Background

Apixaban inosarudzika uye inodzoreredzwa inhibitor yeFactor Xa ine Ki values ​​dze0.08 nM uye 0.17 nM mumunhu netsuro, zvichiteerana[1].

Factor X, inozivikanwawo neiyo eponym Stuart-Prower factor, ienzyme yeiyo coagulation cascade.Factor X inobatiswa, ne hydrolysis, kuita factor Xa nezvose zviri zviviri factor IX.Factor Xa is the activated form of the coagulation factorthrombokinase.Inhibiting Factor Xa inogona kupa imwe nzira yeanticoagulation.Direct Xa inhibitors anozivikanwa anticoagulants [2].

In vitro: Apixabanhas yakaratidza chiyero chepamusoro chesimba, kusarudza, uye kushanda paFactor Xa ine Ki ye 0.08 nM uye 0.17 nM yeHuman Factor Xa uye Rabbit Factor Xa, maererano [1].Apixaban yakawedzera nguva yekuvhara kweplasma yemunhu yakajairwa nehuwandu (EC2x) ye3.6, 0.37, 7.4 uye 0.4 μM, iyo inodiwa zvakateerana kupeta nguva yeprothrombin (PT), yakagadziridzwa prothrombin nguva (mPT), activated partial thromboplastin time ( APTT) uye HepTest.Kunze kwezvo, Apixaban yakaratidza simba repamusoro-soro muplasma yevanhu uye tsuro, asi simba shoma mumakonzo uye imbwa plasma mune zvose PT uye APTT assays [3].

In vivo: Apixaban yakaratidza yakanakisa pharmacokinetics ine yakaderera kwazvo clearance (Cl: 0.02 L kg-1h-1), uye yakaderera vhoriyamu yekugovera (Vdss: 0.2 L / kg) mumbwa.Kunze kwezvo, Apixaban yakaratidzawo mwero hafu yehupenyu neT1 / 2 yemaawa 5.8 uye yakanaka yemuromo bioavailability (F: 58%) [1].Mu arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) uye magetsi akapindirana carotid arterial thrombosis (ECAT) tsuro modhi, Apixaban yakagadzira antithrombotic mhedzisiro neEC50 ye270 nM, 110 nM uye 70 nM nenzira inotsamira mudosi [3. ].Apixaban yakanyanya inhibited factor Xa chiitiko neIC50 ye0.22 μM mu tsuro ex vivo[4].Muchimpanzee, Apixaban yakaratidzawo kugoverwa kuduku (Vdss: 0.17 L kg-1), pasi systemic clearance (Cl: 0.018 L kg-1h-1), uye yakanaka yemuromo bioavailability (F: 59%) [5].

References:
Pinto DJP, Orwat MJ, Koch S, et al.Kuwanikwa kwe1-(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), ine simba, inosarudza, inoshanda, uye nemuromo bioavailable inhibitor yeropa coagulation factor Xa[J].Nyaya yemishonga yemakemikari, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors seAnticoagulants[J].
Wong PC, Crain EJ, Xin B, et al.Apixaban, yemuromo, yakananga uye yakanyanya kusarudza chinhu Xa inhibitor: in vitro, antithrombotic uye antihemostaticstudies[J].Nyaya yeThrombosis uye Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al.Metabolism, pharmacokinetics uye pharmacodynamics yefactor Xa inhibitor apixaban mutsuro[J].Nyaya ye thrombosis uye thrombolysis, 2010, 29 (1): 70-80.
Iye K, Luettgen JM, Zhang D, et al.Preclinical pharmacokinetics uye pharmacodynamics yeapixaban, ine simba uye yakasarudzwa chinhu Xa inhibitor[J].European Journal yezvinodhaka metabolism uye pharmacokinetics, 2011, 36 (3): 129-139.

Apixaban inosarudzika uye inodzoreredzwa inhibitor yeFactor Xa ine Ki values ​​dze0.08 nM uye 0.17 nM mumunhu netsuro, zvichiteerana[1].

Factor X, inozivikanwawo neiyo eponym Stuart-Prower factor, ienzyme yeiyo coagulation cascade.Factor X inobatiswa, ne hydrolysis, kuita factor Xa nezvose zviri zviviri factor IX.Factor Xa is the activated form of the coagulation factorthrombokinase.Inhibiting Factor Xa inogona kupa imwe nzira yeanticoagulation.Direct Xa inhibitors anozivikanwa anticoagulants [2].

In vitro: Apixabanhas yakaratidza chiyero chepamusoro chesimba, kusarudza, uye kushanda paFactor Xa ine Ki ye 0.08 nM uye 0.17 nM yeHuman Factor Xa uye Rabbit Factor Xa, maererano [1].Apixaban yakawedzera nguva yekuvhara kweplasma yemunhu yakajairwa nehuwandu (EC2x) ye3.6, 0.37, 7.4 uye 0.4 μM, iyo inodiwa zvakateerana kupeta nguva yeprothrombin (PT), yakagadziridzwa prothrombin nguva (mPT), activated partial thromboplastin time ( APTT) uye HepTest.Kunze kwezvo, Apixaban yakaratidza simba repamusoro-soro muplasma yevanhu uye tsuro, asi simba shoma mumakonzo uye imbwa plasma mune zvose PT uye APTT assays [3].

In vivo: Apixaban yakaratidza yakanakisa pharmacokinetics ine yakaderera kwazvo clearance (Cl: 0.02 L kg-1h-1), uye yakaderera vhoriyamu yekugovera (Vdss: 0.2 L / kg) mumbwa.Kunze kwezvo, Apixaban yakaratidzawo mwero hafu yehupenyu neT1 / 2 yemaawa 5.8 uye yakanaka yemuromo bioavailability (F: 58%) [1].Mu arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) uye magetsi akapindirana carotid arterial thrombosis (ECAT) tsuro modhi, Apixaban yakagadzira antithrombotic mhedzisiro neEC50 ye270 nM, 110 nM uye 70 nM nenzira inotsamira mudosi [3. ].Apixaban yakanyanya inhibited factor Xa chiitiko neIC50 ye0.22 μM mu tsuro ex vivo[4].Muchimpanzee, Apixaban yakaratidzawo kugoverwa kuduku (Vdss: 0.17 L kg-1), pasi systemic clearance (Cl: 0.018 L kg-1h-1), uye yakanaka yemuromo bioavailability (F: 59%) [5].

References:
Pinto DJP, Orwat MJ, Koch S, et al.Kuwanikwa kwe1-(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), ine simba, inosarudza, inoshanda, uye nemuromo bioavailable inhibitor yeropa coagulation factor Xa[J].Nyaya yemishonga yemakemikari, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors seAnticoagulants[J].
Wong PC, Crain EJ, Xin B, et al.Apixaban, yemuromo, yakananga uye yakanyanya kusarudza chinhu Xa inhibitor: in vitro, antithrombotic uye antihemostaticstudies[J].Nyaya yeThrombosis uye Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al.Metabolism, pharmacokinetics uye pharmacodynamics yefactor Xa inhibitor apixaban mutsuro[J].Nyaya ye thrombosis uye thrombolysis, 2010, 29 (1): 70-80.
Iye K, Luettgen JM, Zhang D, et al.Preclinical pharmacokinetics uye pharmacodynamics yeapixaban, ine simba uye yakasarudzwa chinhu Xa inhibitor[J].European Journal yezvinodhaka metabolism uye pharmacokinetics, 2011, 36 (3): 129-139.

Chimiro chemakemikari