New Fashion Design for Doxycycline Hyclate 100mg Tablets - Rivaroxaban – CPF

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Background

Rivaroxaban, 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide, is a potent small-molecule inhibitor of factor Xa which is a coagulation factor at a critical juncture in the blood coagulation pathway resulting in the generation of thrombin and the formation of clot. Rivaroxaban binds to the Tyr288 in S1 pocket of factor Xa through the interaction of Tyr288 and the chlorine substituent of the chlorothiophene moiety. The inhibition is reversible (koff = 5×10-3s-1), rapid (kon = 1.7×107 mol/L-1 s-1), and in a concentration-dependent manner (Ki = 0.4 nmol/L). Rivaroxaban is currently being studied for the treatment of VTE, prevention of cardiovascular events in patients with acute coronary syndrome, prevention of stroke in patients with atrial fibrillation.

Reference

Elisabeth Perzborn, Susanne Roehrig, Alexander Straub, Dagmar Kubitza, Wolfgang Mueck, and Volker Laux. Rivaroxaban: a new oral factor Xa inhibitor. Arterioscler Thromb Vasc Biol 2010; 30(3): 376-381

Description

Rivaroxaban (BAY 59-7939) is a highly potent,selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).

 

In Vitro

Rivaroxaban (BAY 59-7939) is an oral, direct Factor Xa (FXa) inhibitor in development for the prevention and treatment of arterial and venous thrombosis. Rivaroxaban competitively inhibits human FXa (Ki 0.4 nM) with >10 000-fold greater selectivity than for other serine proteases; it also inhibits prothrombinase activity (IC50 2.1 nM). Rivaroxaban inhibits endogenous FXa more potently in human and rabbit plasma (IC50 21 nM) than rat plasma (IC50 290 nM). It demonstrates anticoagulant effects in human plasma, doubling prothrombin time (PT) and activates partial thromboplastin time at 0.23 and 0.69 μM, respectively.

 

Rivaroxaban (BAY 59-7939) is a potent and selective, direct FXa inhibitor with excellent in vivo activity and good oral bioavailability. Rivaroxaban (BAY 59-7939), administered by i.v. bolus before thrombus induction, reduces thrombus formation (ED50 0.1 mg/kg), inhibits FXa, and prolongs PT dose dependently. PT and FXa are affected slightly at the ED50 (1.8-fold increase and 32% inhibition, respectively). At 0.3 mg/kg (dose leading to almost complete inhibition of thrombus formation), Rivaroxaban moderately prolongs PT (3.2±0.5-fold) and inhibits FXa activity (65±3%).

 

Storage

Powder

-20°C

3 years
 

4°C

2 years
In solvent

-80°C

6 months
 

-20°C

1 month

Chemical structure

Rivaroxaban

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

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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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New Fashion Design for Doxycycline Hyclate 100mg Tablets - Rivaroxaban  – CPF detail pictures


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Our items are commonly identified and trusted by people and can fulfill repeatedly altering economic and social wants of New Fashion Design for Doxycycline Hyclate 100mg Tablets - Rivaroxaban – CPF , The product will supply to all over the world, such as: Guyana, Miami, Cologne, Based on experienced engineers, all orders for drawing-based or sample-based processing are welcomed. We have won a good reputation for outstanding customer service among our overseas customers. We will continue to try the best to offer you good quality products and the best service. We are looking forward to serving you.
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