (2-oxopiperidin-1-yl) phenyl] -4,5,6,7-tetrahydro-1H-pyrazolo [3,4-c] pyridine bioavailability -3-carboxamide was 50%, the peak time after oral administration of 3 hours, half-life of 12 hours, 70% of the feces, 30% excreted by the kidneys. 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 by a high selectivity to inhibit direct inhibition of thrombin and factor Xa thrombosis. 
In the diagnosis of atrial fibrillation patients, Xa factor inhibitor directly 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 superior to aspirin in the prevention of embolic events, including stroke, including aspects. 
The study showed that patients with atrial fibrillation in the prevention of stroke or systemic embolism Majesty, compared with warfarin, the drug can reduce stroke or systemic embolism by 21%, 11% reduction in mortality, 31% lower rate of major bleeding. 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 better than other similar products in the overall mortality and improve safety. 
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 more effective than enoxaparin in preventing patients after knee replacement surgery venous thromboembolism, oral simple help improve patient compliance, but does not increase the risk of bleeding. 
Study Abroad: 
Jointly developed by Bristol-Myers Squibb and Pfizer. May 20, 2011, the EU has been approved for use in the EU 27 member states, which is the world's first drug approved for this indication. US December 28, 2012 approved for the reduction of non-valvular atrial fibrillation at risk of stroke and systemic embolism. 
Domestic: an import tablet listing: Bristol-Myers Squibb Manufacturing Compan (Bristol-Myers 
Squibb / Pfizer EEIG) trade name; Ai toremifene. Currently no enterprise reporting. 
Intellectual Property Status: 
Compound international patents: WO2003026652, publication date: 2003-04-03. 
Compound patent in China: CN1578660, the announcement date: 2005-02-09 Patent Expiration Date: 2025-02-09. 
Market outlook: 
Atrial fibrillation is a common irregular heart beat, atrial fibrillation in Europe about 4.5 million, about 2.2 million US in patients with atrial fibrillation China's estimated 800 million, more than the sum of the number of patients in Europe and America. 
By population aging, chronic heart disease has become increasingly common, and other factors, the incidence of atrial fibrillation global surge has become a rapidly growing public health problem, is expected to 2050, the number of patients with atrial fibrillation will increase threefold. In 80 years, every 10 adults will have a person affected by atrial fibrillation. In people over the age of 40, one in four people may have a suffering atrial fibrillation. In China, the adult population aged 30 or above in the prevalence rate of 0.77 percent, about 600-800 million annually due to increased hospitalization in patients with atrial fibrillation, resulting in extremely serious public health burden. 
Drug treatment of atrial fibrillation is the preferred option, atrial fibrillation as a common disease, the treatment has been relatively standardized, usually drug treatment, including the rhythm-control drugs and anti-arrhythmic drugs. In addition, patients often taking anticoagulants, such as warfarin coagulant and anti-platelet drugs such as aspirin, which reduces the risk of stroke. Therefore, the treatment of patients with atrial fibrillation broad stroke and systemic embolism prevention drug market prospects. 
Progress in the development 
our company has completed the synthesis of small test, test, production technology, manufacturers are seeking cooperation.