Apixaban

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Apixaban VTE Totonu o le Fale

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Apixaban o se sili ona filifilia ma fesuiaʻi le taofiofia o le Factor Xa ma Ki taua o le 0,08 nM ma le 0.17 nM i le tagata ma le lapiti, i le faasologa [1].

Factor X, e lauiloa foi ile igoa ole igoa Stuart – Prower factor, ose enzyme ole coagulation cascade. Vaega X o loʻo faʻagaoioia, e ala i le hydrolysis, i le vaega Xa e ala uma i le itu IX. Factor Xa o le faʻagaina o fomu o le coagulation factorthrombokinase. O le taofiina o le Factor Xa e mafai ona ofoina mai se isi auala mo anticoagulation. O faʻatamaʻi tuusaʻo Xa e taʻutaʻua anticoagulants [2].

In vitro: Apixabanhas faʻaalia le maualuga tikeri o le gafatia, filifilia, ma le aoga i luga o le Factor Xa ma Ki o 0,08 nM ma 0.17 nM mo Human Factor Xa ma Rabbit Factor Xa, faʻatulagaina [1]. Apixaban faaumiumi taimi faʻaputuputuga o masani tagata plasma ma faʻatulagaina (EC2x) o 3.6, 0.37, 7.4 ma 0.4 μM, ia e manaʻomia faʻaluaina le prothrombin taimi (PT), toe faʻaleleia taimi prothrombin (mPT), faʻagaoioia vaega thromboplastin taimi APTT) ma HepTest. E le gata i lea, o Apixaban na faʻaalia le maualuga gafatia i le tagata ma le lapiti plasma, ae laititi le malosi i le rat ma le dog plasma i le PT ma le APTT suʻega [3].

In vivo: Apixaban exihibited sili lelei vailaʻauala ma maualalo maualalo kilia (Cl: 0,02 L kg-1h-1), ma maualalo tele o tufatufaina (Vdss: 0.2 L / kg) i le maile. E le gata i lea, na faʻaalia foi e Apixaban se 'afa afa ola ma le T1 / 2 o le 5.8 itula ma le lelei o le tautala i le tautala (F: 58%) [1]. I le arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) ma le eletise faʻasolosolo o le carotid arterial thrombosis (ECAT) lapiti, na maua ai e Apixaban ni aafiaga antithrombotic ma le EC50 o le 270 nM, 110 nM ma le 70 nM i se auala faʻalagolago i le fua [3 ]. Apixaban na matua taofia le mea taua Xa ma le IC50 o le 0.22 μM i le lapiti ex vivo [4]. I chimpanzee, Apixaban na faʻaalia foi le laʻititi o le tufatufaina (Vdss: 0.17 L kg-1), maualalo le tapunia (Cl: 0,018 L kg-1h-1), ma le lelei o le tautala bioavailability (F: 59%) [5].

Faʻamatalaga:
Pinto DJP, Orwat MJ, Koch S, et al. Mauaina o le 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), o se sili ona malosi, filifilia, aoga, ma tautala faʻaola e faʻatamaia le toto coagulation vaega Xa [J]. Tusi o vailaʻau kemisi, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors o Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, o se tautala, tuusao ma sili ona filifilia Xa mea taofiofia: in vitro, antithrombotic and antihemostaticstudies [J]. Tusi o le Thrombosis ma Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, vailaʻau faʻafomaʻi ma vailaʻau faʻasaina o le mea taua Xa taofiofia apixaban i lapiti [J]. Tusi o le thrombosis ma le thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. Fomaʻi vailaʻau ma vailaʻau mo vailaʻau o le apixaban, o se malosiʻaga ma filifilia ni mea e taofi ai Xa [J]. Tusi a Europa o fualaʻau faʻasaina o vailaʻau ma vailaʻau faʻasaina, 2011, 36 (3): 129-139.

Apixaban o se sili ona filifilia ma fesuiaʻi le taofiofia o le Factor Xa ma Ki taua o le 0,08 nM ma le 0.17 nM i le tagata ma le lapiti, i le faasologa [1].

Factor X, e lauiloa foi ile igoa ole igoa Stuart – Prower factor, ose enzyme ole coagulation cascade. Vaega X o loʻo faʻagaoioia, e ala i le hydrolysis, i le vaega Xa e ala uma i le itu IX. Factor Xa o le faʻagaina o fomu o le coagulation factorthrombokinase. O le taofiina o le Factor Xa e mafai ona ofoina mai se isi auala mo anticoagulation. O faʻatamaʻi tuusaʻo Xa e taʻutaʻua anticoagulants [2].

In vitro: Apixabanhas faʻaalia le maualuga tikeri o le gafatia, filifilia, ma le aoga i luga o le Factor Xa ma Ki o 0,08 nM ma 0.17 nM mo Human Factor Xa ma Rabbit Factor Xa, faʻatulagaina [1]. Apixaban faaumiumi taimi faʻaputuputuga o masani tagata plasma ma faʻatulagaina (EC2x) o 3.6, 0.37, 7.4 ma 0.4 μM, ia e manaʻomia faʻaluaina le prothrombin taimi (PT), toe faʻaleleia taimi prothrombin (mPT), faʻagaoioia vaega thromboplastin taimi APTT) ma HepTest. E le gata i lea, o Apixaban na faʻaalia le maualuga gafatia i le tagata ma le lapiti plasma, ae laititi le malosi i le rat ma le dog plasma i le PT ma le APTT suʻega [3].

In vivo: Apixaban exihibited sili lelei vailaʻauala ma maualalo maualalo kilia (Cl: 0,02 L kg-1h-1), ma maualalo tele o tufatufaina (Vdss: 0.2 L / kg) i le maile. E le gata i lea, na faʻaalia foi e Apixaban se 'afa afa ola ma le T1 / 2 o le 5.8 itula ma le lelei o le tautala i le tautala (F: 58%) [1]. I le arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) ma le eletise faʻasolosolo o le carotid arterial thrombosis (ECAT) lapiti, na maua ai e Apixaban ni aafiaga antithrombotic ma le EC50 o le 270 nM, 110 nM ma le 70 nM i se auala faʻalagolago i le fua [3 ]. Apixaban na matua taofia le mea taua Xa ma le IC50 o le 0.22 μM i le lapiti ex vivo [4]. I chimpanzee, Apixaban na faʻaalia foi le laʻititi o le tufatufaina (Vdss: 0.17 L kg-1), maualalo le tapunia (Cl: 0,018 L kg-1h-1), ma le lelei o le tautala bioavailability (F: 59%) [5].

Faʻamatalaga:
Pinto DJP, Orwat MJ, Koch S, et al. Mauaina o le 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), o se sili ona malosi, filifilia, aoga, ma tautala faʻaola e faʻatamaia le toto coagulation vaega Xa [J]. Tusi o vailaʻau kemisi, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors o Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, o se tautala, tuusao ma sili ona filifilia Xa mea taofiofia: in vitro, antithrombotic and antihemostaticstudies [J]. Tusi o le Thrombosis ma Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, vailaʻau faʻafomaʻi ma vailaʻau faʻasaina o le mea taua Xa taofiofia apixaban i lapiti [J]. Tusi o le thrombosis ma le thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. Fomaʻi vailaʻau ma vailaʻau mo vailaʻau o le apixaban, o se malosiʻaga ma filifilia ni mea e taofi ai Xa [J]. Tusi a Europa o fualaʻau faʻasaina o vailaʻau ma vailaʻau faʻasaina, 2011, 36 (3): 129-139.

Fausaga o vailaʻau

Apixaban

FAUTUAINA

2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

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