Rivaroxaban

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API Lub Npe Kev taw qhia Specification Asmeskas DMF  EU DMF  CEP
Rivaroxaban Anticoagulant Hauv TDP    

Khoom Nthuav dav

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KHOOM NTES

Tom Qab

Rivaroxaban, 5-chloro-N - [[(5S) -2-oxo-3- [4- (3-oxomorpholin-4-yl) phenyl] -1,3-oxazolidin-5-yl] methyl] thiophene-2 -carboxamide, yog ib qho muaj zog-cov roj-molecule inhibitor ntawm factor Xa uas yog qhov teeb meem coagulation ntawm qhov tseem ceeb ntawm cov ntshav ntawm cov ntshav coagulation txoj hauv kev ua rau lub cim ntawm thrombin thiab tsim cov txhaws. Rivaroxaban khi rau Tyr288 hauv S1 hnab tshos ntawm qhov Xa los ntawm kev sib cuam tshuam ntawm Tyr288 thiab chlorine hloov chaw ntawm chlorothiophene moiety. Qhov inhibition yog thim rov qab (koff = 5x10-3s-1), nrawm (kon = 1.7x107 mol / L-1 s-1), thiab nyob rau hauv kev coj ncaj-nyob rau hauv (Ki = 0.4 nmol / L). Rivaroxaban tam sim no tseem tab tom kawm txog kev kho mob VTE, kev tiv thaiv kab mob plawv rau cov neeg mob ntsig txog mob hlab ntsha hlwb, tiv thaiv mob stroke hauv cov neeg mob atrial fibrillation.

Kev siv

Elisabeth Perzborn, Susanne Roehrig, Alexander Straub, Dagmar Kubitza, Wolfgang Mueck, thiab Volker Laux. Rivaroxaban: qhov ncauj tawm tshiab Xa inhibitor. Arterioscler Thromb Vasc Biol 2010; 30 (3): 376-381

Kev piav qhia

Rivaroxaban (BAY 59-7939) yog qhov muaj zog heev,xaiv qhov thiab ncaj qha Factor Xa (FXa) inhibitor, ua tiav lub zog muaj zog tiv thaiv FXa potency (IC50 0.7 nM; Ki 0.4 nM).

 

Hauv Vitro

Rivaroxaban (BAY 59-7939) yog qhov ncauj, ncaj qha Factor Xa (FXa) inhibitor hauv kev txhim kho rau kev tiv thaiv thiab kev kho mob ntawm txoj hlab ntshav thiab txoj hlab ntshav. Rivaroxaban kev sib tw tiv thaiv tib neeg FXa (Ki 0.4 nM) nrog> 10 000-xaiv ntau dua kev xaiv ntau dua rau lwm cov kev pabcuam serine; nws kuj inhibits prothrombinase kev ua haujlwm (IC50 2.1 nM). Rivaroxaban inhibits endogenous FXa ntau zog hauv tib neeg thiab luav ntshav (IC50 21 nM) dua li cov ntshav plasma (IC50 290 nM). Nws qhia txog cov teebmeem anticoagulant hauv tib neeg plasma, ob zaug prothrombin lub sijhawm (PT) thiab ua kom lub sijhawm thromboplastin tsawg dua ntawm 0.23 thiab 0.69μM, ntsig txog.

 

Rivaroxaban (BAY 59-7939) yog qhov muaj zog thiab xaiv, ncaj qha FXa inhibitor nrog zoo heev hauv kev ua haujlwm vivo thiab zoo qhov ncauj bioavailability. Rivaroxaban (BAY 59-7939), tswj hwm los ntawm iv bolus ua ntej thrombus induction, txo qhov kev txhim kho thrombus (ED50 0.1 mg / kg), inhibits FXa, thiab lub sijhawm ntev PT koob tshuaj vam khom. PT thiab FXa cuam tshuam me ntsis ntawm ED50 (1.8-nce ntxiv thiab 32% inhibition, feem). Ntawm 0.3 mg / kg (koob tshuaj uas ua rau yuav luag tiav qhov inhibition ntawm thrombus tsim), Rivaroxaban muaj pes nrab mus ntev PT (3.2±0.5-fold) thiab inhibits FXa kev ua (65±3%).

 

Cia

Hmoov

-20 ° C

3 xyoos
 

4 ° C

2 xyoos
Hauv hnyav

-80 ° C

6 hli
 

-20 ° C

1 hlis

Tshuaj qauv

Rivaroxaban

TXUJ CI NTSEEG

Quality management1

Kev Tawm Tsam 18 Cov Kev Ntsuas Xyuas Kom Zoo Kom Zoo Li Qub uas tau pom zoo 4, thiab 6 tej yaam num yog nyob rau hauv kev pom zoo.

Quality management2

Advanced thoob ntiaj teb zoo tswj system tau tso paus ruaj khov rau kev muag khoom.

Quality management3

Kev saib xyuas kev ua tau zoo khiav thoob plaws lub neej tag nrho ntawm cov khoom kom ntseeg tau tias qhov zoo thiab ua kom zoo. 

Quality management4

Pawg kws tshaj lij ntxawg koom tes txhawb nqa qhov kev xav tau zoo thaum thov thiab sau npe.

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