Special Price for Daclatasvir Plus Sofosbuvir - Apixaban – CPF

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Background

Apixaban is a highly selective and reversible inhibitor of Factor Xa with Ki values of 0.08 nM and 0.17 nM in human and rabbit, respectively[1].

Factor X, also known by the eponym Stuart–Prower factor, is an enzyme of the coagulation cascade. Factor X is activated, by hydrolysis, into factor Xa by both factor IX. Factor Xa is the activated form of the coagulation factorthrombokinase.Inhibiting Factor Xa could offer an alternate method for anticoagulation. Direct Xa inhibitors are popular anticoagulants [2].

In vitro: Apixabanhas exhibited a high degree of potency, selectivity, and efficacy on Factor Xa with Ki of 0.08 nM and 0.17 nM for Human Factor Xa and Rabbit Factor Xa, respectively [1]. Apixaban prolonged the clotting times of normal human plasma with the concentrations (EC2x) of 3.6, 0.37, 7.4 and 0.4 μM, which are required respectively to double the prothrombin time (PT), modified prothrombin time (mPT), activated partial thromboplastin time (APTT) and HepTest. Besides, Apixaban showed the highest potency in human and rabbit plasma, but less potency in rat and dog plasma in both the PT and APTT assays [3].

In vivo: Apixaban exihibited the excellent pharmacokinetics with very low clearance (Cl: 0.02 L kg-1h-1), and low volume of distribution (Vdss: 0.2 L/kg) in the dog. Besides, Apixaban also showed a moderate half-life with T1/2 of 5.8 hours and good oral bioavailability (F: 58%) [1]. In the arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models, Apixaban produced antithrombotic effects with EC50 of 270 nM, 110 nM and 70 nM in a dose-dependent manner[3]. Apixaban significantly inhibited factor Xa activity with an IC50 of 0.22 μM in rabbit ex vivo[4]. In chimpanzee, Apixaban also showed small volume of distribution (Vdss: 0.17 L kg-1), low systemic clearance (Cl: 0.018 L kg-1h-1), and good oral bioavailability (F: 59%) [5].

References:
Pinto D J P, Orwat M J, Koch S, et al. Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl) phenyl)-4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4-c] pyridine-3-carboxamide (Apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa[J]. Journal of medicinal chemistry, 2007, 50(22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors as Anticoagulants[J].
Wong P C, Crain E J, Xin B, et al. Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostaticstudies[J]. Journal of Thrombosis and Haemostasis, 2008, 6(5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics and pharmacodynamics of the factor Xa inhibitor apixaban in rabbits[J]. Journal of thrombosis and thrombolysis, 2010, 29(1): 70-80.
He K, Luettgen J M, Zhang D, et al. Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor[J]. European journal of drug metabolism and pharmacokinetics, 2011, 36(3): 129-139.

Apixaban is a highly selective and reversible inhibitor of Factor Xa with Ki values of 0.08 nM and 0.17 nM in human and rabbit, respectively[1].

Factor X, also known by the eponym Stuart–Prower factor, is an enzyme of the coagulation cascade. Factor X is activated, by hydrolysis, into factor Xa by both factor IX. Factor Xa is the activated form of the coagulation factorthrombokinase.Inhibiting Factor Xa could offer an alternate method for anticoagulation. Direct Xa inhibitors are popular anticoagulants [2].

In vitro: Apixabanhas exhibited a high degree of potency, selectivity, and efficacy on Factor Xa with Ki of 0.08 nM and 0.17 nM for Human Factor Xa and Rabbit Factor Xa, respectively [1]. Apixaban prolonged the clotting times of normal human plasma with the concentrations (EC2x) of 3.6, 0.37, 7.4 and 0.4 μM, which are required respectively to double the prothrombin time (PT), modified prothrombin time (mPT), activated partial thromboplastin time (APTT) and HepTest. Besides, Apixaban showed the highest potency in human and rabbit plasma, but less potency in rat and dog plasma in both the PT and APTT assays [3].

In vivo: Apixaban exihibited the excellent pharmacokinetics with very low clearance (Cl: 0.02 L kg-1h-1), and low volume of distribution (Vdss: 0.2 L/kg) in the dog. Besides, Apixaban also showed a moderate half-life with T1/2 of 5.8 hours and good oral bioavailability (F: 58%) [1]. In the arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models, Apixaban produced antithrombotic effects with EC50 of 270 nM, 110 nM and 70 nM in a dose-dependent manner[3]. Apixaban significantly inhibited factor Xa activity with an IC50 of 0.22 μM in rabbit ex vivo[4]. In chimpanzee, Apixaban also showed small volume of distribution (Vdss: 0.17 L kg-1), low systemic clearance (Cl: 0.018 L kg-1h-1), and good oral bioavailability (F: 59%) [5].

References:
Pinto D J P, Orwat M J, Koch S, et al. Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl) phenyl)-4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4-c] pyridine-3-carboxamide (Apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa[J]. Journal of medicinal chemistry, 2007, 50(22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors as Anticoagulants[J].
Wong P C, Crain E J, Xin B, et al. Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostaticstudies[J]. Journal of Thrombosis and Haemostasis, 2008, 6(5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics and pharmacodynamics of the factor Xa inhibitor apixaban in rabbits[J]. Journal of thrombosis and thrombolysis, 2010, 29(1): 70-80.
He K, Luettgen J M, Zhang D, et al. Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor[J]. European journal of drug metabolism and pharmacokinetics, 2011, 36(3): 129-139.

Chemical structure

Apixaban

2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

OUR STRENGTH

Quality management1

Proposal 18 Quality Consistency Evaluation projects which have approved 4, and 6 projects are under approving.

Quality management2

Advanced international quality management system has laid solid foundation for sales.

Quality management3

Quality supervision runs through the whole life cycle of the product to ensure the quality and therapeutic effect. 

Quality management4

Professional Regulatory Affairs team supports the quality demands during the application and registration.


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We attempt for excellence, provider the customers", hopes to be the most beneficial cooperation team and dominator enterprise for staff, suppliers and shoppers, realizes value share and continuous advertising for Special Price for Daclatasvir Plus Sofosbuvir - Apixaban – CPF , The product will supply to all over the world, such as: Berlin, Egypt, Vietnam, Our company has built stable business relationships with many well-known domestic companies as well as oversea customers. With the goal of providing high quality products to customers at low cots, we are committed to improving its capacities in research, development, manufacturing and management. We have honored to receive recognition from our customers. Till now we have passed ISO9001 in 2005 and ISO/TS16949 in 2008. Enterprises of "quality of survival, the credibility of development" for the purpose, sincerely welcome domestic and foreign businessmen to visit to discuss cooperation.
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    5 Stars By Martin Tesch from Zambia - 2017.08.18 11:04
    A nice supplier in this industry, after a detail and careful discussion, we reached a consensus agreement. Hope that we cooperate smoothly.
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