Apixaban
Keeb kwm
Apixaban yog ib qho kev xaiv zoo heev thiab thim rov qab inhibitor ntawm Factor Xa nrog Ki qhov txiaj ntsig ntawm 0.08 nM thiab 0.17 nM hauv tib neeg thiab luav, raws li [1].
Factor X, tseem paub los ntawm eponym Stuart-Prower factor, yog ib qho enzyme ntawm coagulation cascade. Factor X yog qhib, los ntawm hydrolysis, mus rau hauv yam Xa los ntawm ob qho tib si IX. Factor Xa yog daim ntawv qhib ntawm cov coagulation factorthrombokinase.Inhibiting Factor Xa tuaj yeem muab lwm txoj hauv kev rau kev tiv thaiv coagulation. Direct Xa inhibitors yog nrov anticoagulants [2].
Nyob rau hauv vitro: Apixabanhas tau nthuav tawm cov qib siab ntawm potency, selectivity, thiab kev ua tau zoo ntawm Factor Xa nrog Ki ntawm 0.08 nM thiab 0.17 nM rau Human Factor Xa thiab Rabbit Factor Xa, raws li [1]. Apixaban ncua lub sijhawm ua ntshav ntawm tib neeg cov ntshav nrog cov concentrations (EC2x) ntawm 3.6, 0.37, 7.4 thiab 0.4 μM, uas yuav tsum tau ua raws li ob npaug ntawm lub sijhawm prothrombin (PT), hloov kho lub sijhawm prothrombin (mPT), qhib lub sijhawm thromboplastin ib nrab ( APTT) thiab HepTest. Dhau li ntawd, Apixaban tau pom qhov muaj zog tshaj plaws hauv tib neeg thiab luav plasma, tab sis tsawg dua potency hauv nas thiab dev ntshav hauv ob qho tib si PT thiab APTT kev soj ntsuam [3].
Hauv vivo: Apixaban tau nthuav tawm cov tshuaj pharmacokinetics zoo heev nrog kev tshem tawm tsawg heev (Cl: 0.02 L kg-1h-1), thiab qis ntim ntawm kev faib tawm (Vdss: 0.2 L / kg) hauv tus dev. Tsis tas li ntawd, Apixaban kuj tau pom qhov nruab nrab ib nrab-lub neej nrog T1 / 2 ntawm 5.8 teev thiab qhov ncauj zoo bioavailability (F: 58%) [1]. Hauv arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) thiab hluav taws xob kho mob carotid arterial thrombosis (ECAT) luav qauv, Apixaban tsim cov tshuaj tiv thaiv thrombotic nrog EC50 ntawm 270 nM, 110 nM thiab 70 nM nyob rau hauv kev noj tshuaj[3 ]. Apixaban cuam tshuam ntau yam Xa kev ua haujlwm nrog IC50 ntawm 0.22 μM hauv luav ex vivo[4]. Hauv chimpanzee, Apixaban kuj tau pom qhov ntim me me ntawm kev faib tawm (Vdss: 0.17 L kg-1), kev tshem tawm qis (Cl: 0.018 L kg-1h-1), thiab qhov ncauj zoo bioavailability (F: 59%) [5].
Cov ntaub ntawv:
Pinto DJP, Orwat MJ, Koch S, et al. Kev 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 zog heev, xaiv, ua tau zoo, thiab Qhov ncauj bioavailable inhibitor ntawm ntshav coagulation factor Xa[J]. Phau ntawv Journal of medicinal chemistry, 2007, 50(22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors as Anticoagulants[J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, qhov ncauj, ncaj qha thiab xaiv qhov zoo tshaj Xa inhibitor: hauv vitro, antithrombotic thiab antihemostaticstudies [J]. Phau ntawv Journal of Thrombosis thiab Haemostasis, 2008, 6(5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics thiab pharmacodynamics ntawm qhov tseem ceeb Xa inhibitor apixaban hauv luav [J]. Phau ntawv Journal of thrombosis thiab thrombolysis, 2010, 29(1): 70-80.
He K, Luettgen JM, Zhang D, et al. Preclinical pharmacokinetics thiab pharmacodynamics ntawm apixaban, muaj zog thiab xaiv yam tseem ceeb Xa inhibitor [J]. European Journal of drug metabolism thiab pharmacokinetics, 2011, 36(3): 129-139.
Apixaban yog ib qho kev xaiv zoo heev thiab thim rov qab inhibitor ntawm Factor Xa nrog Ki qhov txiaj ntsig ntawm 0.08 nM thiab 0.17 nM hauv tib neeg thiab luav, raws li [1].
Factor X, tseem paub los ntawm eponym Stuart-Prower factor, yog ib qho enzyme ntawm coagulation cascade. Factor X yog qhib, los ntawm hydrolysis, mus rau hauv yam Xa los ntawm ob qho tib si IX. Factor Xa yog daim ntawv qhib ntawm cov coagulation factorthrombokinase.Inhibiting Factor Xa tuaj yeem muab lwm txoj hauv kev rau kev tiv thaiv coagulation. Direct Xa inhibitors yog nrov anticoagulants [2].
Nyob rau hauv vitro: Apixabanhas tau nthuav tawm cov qib siab ntawm potency, selectivity, thiab kev ua tau zoo ntawm Factor Xa nrog Ki ntawm 0.08 nM thiab 0.17 nM rau Human Factor Xa thiab Rabbit Factor Xa, raws li [1]. Apixaban ncua lub sijhawm ua ntshav ntawm tib neeg cov ntshav nrog cov concentrations (EC2x) ntawm 3.6, 0.37, 7.4 thiab 0.4 μM, uas yuav tsum tau ua raws li ob npaug ntawm lub sijhawm prothrombin (PT), hloov kho lub sijhawm prothrombin (mPT), qhib lub sijhawm thromboplastin ib nrab ( APTT) thiab HepTest. Dhau li ntawd, Apixaban tau pom qhov muaj zog tshaj plaws hauv tib neeg thiab luav plasma, tab sis tsawg dua potency hauv nas thiab dev ntshav hauv ob qho tib si PT thiab APTT kev soj ntsuam [3].
Hauv vivo: Apixaban tau nthuav tawm cov tshuaj pharmacokinetics zoo heev nrog kev tshem tawm tsawg heev (Cl: 0.02 L kg-1h-1), thiab qis ntim ntawm kev faib tawm (Vdss: 0.2 L / kg) hauv tus dev. Tsis tas li ntawd, Apixaban kuj tau pom qhov nruab nrab ib nrab-lub neej nrog T1 / 2 ntawm 5.8 teev thiab qhov ncauj zoo bioavailability (F: 58%) [1]. Hauv arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) thiab hluav taws xob kho mob carotid arterial thrombosis (ECAT) luav qauv, Apixaban tsim cov tshuaj tiv thaiv thrombotic nrog EC50 ntawm 270 nM, 110 nM thiab 70 nM nyob rau hauv kev noj tshuaj[3 ]. Apixaban cuam tshuam ntau yam Xa kev ua haujlwm nrog IC50 ntawm 0.22 μM hauv luav ex vivo[4]. Hauv chimpanzee, Apixaban kuj tau pom qhov ntim me me ntawm kev faib tawm (Vdss: 0.17 L kg-1), kev tshem tawm qis (Cl: 0.018 L kg-1h-1), thiab qhov ncauj zoo bioavailability (F: 59%) [5].
Cov ntaub ntawv:
Pinto DJP, Orwat MJ, Koch S, et al. Kev 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 zog heev, xaiv, ua tau zoo, thiab Qhov ncauj bioavailable inhibitor ntawm ntshav coagulation factor Xa[J]. Phau ntawv Journal of medicinal chemistry, 2007, 50(22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors as Anticoagulants[J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, qhov ncauj, ncaj qha thiab xaiv qhov zoo tshaj Xa inhibitor: hauv vitro, antithrombotic thiab antihemostaticstudies [J]. Phau ntawv Journal of Thrombosis thiab Haemostasis, 2008, 6(5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics thiab pharmacodynamics ntawm qhov tseem ceeb Xa inhibitor apixaban hauv luav [J]. Phau ntawv Journal of thrombosis thiab thrombolysis, 2010, 29(1): 70-80.
He K, Luettgen JM, Zhang D, et al. Preclinical pharmacokinetics thiab pharmacodynamics ntawm apixaban, muaj zog thiab xaiv yam tseem ceeb Xa inhibitor [J]. European Journal of drug metabolism thiab pharmacokinetics, 2011, 36(3): 129-139.
Cov qauv tshuaj
Tswv yim18Quality Consistency Evaluation tej yaam num uas tau pom zoo4, thiab6tej yaam num raug tso cai.
Advanced thoob ntiaj teb kev tswj hwm qhov system tau tso lub hauv paus ruaj khov rau kev muag khoom.
Kev saib xyuas zoo khiav los ntawm tag nrho lub neej voj voog ntawm cov khoom kom ntseeg tau tias qhov zoo thiab kho cov nyhuv.
Pab Pawg Kev Tswj Xyuas Kev Tswj Xyuas Kev Ua Haujlwm txhawb nqa qhov kev xav tau zoo thaum lub sijhawm thov thiab sau npe.
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