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Apixaban jẹ oludaniloju ti o yan pupọ ati iyipada ti Factor Xa pẹlu awọn iye Ki ti 0.08 nM ati 0.17 nM ninu eniyan ati ehoro, lẹsẹsẹ [1].

Factor X, ti a tun mọ nipasẹ eponym Stuart–Prower ifosiwewe, jẹ enzymu ti kasikedi coagulation. Factor X ti mu ṣiṣẹ, nipasẹ hydrolysis, sinu ifosiwewe Xa nipasẹ mejeeji ifosiwewe IX. Factor Xa jẹ fọọmu ti a mu ṣiṣẹ ti coagulation factorthrombokinase. Idinku Factor Xa le funni ni ọna miiran fun anticoagulation. Awọn oludena Xa taara jẹ awọn oogun apakokoro ti o gbajumọ [2].

In vitro: Apixabanhas ṣe afihan iwọn giga ti agbara, yiyan, ati ipa lori Factor Xa pẹlu Ki ti 0.08 nM ati 0.17 nM fun Eda Eniyan Xa ati Ehoro Factor Xa, lẹsẹsẹ [1]. Apixaban ṣe gigun awọn akoko didi ti pilasima eniyan deede pẹlu awọn ifọkansi (EC2x) ti 3.6, 0.37, 7.4 ati 0.4 μM, eyiti o nilo ni atele lati ṣe ilọpo meji akoko prothrombin (PT), akoko prothrombin ti a yipada (mPT), akoko thromboplastin apakan ti mu ṣiṣẹ ( APTT) ati HepTest. Yato si, Apixaban ṣe afihan agbara ti o ga julọ ninu eniyan ati pilasima ehoro, ṣugbọn agbara ti o dinku ni eku ati pilasima aja ni mejeeji awọn idanwo PT ati APTT [3].

Ni vivo: Apixaban ṣe afihan pharmacokinetics ti o dara julọ pẹlu imukuro kekere (Cl: 0.02 L kg-1h-1), ati iwọn kekere ti pinpin (Vdss: 0.2 L / kg) ninu aja. Yato si, Apixaban tun ṣe afihan igbesi aye idaji iwọntunwọnsi pẹlu T1 / 2 ti awọn wakati 5.8 ati bioavailability oral ti o dara (F: 58%) [1]. Ninu thrombosis arteriovenous-shunt (AVST), iṣọn-ẹjẹ iṣọn-ẹjẹ (VT) ati awọn awoṣe ehoro carotid arterial thrombosis (ECAT) ti itanna, Apixaban ṣe awọn ipa antithrombotic pẹlu EC50 ti 270 nM, 110 nM ati 70 nM ni ọna ti o gbẹkẹle iwọn lilo [3] ]. Apixaban ṣe idiwọ iṣẹ Xa ifosiwewe ni pataki pẹlu IC50 ti 0.22 μM ni ehoro ex vivo[4]. Ni chimpanzee, Apixaban tun ṣe afihan iwọn kekere ti pinpin (Vdss: 0.17 L kg-1), imukuro eto kekere (Cl: 0.018 L kg-1h-1), ati bioavailability oral ti o dara (F: 59%) [5].

Awọn itọkasi:
Pinto DJP, Orwat MJ, Koch S, et al. Awari ti 1- (4-methoxyphenyl) -7-oxo-6- (4- (2-oxopiperidin-1-yl) phenyl) -4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4- c] pyridine-3-carboxamide (Apixaban, BMS-562247), ti o lagbara pupọ, yiyan, ti o munadoko, ati ẹnu onidalẹkun bioavailable ti ẹjẹ coagulation ifosiwewe Xa[J]. Iwe akosile ti kemistri oogun, 2007, 50 (22): 5339-5356.
Sidhu P S. Taara ifosiwewe Xa inhibitors bi Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, ohun ẹnu, taara ati yiyan ifosiwewe Xa inhibitor: in vitro, antithrombotic ati antihemostaticstudies[J]. Iwe akosile ti Thrombosis ati Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics ati pharmacodynamics ti ifosiwewe Xa inhibitor apixaban ninu awọn ehoro[J]. Iwe akosile ti thrombosis ati thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. Pharmacokinetics preclinical ati pharmacodynamics ti apixaban, agbara ati yiyan ifosiwewe Xa inhibitor[J]. Iwe akọọlẹ European ti iṣelọpọ oogun ati awọn oogun oogun, 2011, 36 (3): 129-139.

Apixaban jẹ oludaniloju ti o yan pupọ ati iyipada ti Factor Xa pẹlu awọn iye Ki ti 0.08 nM ati 0.17 nM ninu eniyan ati ehoro, lẹsẹsẹ [1].

Factor X, ti a tun mọ nipasẹ eponym Stuart–Prower ifosiwewe, jẹ enzymu ti kasikedi coagulation. Factor X ti mu ṣiṣẹ, nipasẹ hydrolysis, sinu ifosiwewe Xa nipasẹ mejeeji ifosiwewe IX. Factor Xa jẹ fọọmu ti a mu ṣiṣẹ ti coagulation factorthrombokinase. Idinku Factor Xa le funni ni ọna miiran fun anticoagulation. Awọn oludena Xa taara jẹ awọn oogun apakokoro ti o gbajumọ [2].

In vitro: Apixabanhas ṣe afihan iwọn giga ti agbara, yiyan, ati ipa lori Factor Xa pẹlu Ki ti 0.08 nM ati 0.17 nM fun Eda Eniyan Xa ati Ehoro Factor Xa, lẹsẹsẹ [1]. Apixaban ṣe gigun awọn akoko didi ti pilasima eniyan deede pẹlu awọn ifọkansi (EC2x) ti 3.6, 0.37, 7.4 ati 0.4 μM, eyiti o nilo ni atele lati ṣe ilọpo meji akoko prothrombin (PT), akoko prothrombin ti a yipada (mPT), akoko thromboplastin apakan ti mu ṣiṣẹ ( APTT) ati HepTest. Yato si, Apixaban ṣe afihan agbara ti o ga julọ ninu eniyan ati pilasima ehoro, ṣugbọn agbara ti o dinku ni eku ati pilasima aja ni mejeeji awọn idanwo PT ati APTT [3].

Ni vivo: Apixaban ṣe afihan pharmacokinetics ti o dara julọ pẹlu imukuro kekere (Cl: 0.02 L kg-1h-1), ati iwọn kekere ti pinpin (Vdss: 0.2 L / kg) ninu aja. Yato si, Apixaban tun ṣe afihan igbesi aye idaji iwọntunwọnsi pẹlu T1 / 2 ti awọn wakati 5.8 ati bioavailability oral ti o dara (F: 58%) [1]. Ninu thrombosis arteriovenous-shunt (AVST), iṣọn-ẹjẹ iṣọn-ẹjẹ (VT) ati awọn awoṣe ehoro carotid arterial thrombosis (ECAT) ti itanna, Apixaban ṣe awọn ipa antithrombotic pẹlu EC50 ti 270 nM, 110 nM ati 70 nM ni ọna ti o gbẹkẹle iwọn lilo [3] ]. Apixaban ṣe idiwọ iṣẹ Xa ifosiwewe ni pataki pẹlu IC50 ti 0.22 μM ni ehoro ex vivo[4]. Ni chimpanzee, Apixaban tun ṣe afihan iwọn kekere ti pinpin (Vdss: 0.17 L kg-1), imukuro eto kekere (Cl: 0.018 L kg-1h-1), ati bioavailability oral ti o dara (F: 59%) [5].

Awọn itọkasi:
Pinto DJP, Orwat MJ, Koch S, et al. Awari ti 1- (4-methoxyphenyl) -7-oxo-6- (4- (2-oxopiperidin-1-yl) phenyl) -4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4- c] pyridine-3-carboxamide (Apixaban, BMS-562247), ti o lagbara pupọ, yiyan, ti o munadoko, ati ẹnu onidalẹkun bioavailable ti ẹjẹ coagulation ifosiwewe Xa[J]. Iwe akosile ti kemistri oogun, 2007, 50 (22): 5339-5356.
Sidhu P S. Taara ifosiwewe Xa inhibitors bi Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, ohun ẹnu, taara ati yiyan ifosiwewe Xa inhibitor: in vitro, antithrombotic ati antihemostaticstudies[J]. Iwe akosile ti Thrombosis ati Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics ati pharmacodynamics ti ifosiwewe Xa inhibitor apixaban ninu awọn ehoro[J]. Iwe akosile ti thrombosis ati thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. Pharmacokinetics preclinical ati pharmacodynamics ti apixaban, agbara ati yiyan ifosiwewe Xa inhibitor[J]. Iwe akọọlẹ European ti iṣelọpọ oogun ati awọn oogun oogun, 2011, 36 (3): 129-139.

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