Apixaban

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Apixaban ke inhibitor e khethang le e ka fetoloang haholo ea Factor Xa e nang le litekanyetso tsa Ki tsa 0.08 nM le 0.17 nM ho motho le mmutla, ka ho latellana [1].

Factor X, eo hape e tsejoang ka lebitso la Stuart – Prower factor, ke enzyme ea phallo ea coagulation. Ntlha X e kentsoe tšebetsong ke hydrolysis, hore e be factor Xa ka bobeli ba factor IX. Factor Xa ke mofuta o sebelisitsoeng oa coagulation factorthrombokinase. Ho thibela Factor Xa ho ka fana ka mokhoa o mong oa anticoagulation. Direct Xa inhibitors ke li-anticoagulants tse tsebahalang [2].

In vitro: Apixabanhas e bonts'itse matla a mangata, khetho, le ts'ebetso ho Factor Xa le Ki ea 0.08 nM le 0.17 nM bakeng sa Human Factor Xa le Rabbit Factor Xa, ka ho latellana [1]. Apixaban e lelefalitse linako tse koalang tsa plasma e tloaelehileng ea motho ka likhakanyo (EC2x) tsa 3.6, 0.37, 7.4 le 0.4 μM, tse hlokoang ka ho latellana ho pheta nako ea prothrombin (PT), e fetotsoeng nako ea prothrombin (mPT), e sebelisitsoeng nako ea karoloana ea thromboplastin ( APTT) le HepTest. Ntle ho moo, Apixaban o bontšitse matla a phahameng ka ho fetisisa maling a batho le a mmutla, empa a fokola haholo ka lero la lero la ntja le la ntja ho liteko tsa PT le APTT [3] ka bobeli.

In vivo: Apixaban o hlahisitse li-pharmacokinetics tse ntle haholo tse nang le tumello e tlase haholo (Cl: 0.02 L kg-1h-1), le palo e tlase ea kabo (Vdss: 0.2 L / kg) ka ntja. Ntle le moo, Apixaban o boetse a bonts'a halofo ea bophelo bo itekanetseng le T1 / 2 ea lihora tsa 5.8 le bioavailability e ntle ea molomo (F: 58%) [1]. Ho arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) le meetso ea mebutlanyana ea carotid arterial thrombosis (ECAT), Apixaban e hlahisitse litlamorao tsa antithrombotic le EC50 ea 270 nM, 110 nM le 70 nM ka mokhoa o itšetlehileng ka tekanyetso [3] ]. Apixaban e thibela tšebetso ea factor Xa ka IC50 ea 0.22 μM ka mmutlanyana ex vivo [4]. Ho chimpanzee, Apixaban hape o bontšitse palo e nyane ea kabo (Vdss: 0.17 L kg-1), clearance system clearance (Cl: 0.018 L kg-1h-1), le bioavailability e ntle ea molomo (F: 59%) [5].

Litšupiso:
Pinto DJP, Orwat MJ, Koch S, le al. Ho sibolloa ha 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), inhibitor e matla haholo, e khethang, e sebetsang hantle le e sa bonoeng ka molomo ea coagulation factor Xa [J]. Journal ea k'hemistri ea bongaka, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors joalo ka li-Anticoagulants [J].
PC ea Wong, Crain EJ, Xin B, et al. Apixaban, molomo, o tobileng le o khethang haholo Xa inhibitor: in vitro, antithrombotic and antihemostaticstudies [J]. Tlaleho ea Thrombosis le Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, le al. Metabolism, pharmacokinetics le pharmacodynamics ea factor Xa inhibitor apixaban ho mebutlanyana [J]. Tlaleho ea thrombosis le thrombolysis, 2010, 29 (1): 70-80.
Eena K, Luettgen JM, Zhang D, et al. Preclinical pharmacokinetics le pharmacodynamics ea apixaban, ntho e matla le e khethollang Xa inhibitor [J]. Koranta ea Europe ea metabolism ea lithethefatsi le pharmacokinetics, 2011, 36 (3): 129-139.

Apixaban ke inhibitor e khethang le e ka fetoloang haholo ea Factor Xa e nang le litekanyetso tsa Ki tsa 0.08 nM le 0.17 nM ho motho le mmutla, ka ho latellana [1].

Factor X, eo hape e tsejoang ka lebitso la Stuart – Prower factor, ke enzyme ea phallo ea coagulation. Ntlha X e kentsoe tšebetsong ke hydrolysis, hore e be factor Xa ka bobeli ba factor IX. Factor Xa ke mofuta o sebelisitsoeng oa coagulation factorthrombokinase. Ho thibela Factor Xa ho ka fana ka mokhoa o mong oa anticoagulation. Direct Xa inhibitors ke li-anticoagulants tse tsebahalang [2].

In vitro: Apixabanhas e bonts'itse matla a mangata, khetho, le ts'ebetso ho Factor Xa le Ki ea 0.08 nM le 0.17 nM bakeng sa Human Factor Xa le Rabbit Factor Xa, ka ho latellana [1]. Apixaban e lelefalitse linako tse koalang tsa plasma e tloaelehileng ea motho ka likhakanyo (EC2x) tsa 3.6, 0.37, 7.4 le 0.4 μM, tse hlokoang ka ho latellana ho pheta nako ea prothrombin (PT), e fetotsoeng nako ea prothrombin (mPT), e sebelisitsoeng nako ea karoloana ea thromboplastin ( APTT) le HepTest. Ntle ho moo, Apixaban o bontšitse matla a phahameng ka ho fetisisa maling a batho le a mmutla, empa a fokola haholo ka lero la lero la ntja le la ntja ho liteko tsa PT le APTT [3] ka bobeli.

In vivo: Apixaban o hlahisitse li-pharmacokinetics tse ntle haholo tse nang le tumello e tlase haholo (Cl: 0.02 L kg-1h-1), le palo e tlase ea kabo (Vdss: 0.2 L / kg) ka ntja. Ntle le moo, Apixaban o boetse a bonts'a halofo ea bophelo bo itekanetseng le T1 / 2 ea lihora tsa 5.8 le bioavailability e ntle ea molomo (F: 58%) [1]. Ho arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) le meetso ea mebutlanyana ea carotid arterial thrombosis (ECAT), Apixaban e hlahisitse litlamorao tsa antithrombotic le EC50 ea 270 nM, 110 nM le 70 nM ka mokhoa o itšetlehileng ka tekanyetso [3] ]. Apixaban e thibela tšebetso ea factor Xa ka IC50 ea 0.22 μM ka mmutlanyana ex vivo [4]. Ho chimpanzee, Apixaban hape o bontšitse palo e nyane ea kabo (Vdss: 0.17 L kg-1), clearance system clearance (Cl: 0.018 L kg-1h-1), le bioavailability e ntle ea molomo (F: 59%) [5].

Litšupiso:
Pinto DJP, Orwat MJ, Koch S, le al. Ho sibolloa ha 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), inhibitor e matla haholo, e khethang, e sebetsang hantle le e sa bonoeng ka molomo ea coagulation factor Xa [J]. Journal ea k'hemistri ea bongaka, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors joalo ka li-Anticoagulants [J].
PC ea Wong, Crain EJ, Xin B, et al. Apixaban, molomo, o tobileng le o khethang haholo Xa inhibitor: in vitro, antithrombotic and antihemostaticstudies [J]. Tlaleho ea Thrombosis le Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, le al. Metabolism, pharmacokinetics le pharmacodynamics ea factor Xa inhibitor apixaban ho mebutlanyana [J]. Tlaleho ea thrombosis le thrombolysis, 2010, 29 (1): 70-80.
Eena K, Luettgen JM, Zhang D, et al. Preclinical pharmacokinetics le pharmacodynamics ea apixaban, ntho e matla le e khethollang Xa inhibitor [J]. Koranta ea Europe ea metabolism ea lithethefatsi le pharmacokinetics, 2011, 36 (3): 129-139.

Sebopeho sa lik'hemik'hale

Apixaban

NTHATISI

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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