Background

Rivaroxaban, 5-chloro-N-[[(5S)-2-oxo-3--[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2 -carboxamide, ine simba diki-molecule inhibitor ye factor Xa inova coagulation factor panguva yakaoma muropa coagulation nzira inokonzeresa chizvarwa. thrombin uye kuumbwa kwevhavha. Rivaroxaban inosungira kuTyr288 muhomwe yeS1 yefactor Xa kuburikidza nekubatana kweTyr288 uye chlorine inotsiva ye chlorothiophene moiety. Iyo inhibition inodzoreredzwa (koff = 5x10-3s-1), nekukurumidza (kon = 1.7x107 mol / L-1 s-1), uye nenzira inotenderera-inotenderera (Ki = 0.4 nmol / L). Rivaroxaban parizvino iri kudzidzwa kurapwa kweVTE, kudzivirira kwezviitiko zvemoyo muvarwere vane acute coronary syndrome, kudzivirira sitiroko kune varwere vane atrial fibrillation.

Reference

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

Tsanangudzo

Rivaroxaban (BAY 59-7939) ine simba zvakanyanya,inosarudza uye yakananga Factor Xa (FXa) inhibitor, kuwana simba rakasimba mu-anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).

In Vitro

Rivaroxaban (BAY 59-7939) ndeyemuromo, yakananga Factor Xa (FXa) inhibitor mukusimudzira kudzivirira uye kurapwa kwe arterial uye venous thrombosis. Rivaroxaban inokwikwidza inhibits FXa yemunhu (Ki 0.4 nM) ne> 10 000-yakakura kusarudza kupfuura kune mamwe serine proteases; inodzivisawo basa reprothrombinase (IC50 2.1 nM). Rivaroxaban inhibits endogenous FXa zvakanyanya zvakanyanya mumunhu uye tsuro plasma (IC50 21 nM) kupfuura rat plasma (IC50 290 nM). Inoratidza anticoagulant mhedzisiro muplasma yevanhu, yakapetwa kaviri prothrombin nguva (PT) uye inomisa chikamu che thromboplastin nguva pa 0.23 uye 0.69μM, zvichiteerana.

Rivaroxaban (BAY 59-7939) ine simba uye inosarudza, yakananga FXa inhibitor ine yakanakisa mu vivo chiitiko uye yakanaka yemuromo bioavailability. Rivaroxaban (BAY 59-7939), inotungamirirwa nev bolus isati yasvika thrombus induction, inoderedza thrombus formation (ED50 0.1 mg / kg), inhibits FXa, uye inowedzera PT dose zvichienderana. PT uye FXa zvinokanganiswa zvishoma paED50 (1.8-fold kuwedzera uye 32% inhibition, maererano). Pa 0.3 mg/kg (dose rinotungamira kunenge kuvharika kwakazara kwekuumbwa kwethrombus), Rivaroxaban zvine mwero inowedzera PT (3.2)±0.5-peta) uye inhibits FXa chiitiko (65±3%).

Storage

Chimiro chemakemikari