Apixaban

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Apixaban yog qhov muaj kev xaiv heev thiab thim rov qab ntawm qhov cuam tshuam Xa nrog Ki qhov tseem ceeb ntawm 0.08 nM thiab 0.17 nM hauv tib neeg thiab luav, feem [1].

Factor X, kuj paub los ntawm eponym Stuart – Prower qhov zoo tshaj, yog ib qho enzyme ntawm coagulation cascade. Factor X yog qhib kom ua, los ntawm hydrolysis, rau hauv Xa Xa los ntawm ob qho ntawm IX. Qhov Xa Xa yog daim ntawv foos ntawm coagulation factorthrombokinase.Inhibiting Factor Xa tuaj yeem muab lwm txoj hauv kev rau cov tshuaj tiv thaiv kev tsis haum. Kev Xa Xa ncaj qha cov tshuaj tiv thaiv yog nrov anticoagulants [2].

Hauv vitro: Apixabanhas nthuav tawm qib siab ntawm lub zog, xaiv tau, thiab ua tau zoo ntawm Factor Xa nrog Ki ntawm 0.08 nM thiab 0.17 nM rau Human Factor Xa thiab Rabbit Factor Xa, feem [1]. Apixaban lub sijhawm ua kom cov ntshav txhaws lub sijhawm ntawm tib neeg plasma nrog cov ntsiab lus (EC2x) ntawm 3.6, 0.37, 7.4 thiab 0.4 μM, uas yuav tsum tau muaj feem ob zaug prothrombin lub sijhawm (PT), hloov lub sijhawm prothrombin (mPT), qhib lub sijhawm thromboplastin lub sijhawm ( APTT) thiab HepTest. Dhau li ntawd, Apixaban pom tias muaj qhov siab tshaj plaws ntawm tib neeg thiab luav ntshav, tab sis tsawg dua potency hauv cov nas thiab dev plasma nyob rau hauv ob qho PT thiab APTT tshaj tawm [3].

Hauv vivo: Apixaban exihibited cov tshuaj muaj txiaj ntsig zoo nrog kev tshem tawm tsawg heev (Cl: 0.02 L kg-1h-1), thiab kev faib tawm tsawg (Vdss: 0.2 L / kg) hauv tus dev. Dhau li ntawm, Apixaban tseem qhia tau tias muaj ib nrab lub neej nrog T1 / 2 ntawm 5.8 teev thiab zoo rau lub qhov ncauj ua kom zoo (F: 58%) [1]. Hauv cov hlab ntsha-shunt thrombosis (AVST), mob rau lub cev (venous thrombosis (VT) thiab hluav taws xob sib kis carotid arterial thrombosis (ECAT) luav qauv, Apixaban tsim cov tshuaj tiv thaiv antithrombotic nrog EC50 ntawm 270 nM, 110 nM thiab 70 nM raws kev siv koob tshuaj [3 ]. Apixaban qhov tseem ceeb tshaj plaws Qhov cuam tshuam Xa kev ua haujlwm nrog IC50 ntawm 0.22 μM hauv luav ex vivo [4]. Hauv qhov chimpanzee, Apixaban kuj pom cov ntim me me ntawm kev faib tawm (Vdss: 0.17 L kg-1), kev ua haujlwm tsis muaj qhov system (Cl: 0.018 L kg-1h-1), thiab qhov ncauj zoo ntawm lub cev (F: 59%) [5].

Chiv keeb:
Pinto DJP, Orwat MJ, Koch S, li al. Tshawb pom ntawm 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), muaj peev xwm heev, xaiv tau zoo, ua haujlwm tau zoo, thiab qhov ncauj ntawm lub cev muaj zog inhibitor ntawm cov ntshav coagulation factor Xa [J]. Phau ntawv teev cov tshuaj muaj tshuaj, 2007, 50 (22): 5339-5356.
Sidhu P S. Cov Khoom Muag Xa Txoj Cai Xa ncaj ncees raws li Anticoagulants [J].
Wong PC, Crain EJ, X B, li al. Apixaban, qhov ncauj, ncaj qha thiab xaiv qhov muaj feem Xa inhibitor: hauv vitro, antithrombotic thiab antihemostaticstudies [J]. Phau ntawv Journal of Thrombosis and Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, li al. Cov roj ntsha, cov tshuaj lag luam tshuaj thiab cov chaw muag tshuaj ntawm lub ntsiab Xa inhibitor apixaban hauv luav [J]. Phau ntawv Journal ntawm thrombosis thiab thrombolysis, 2010, 29 (1): 70-80.
Nws K, Luettgen JM, Zhang D, li al. Precinical pharmacokinetics thiab pharmacodynamics ntawm apixaban, lub zog thiab xaiv qhov tseem ceeb Xa inhibitor [J]. Cov phau ntawv xov xwm European ntawm cov tshuaj metabolism hauv thiab cov tshuaj pharmacokinetics, 2011, 36 (3): 129-139.

Apixaban yog qhov muaj kev xaiv heev thiab thim rov qab ntawm qhov cuam tshuam Xa nrog Ki qhov tseem ceeb ntawm 0.08 nM thiab 0.17 nM hauv tib neeg thiab luav, feem [1].

Factor X, kuj paub los ntawm eponym Stuart – Prower qhov zoo tshaj, yog ib qho enzyme ntawm coagulation cascade. Factor X yog qhib kom ua, los ntawm hydrolysis, rau hauv Xa Xa los ntawm ob qho ntawm IX. Qhov Xa Xa yog daim ntawv foos ntawm coagulation factorthrombokinase.Inhibiting Factor Xa tuaj yeem muab lwm txoj hauv kev rau cov tshuaj tiv thaiv kev tsis haum. Kev Xa Xa ncaj qha cov tshuaj tiv thaiv yog nrov anticoagulants [2].

Hauv vitro: Apixabanhas nthuav tawm qib siab ntawm lub zog, xaiv tau, thiab ua tau zoo ntawm Factor Xa nrog Ki ntawm 0.08 nM thiab 0.17 nM rau Human Factor Xa thiab Rabbit Factor Xa, feem [1]. Apixaban lub sijhawm ua kom cov ntshav txhaws lub sijhawm ntawm tib neeg plasma nrog cov ntsiab lus (EC2x) ntawm 3.6, 0.37, 7.4 thiab 0.4 μM, uas yuav tsum tau muaj feem ob zaug prothrombin lub sijhawm (PT), hloov lub sijhawm prothrombin (mPT), qhib lub sijhawm thromboplastin lub sijhawm ( APTT) thiab HepTest. Dhau li ntawd, Apixaban pom tias muaj qhov siab tshaj plaws ntawm tib neeg thiab luav ntshav, tab sis tsawg dua potency hauv cov nas thiab dev plasma nyob rau hauv ob qho PT thiab APTT tshaj tawm [3].

Hauv vivo: Apixaban exihibited cov tshuaj muaj txiaj ntsig zoo nrog kev tshem tawm tsawg heev (Cl: 0.02 L kg-1h-1), thiab kev faib tawm tsawg (Vdss: 0.2 L / kg) hauv tus dev. Dhau li ntawm, Apixaban tseem qhia tau tias muaj ib nrab lub neej nrog T1 / 2 ntawm 5.8 teev thiab zoo rau lub qhov ncauj ua kom zoo (F: 58%) [1]. Hauv cov hlab ntsha-shunt thrombosis (AVST), mob rau lub cev (venous thrombosis (VT) thiab hluav taws xob sib kis carotid arterial thrombosis (ECAT) luav qauv, Apixaban tsim cov tshuaj tiv thaiv antithrombotic nrog EC50 ntawm 270 nM, 110 nM thiab 70 nM raws kev siv koob tshuaj [3 ]. Apixaban qhov tseem ceeb tshaj plaws Qhov cuam tshuam Xa kev ua haujlwm nrog IC50 ntawm 0.22 μM hauv luav ex vivo [4]. Hauv qhov chimpanzee, Apixaban kuj pom cov ntim me me ntawm kev faib tawm (Vdss: 0.17 L kg-1), kev ua haujlwm tsis muaj qhov system (Cl: 0.018 L kg-1h-1), thiab qhov ncauj zoo ntawm lub cev (F: 59%) [5].

Chiv keeb:
Pinto DJP, Orwat MJ, Koch S, li al. Tshawb pom ntawm 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), muaj peev xwm heev, xaiv tau zoo, ua haujlwm tau zoo, thiab qhov ncauj ntawm lub cev muaj zog inhibitor ntawm cov ntshav coagulation factor Xa [J]. Phau ntawv teev cov tshuaj muaj tshuaj, 2007, 50 (22): 5339-5356.
Sidhu P S. Cov Khoom Muag Xa Txoj Cai Xa ncaj ncees raws li Anticoagulants [J].
Wong PC, Crain EJ, X B, li al. Apixaban, qhov ncauj, ncaj qha thiab xaiv qhov muaj feem Xa inhibitor: hauv vitro, antithrombotic thiab antihemostaticstudies [J]. Phau ntawv Journal of Thrombosis and Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, li al. Cov roj ntsha, cov tshuaj lag luam tshuaj thiab cov chaw muag tshuaj ntawm lub ntsiab Xa inhibitor apixaban hauv luav [J]. Phau ntawv Journal ntawm thrombosis thiab thrombolysis, 2010, 29 (1): 70-80.
Nws K, Luettgen JM, Zhang D, li al. Precinical pharmacokinetics thiab pharmacodynamics ntawm apixaban, lub zog thiab xaiv qhov tseem ceeb Xa inhibitor [J]. Cov phau ntawv xov xwm European ntawm cov tshuaj metabolism hauv thiab cov tshuaj pharmacokinetics, 2011, 36 (3): 129-139.

Tshuaj qauv

Apixaban

TXUJ CI NTSEEG

Quality management1

Kev Tawm Tsam 18 Cov Kev Ntsuas Xyuas Kom Zoo Kom Zoo Li Qub uas tau pom zoo 4, thiab 6 tej yaam num yog nyob rau hauv kev pom zoo.

Quality management2

Advanced thoob ntiaj teb zoo tswj system tau tso paus ruaj khov rau kev muag khoom.

Quality management3

Kev saib xyuas kev ua tau zoo khiav thoob plaws lub neej tag nrho ntawm cov khoom kom ntseeg tau tias qhov zoo thiab ua kom zoo. 

Quality management4

Pawg kws tshaj lij ntxawg koom tes txhawb nqa qhov kev xav tau zoo thaum thov thiab sau npe.

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