Apixaban

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Ingoa o API Tohu Whakatakotoranga US DMF EU DMF CEP
Apixaban VTE I-Roto

Taipitopito Hua

Tohu Hua

WHAKAWEHE KOREUTU

Papamuri

Ko te Apixaban he kaiwhakawhiwhi tino whiriwhiri me te whakahoki i te Factor Xa me nga uara Ki o 0,08 nM me te 0.17 nM o te tangata me te koni, [1].

Factor X, e mohiotia ana e te ingoa ingoa Stuart – Prower factor, he hauropi mo te cascade coagulation. Tauwehenga X kua whakahohehia, na te waahora, ki te tauwehenga Xa e te waahanga IX. Factor Xa te momo whakahohe o te coagulation factrombrombokinase. Ko te aukati i te Factor Xa ka taea te whakaputa i tetahi atu tikanga mo te anticoagulation. Ko nga aukati Direct Xa he anticoagulants rongonui [2].

I roto i te vitro: I whakaatuhia e Apixabanhas te kaha nui, te kowhiri, me te whaihua ki te Factor Xa me te Ki o te 0,08 nM me te 0.17 nM mo te Tangata Tangata Xa me te Raiti Raina Xa, [1]. I roa a Apixaban i nga wa whakakakahu o te plasma tangata noa me nga kukū (EC2x) o 3.6, 0.37, 7.4 me 0.4 μM, e hiahiatia ana kia taarua te waa prothrombin (PT), te wa prothrombin whakarereke (mPT), te wa e whakaohohia ana te wa thromboplastin ( APTT) me HepTest. I tua atu, i whakaatu a Apixaban i te kaha nui o te plasma tangata me te koni, engari he iti ake te kaha o te kiore me te kuri plasma i roto i nga whakamatautau PT me APTT [3].

In vivo: I whakaputahia e Apixaban nga rongoa rongoa rongoa pai me te maamaa iti (Cl: 0,02 L kg-1h-1), me te rahinga o te tohatoha (Vdss: 0.2 L / kg) kei roto i te kuri. Ano hoki, i whakaatuhia e Apixaban te haurua haurua o te ora me te T1 / 2 o te 5.8 haora me te koiora koiora a-waha (F: 58%) [1]. I roto i te thrombosis arteriovenous-shunt (AVST), te venous thrombosis (VT) me te tauira o te carotid arterial thrombosis (ECAT) tauira rapeti, i whakaputahia e Apixaban nga hua antithrombotic me EC50 o 270 nM, 110 nM me 70 nM i runga i te tikanga rongoa horopeta [3 ]. Ko te Apixaban te aukati i te mahi Xa me te IC50 o te 0.22 μM o te koni ex vivo [4]. I roto i te chimpanzee, i whakaatuhia e Apixaban te rahinga iti o te tohatoha (Vdss: 0.17 L kg-1), te maamaatanga iti (Cl: 0,018 L kg-1h-1), me te koiora koiora a-waha (F: 59%) [5].

Tohutoro:
Pinto DJP, Orwat MJ, Koch S, et al. Te kitenga o te 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), he tino kaha, whiriwhiri, whai hua, me te aukati i te koiora a-waha o te tauwehenga toto totohe Xa [J]. Tuhinga o te matū rongoa, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors hei Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, he aukati, he tika, he tino whiriwhiri i te Xa aukati: in vitro, antithrombotic and antihemostaticstudies [J]. Tuhinga o Thrombosis me Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, rongoa rongoa me nga rongoa rongoa rongoa o te take Xa aukati apixaban i roto i nga rapeti [J]. Tuhinga o mua me te thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. Nga rongoa rongoa rongoa me nga rongoa rongoa o te apixaban, he tino kaha me te kowhiri i te Xa aukati [J]. Pukapuka a te Pakeha mo te paukino me te rongoora rongoa, 2011, 36 (3): 129-139.

Ko te Apixaban he kaiwhakawhiwhi tino whiriwhiri me te whakahoki i te Factor Xa me nga uara Ki o 0,08 nM me te 0.17 nM o te tangata me te koni, [1].

Factor X, e mohiotia ana e te ingoa ingoa Stuart – Prower factor, he hauropi mo te cascade coagulation. Tauwehenga X kua whakahohehia, na te waahora, ki te tauwehenga Xa e te waahanga IX. Factor Xa te momo whakahohe o te coagulation factrombrombokinase. Ko te aukati i te Factor Xa ka taea te whakaputa i tetahi atu tikanga mo te anticoagulation. Ko nga aukati Direct Xa he anticoagulants rongonui [2].

I roto i te vitro: I whakaatuhia e Apixabanhas te kaha nui, te kowhiri, me te whaihua ki te Factor Xa me te Ki o te 0,08 nM me te 0.17 nM mo te Tangata Tangata Xa me te Raiti Raina Xa, [1]. I roa a Apixaban i nga wa whakakakahu o te plasma tangata noa me nga kukū (EC2x) o 3.6, 0.37, 7.4 me 0.4 μM, e hiahiatia ana kia taarua te waa prothrombin (PT), te wa prothrombin whakarereke (mPT), te wa e whakaohohia ana te wa thromboplastin ( APTT) me HepTest. I tua atu, i whakaatu a Apixaban i te kaha nui o te plasma tangata me te koni, engari he iti ake te kaha o te kiore me te kuri plasma i roto i nga whakamatautau PT me APTT [3].

In vivo: I whakaputahia e Apixaban nga rongoa rongoa rongoa pai me te maamaa iti (Cl: 0,02 L kg-1h-1), me te rahinga o te tohatoha (Vdss: 0.2 L / kg) kei roto i te kuri. Ano hoki, i whakaatuhia e Apixaban te haurua haurua o te ora me te T1 / 2 o te 5.8 haora me te koiora koiora a-waha (F: 58%) [1]. I roto i te thrombosis arteriovenous-shunt (AVST), te venous thrombosis (VT) me te tauira o te carotid arterial thrombosis (ECAT) tauira rapeti, i whakaputahia e Apixaban nga hua antithrombotic me EC50 o 270 nM, 110 nM me 70 nM i runga i te tikanga rongoa horopeta [3 ]. Ko te Apixaban te aukati i te mahi Xa me te IC50 o te 0.22 μM o te koni ex vivo [4]. I roto i te chimpanzee, i whakaatuhia e Apixaban te rahinga iti o te tohatoha (Vdss: 0.17 L kg-1), te maamaatanga iti (Cl: 0,018 L kg-1h-1), me te koiora koiora a-waha (F: 59%) [5].

Tohutoro:
Pinto DJP, Orwat MJ, Koch S, et al. Te kitenga o te 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), he tino kaha, whiriwhiri, whai hua, me te aukati i te koiora a-waha o te tauwehenga toto totohe Xa [J]. Tuhinga o te matū rongoa, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors hei Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, he aukati, he tika, he tino whiriwhiri i te Xa aukati: in vitro, antithrombotic and antihemostaticstudies [J]. Tuhinga o Thrombosis me Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, rongoa rongoa me nga rongoa rongoa rongoa o te take Xa aukati apixaban i roto i nga rapeti [J]. Tuhinga o mua me te thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. Nga rongoa rongoa rongoa me nga rongoa rongoa o te apixaban, he tino kaha me te kowhiri i te Xa aukati [J]. Pukapuka a te Pakeha mo te paukino me te rongoora rongoa, 2011, 36 (3): 129-139.

Hanganga matū

Apixaban

WHAKAMAHI

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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