Apixaban

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Ka inoa o API Hōʻike Hoakaka US DMF EU DMF CEP
Apixaban VTE Ma-Hale

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Papa kāʻei kua

ʻO Apixaban kahi mea koho a me ka mea hiki ke hoʻoliʻiliʻi pono o Factor Xa me nā waiwai Ki o 0,08 nM a me 0.17 nM i loko o ke kanaka a me ka lāpaki, [1].

ʻO ka mea X, i ʻike ʻia e ka huaʻōlelo ʻo Stuart – Prower factor, kahi enzyme o ka cascade coagulation. Hoʻokomo ʻia ka X kumu, e ka hydrolysis, i ka helu Xa e nā helu IX. ʻO Factor Xa ke ʻano i hoʻohele ʻia o ka coagulation factorthrombokinase. Hiki i ka Factor Xa ke hāʻawi i kahi ʻano ʻē aʻe no ka anticoagulation. ʻO nā mea kuhikuhi pololei Xa nā anticoagulants [2] kaulana.

In vitro: Ua hōʻike ʻo Apixabanhas i kahi kiʻekiʻe o ka potency, selectivity, a me ka pono ma Factor Xa me Ki o 0.08 nM a me 0.17 nM no Human Factor Xa a me Rabbit Factor Xa, i kēlā me kēia [1]. Ua hoʻolōʻihi ʻo Apixaban i nā manawa ʻōpala o ka plasma kanaka maʻamau me nā concentrations (EC2x) o 3.6, 0.37, 7.4 a me 0.4 μM, e koi ʻia i kēlā me kēia e pālua i ka manawa prothrombin (PT), manawa prothrombin i hoʻololi ʻia (mPT), hoʻoiho i ka manawa thromboplastin hapa APTT) a me HepTest. Ma waho aʻe, ua hōʻike ʻo Apixaban i ka mana kiʻekiʻe loa ma ka plasma kanaka a me ka lāpaki, akā ʻoi aku ka liʻiliʻi o ka ikaika i ka plasma iole a me ka ʻīlio i nā hoʻokolohua PT a me APTT [3].

In vivo: Ua hana ʻo Apixaban i nā lāʻau lapaʻau maikaʻi loa me ka ʻae haʻahaʻa loa (Cl: 0.02 L kg-1h-1), a me ka haʻahaʻa o ka hāʻawi (Vdss: 0.2 L / kg) i ka ʻīlio. Ma waho aʻe, ua hōʻike ʻo Apixaban i kahi hapalua hapalua o ke ola me T1 / 2 o 5.8 mau hola a me ka bioavailability waha maikaʻi (F: 58%) [1]. I loko o ka thrombosis arteriovenous-shunt (AVST), thrombosis venous thrombosis (VT) a me nā electronics mediator carotid thrombosis (ECAT), hana ʻo Apixaban i nā hopena antithrombotic me EC50 o 270 nM, 110 nM a me 70 nM i kahi ʻano hilinaʻi lāʻau [3 ]. Ua kāohi nui ʻo Apixaban i ka hana Xa me kahi IC50 o 0.22 μM ma ka rabbit ex vivo [4]. I ka chimpanzee, ua hōʻike pū ʻo Apixaban i ka liʻiliʻi o ka hāʻawi (Vdss: 0.17 L kg-1), ka hoʻoliʻiliʻi ʻōnaehana haʻahaʻa (Cl: 0.018 L kg-1h-1), a me ka bioavailability waha maikaʻi (F: 59%) [5].

Nā kūmole:
Pinto DJP, Orwat MJ, Koch S, et al. ʻIke o 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), kahi mea ikaika loa, koho, pono, a me ka mea kūwaho bioavailable oral of factor coagulation koko Xa [J]. Ka puke pai o ke kelekema lāʻau, 2007, 50 (22): 5339-5356.
ʻO Sidhu P S. Direct Factor Xa Inhibitors ma ke ʻano he Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. ʻO Apixaban, kahi mea waha, kuhikuhi a me ke koho pono Xa mea kāohi: in vitro, antithrombotic and antihemostaticstudies [J]. Ka Nupepa o Thrombosis a me Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. ʻO ka metabolism, pharmokokinetics a me nā pharmodnamnamics o ka mea Xa mea pāpā i ka apixaban i nā lāpaki [J]. Ka puke pai o thrombosis a me thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. ʻO nā pharmacokinetics preclinical a me nā pharmacodynamics o apixaban, kahi mana a me ke koho Xa mea kāohi [J]. Nūpepa ʻEulopa o ka hoʻokuʻi lāʻau a me nā pharmacokinetics, 2011, 36 (3): 129-139.

ʻO Apixaban kahi mea koho a me ka mea hiki ke hoʻoliʻiliʻi pono o Factor Xa me nā waiwai Ki o 0,08 nM a me 0.17 nM i loko o ke kanaka a me ka lāpaki, [1].

ʻO ka mea X, i ʻike ʻia e ka huaʻōlelo ʻo Stuart – Prower factor, kahi enzyme o ka cascade coagulation. Hoʻokomo ʻia ka X kumu, e ka hydrolysis, i ka helu Xa e nā helu IX. ʻO Factor Xa ke ʻano i hoʻohele ʻia o ka coagulation factorthrombokinase. Hiki i ka Factor Xa ke hāʻawi i kahi ʻano ʻē aʻe no ka anticoagulation. ʻO nā mea kuhikuhi pololei Xa nā anticoagulants [2] kaulana.

In vitro: Ua hōʻike ʻo Apixabanhas i kahi kiʻekiʻe o ka potency, selectivity, a me ka pono ma Factor Xa me Ki o 0.08 nM a me 0.17 nM no Human Factor Xa a me Rabbit Factor Xa, i kēlā me kēia [1]. Ua hoʻolōʻihi ʻo Apixaban i nā manawa ʻōpala o ka plasma kanaka maʻamau me nā concentrations (EC2x) o 3.6, 0.37, 7.4 a me 0.4 μM, e koi ʻia i kēlā me kēia e pālua i ka manawa prothrombin (PT), manawa prothrombin i hoʻololi ʻia (mPT), hoʻoiho i ka manawa thromboplastin hapa APTT) a me HepTest. Ma waho aʻe, ua hōʻike ʻo Apixaban i ka mana kiʻekiʻe loa ma ka plasma kanaka a me ka lāpaki, akā ʻoi aku ka liʻiliʻi o ka ikaika i ka plasma iole a me ka ʻīlio i nā hoʻokolohua PT a me APTT [3].

In vivo: Ua hana ʻo Apixaban i nā lāʻau lapaʻau maikaʻi loa me ka ʻae haʻahaʻa loa (Cl: 0.02 L kg-1h-1), a me ka haʻahaʻa o ka hāʻawi (Vdss: 0.2 L / kg) i ka ʻīlio. Ma waho aʻe, ua hōʻike ʻo Apixaban i kahi hapalua hapalua o ke ola me T1 / 2 o 5.8 mau hola a me ka bioavailability waha maikaʻi (F: 58%) [1]. I loko o ka thrombosis arteriovenous-shunt (AVST), thrombosis venous thrombosis (VT) a me nā electronics mediator carotid thrombosis (ECAT), hana ʻo Apixaban i nā hopena antithrombotic me EC50 o 270 nM, 110 nM a me 70 nM i kahi ʻano hilinaʻi lāʻau [3 ]. Ua kāohi nui ʻo Apixaban i ka hana Xa me kahi IC50 o 0.22 μM ma ka rabbit ex vivo [4]. I ka chimpanzee, ua hōʻike pū ʻo Apixaban i ka liʻiliʻi o ka hāʻawi (Vdss: 0.17 L kg-1), ka hoʻoliʻiliʻi ʻōnaehana haʻahaʻa (Cl: 0.018 L kg-1h-1), a me ka bioavailability waha maikaʻi (F: 59%) [5].

Nā kūmole:
Pinto DJP, Orwat MJ, Koch S, et al. ʻIke o 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), kahi mea ikaika loa, koho, pono, a me ka mea kūwaho bioavailable oral of factor coagulation koko Xa [J]. Ka puke pai o ke kelekema lāʻau, 2007, 50 (22): 5339-5356.
ʻO Sidhu P S. Direct Factor Xa Inhibitors ma ke ʻano he Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. ʻO Apixaban, kahi mea waha, kuhikuhi a me ke koho pono Xa mea kāohi: in vitro, antithrombotic and antihemostaticstudies [J]. Ka Nupepa o Thrombosis a me Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. ʻO ka metabolism, pharmokokinetics a me nā pharmodnamnamics o ka mea Xa mea pāpā i ka apixaban i nā lāpaki [J]. Ka puke pai o thrombosis a me thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. ʻO nā pharmacokinetics preclinical a me nā pharmacodynamics o apixaban, kahi mana a me ke koho Xa mea kāohi [J]. Nūpepa ʻEulopa o ka hoʻokuʻi lāʻau a me nā pharmacokinetics, 2011, 36 (3): 129-139.

ʻAno kemika

Apixaban

CERTIFICATE

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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