Kāpae

Rivaroxaban, 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2 -carboxamide, he mea hoʻopaneʻe liʻiliʻi liʻiliʻi ikaika o ka factor Xa he kumu coagulation i kahi manawa koʻikoʻi i ke ala coagulation koko e hopena ai i ka hana o ka thrombin a me ka hoʻokumu ʻana o ka clot. Hoʻopaʻa ʻo Rivaroxaban i ka Tyr288 ma ka ʻeke S1 o ka helu Xa ma o ka launa pū ʻana o Tyr288 a me ka chlorine substituent o ka chlorothiophene moiety. Hiki ke hoʻohuli ʻia ka inhibition (koff = 5x10-3s-1), wikiwiki (kon = 1.7x107 mol/L-1 s-1), a ma ke ʻano hilinaʻi (Ki = 0.4 nmol/L). Ke aʻo ʻia nei ʻo Rivaroxaban no ka mālama ʻana i ka VTE, ka pale ʻana i nā hanana cardiovascular i nā poʻe maʻi me ka maʻi coronary acute, ka pale ʻana i ka hahau i nā maʻi me ka fibrillation atrial.

Kuhikuhi

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

wehewehe

ʻO Rivaroxaban (BAY 59-7939) kahi mea ikaika loa，koho a pololei Factor Xa (FXa) inhibitor, e loaʻa i ka ikaika loaʻa i ka anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).

In Vitro

ʻO Rivaroxaban (BAY 59-7939) he waha, pololei Factor Xa (FXa) inhibitor i ka hoʻomohala ʻana no ka pale ʻana a me ka mālama ʻana i ka thrombosis arterial a me venous. ʻO Rivaroxaban ka hoʻokūkū hoʻokūkū i ka FXa kanaka (Ki 0.4 nM) me ka> 10 000-fold ka koho nui aʻe ma mua o nā proteases serine; ke pale aku nei i ka hana prothrombinase (IC50 2.1 nM). Rivaroxaban inhibits endogenous FXa oi potently i loko o kanaka a me ka rabbit plasma (IC50 21 nM) ma mua o rat plasma (IC50 290 nM). Hōʻike ia i nā hopena anticoagulant i loko o ka plasma kanaka, pālua ka manawa prothrombin (PT) a hoʻāla i ka manawa thromboplastin hapa ma 0.23 a me 0.69μM, kēlā me kēia.

ʻO Rivaroxaban (BAY 59-7939) he mea ikaika a koho, kuhikuhi FXa inhibitor me ka maikaʻi o ka hana vivo a me ka bioavailability waha. Rivaroxaban (BAY 59-7939), lawelawe ʻia e iv bolus ma mua o ka hoʻokomo ʻana i ka thrombus, hoʻemi i ka hoʻokumu ʻana o ka thrombus (ED50 0.1 mg / kg), hoʻopaʻa i ka FXa, a hoʻolōʻihi i ka dosis PT ma muli o ka hilinaʻi. Hoʻopilikia iki ʻia ʻo PT a me FXa i ka ED50 (1.8-fold piʻi a me 32% inhibition, kēlā me kēia). Ma ka 0.3 mg / kg (ka hopena e alakaʻi i ka hoʻopau piha ʻana i ka hoʻokumu ʻana o ka thrombus), hoʻolōʻihi ʻia ʻo Rivaroxaban i ka PT (3.2±0.5-fold) a pale i ka hana FXa (65±3%).

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