China Rivaroxaban tita ati awọn olupese

Rivaroxaban

Apejuwe kukuru:

Orukọ API	Itọkasi	Sipesifikesonu	US DMF	EU DMF	CEP
Rivaroxaban	Anticoagulant	Ninu Ile	TDP

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abẹlẹ

Rivaroxaban, 5-chloro-N-[[(5S)-2-oxo-3-[4- (3-oxomorpholin-4-yl) phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2 -carboxamide, jẹ oludaniloju kekere-molecule ti o lagbara ti ifosiwewe Xa eyiti o jẹ ifosiwewe coagulation ni akoko pataki kan ni ipa ọna coagulation ẹjẹ ti o yorisi iran ti thrombin ati dida didi. Rivaroxaban sopọ mọ Tyr288 ni S1 apo ti ifosiwewe Xa nipasẹ ibaraenisepo ti Tyr288 ati aropo chlorine ti awọn ohun elo chlorothiophene. Idinamọ jẹ iyipada (koff = 5x10-3s-1), ni kiakia (kon = 1.7x107 mol / L-1 s-1), ati ni ọna ti o gbẹkẹle (Ki = 0.4 nmol / L). Rivaroxaban ti wa ni iwadi lọwọlọwọ fun itọju VTE, idena ti awọn iṣẹlẹ inu ọkan ati ẹjẹ ni awọn alaisan ti o ni iṣọn-ẹjẹ iṣọn-ẹjẹ nla, idena ti ikọlu ni awọn alaisan ti o ni fibrillation atrial.

Itọkasi

Elisabeth Perzborn, Susanne Roehrig, Alexander Straub, Dagmar Kubitza, Wolfgang Mueck, ati Volker Laux. Rivaroxaban: ifosiwewe ẹnu tuntun Xa inhibitor. Arterioscler Thromb Vasc Biol 2010; 30 (3): 376-381

Apejuwe

Rivaroxaban (BAY 59-7939) jẹ alagbara pupọ,yiyan ati taara Factor Xa (FXa) inhibitor, iyọrisi anfani ti o lagbara ni agbara anti-FXa (IC50 0.7 nM; Ki 0.4 nM).

Ninu Vitro

Rivaroxaban (BAY 59-7939) jẹ ẹnu, taara Factor Xa (FXa) inhibitor ni idagbasoke fun idena ati itọju ti iṣọn-ẹjẹ ati iṣọn-ẹjẹ. Rivaroxaban ifigagbaga ni idinamọ FXa eniyan (Ki 0.4 nM) pẹlu>10 000-ayan yiyan ti o tobi ju fun awọn proteases serine miiran; o tun ṣe idiwọ iṣẹ ṣiṣe prothrombinase (IC50 2.1 nM). Rivaroxaban ṣe idiwọ FXa endogenous diẹ sii ni agbara ninu eniyan ati pilasima ehoro (IC50 21 nM) ju pilasima eku (IC50 290 nM). O ṣe afihan awọn ipa anticoagulant ni pilasima eniyan, akoko prothrombin ilọpo meji (PT) ati mu akoko thromboplastin apakan ṣiṣẹ ni 0.23 ati 0.69μM, lẹsẹsẹ.

Rivaroxaban (BAY 59-7939) jẹ agbara ati yiyan, inhibitor FXa taara pẹlu didara julọ ni iṣẹ vivo ati bioavailability roba ti o dara. Rivaroxaban (BAY 59-7939), ti a nṣakoso nipasẹ iv bolus ṣaaju ifilọlẹ thrombus, dinku idasile thrombus (ED50 0.1 mg/kg), ṣe idiwọ FXa, ati gigun iwọn lilo PT ni igbẹkẹle. PT ati FXa ni ipa diẹ ni ED50 (ilosoke 1.8-agbo ati 32% idinamọ, lẹsẹsẹ). Ni 0.3 miligiramu / kg (iwọn lilo ti o yori si idinamọ pipe ti iṣelọpọ thrombus), Rivaroxaban ni iwọntunwọnsi pẹ PT (3.2±0.5-agbo) ati idilọwọ iṣẹ FXa (65±3%).

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