Apixaban

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Apixaban VTE Mumba

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CHIDZIDZO CHIDZIDZO

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Apixaban inonyanya kusarudza uye inodzosera inhibitor yeFactor Xa nemaKi maitiro e0.08 nM uye 0.17 nM muvanhu netsuro, zvichiteerana [1].

Factor X, inozivikanwawo neiyo eponym Stuart-Prower factor, ndiyo enzyme yeiyo coagulation cascade. Chinhu X chinoshandiswa, nehydrolysis, kuita factor Xa nezvose zviri zviviri IX. Factor Xa ndiyo fomu yakamisikidzwa yecoagulation factorthrombokinase, Inhibiting Factor Xa inogona kupa imwe nzira yeanodzivirira. Direct Xa inhibitors inozivikanwa anticoagulants [2].

In vitro: Apixabanhas yakaratidza huwandu hwesimba, kusarudza, uye kushanda paFactor Xa neKi ye0.08 nM uye 0.17 nM yeHuman Factor Xa uye Rabbit Factor Xa, zvichiteerana [1]. Apixaban yakawedzera nguva dzekugwamba dzeyakajairika plasma yemunhu pamwe nemabatiro (EC2x) e3.6, 0.37, 7.4 uye 0.4 μM, ayo anodikanwa zvakateedzana kuti awedzere iyo prothrombin nguva (PT), yakagadziridzwa prothrombin nguva (mPT), yakamisirwa chikamu chetromboplastin nguva ( APTT) uye HepTest. Kunze kwezvo, Apixaban yakaratidza simba rakakwirira kwazvo muplasma yemunhu uye yetsuro, asi shoma potency mumakonzo nembwa yeplasma mune zvese PT uye APTT zviyero [3].

Mu vivo: Apixaban akaratidzira yakanakisa pharmacokinetics ine yakadzika kwazvo clearance (Cl: 0.02 L kg-1h-1), uye yakaderera vhoriyamu yekuparadzira (Vdss: 0.2 L / kg) imbwa. Kunze kwezvo, Apixaban akaratidzawo zvine mwero hafu-yehupenyu neT1 / 2 maawa 5.8 uye yakanaka yemuromo bioavailability (F: 58%) [1]. Mune arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) uye nemagetsi anogadziriswa carotid arterial thrombosis (ECAT) mhando dzetsuro, Apixaban yakaburitsa antithrombotic mhedzisiro neEC50 ye270 nM, 110 nM uye 70 nM munzira inotarisirwa nedosi [3 ]. Apixaban zvakanyanya kudzivirirwa chinhu Xa chiitiko neIC50 ye0.22 μM muhuro ex vivo [4]. Mune chimpanzi, Apixaban zvakare yakaratidza diki vhoriyamu yekuparadzira (Vdss: 0.17 L kg-1), yakaderera systemic clearance (Cl: 0.018 L kg-1h-1), uye yakanaka yemuromo bioavailability (F: 59%) [5].

Zvinyorwa:
Pinto DJP, Orwat MJ, Koch S, uye al. Kuwanika 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 kwazvo, inosarudza, inoshanda, uye nemuromo isingawanikwe inhibitor yeropa coagulation factor Xa [J]. Zvinyorwa zvemishonga chemistry, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors seAnticoagulants [J].
PC yeWong, Crain EJ, Xin B, et al. Apixaban, yemuromo, yakanangana uye inonyanya kusarudza chinhu Xa inhibitor: in vitro, antithrombotic uye antihemostaticstudies [J]. Zvinyorwa zveThrombosis uye Haemostasis, 2008, 6 (5): 820-829.
Zhang D, Iye K, Raghavan N, et al. Metabolism, pharmacokinetics uye pharmacodynamics yechinhu Xa inhibitor apixaban mumatsuro [J]. Zvinyorwa zve thrombosis uye thrombolysis, 2010, 29 (1): 70-80.
Iye K, Luettgen JM, Zhang D, et al. Preclinical pharmacokinetics uye pharmacodynamics yeapixaban, ine simba uye inosarudza chinhu Xa inhibitor [J]. European magazine yezvinodhaka metabolism uye pharmacokinetics, 2011, 36 (3): 129-139.

Apixaban inonyanya kusarudza uye inodzosera inhibitor yeFactor Xa nemaKi maitiro e0.08 nM uye 0.17 nM muvanhu netsuro, zvichiteerana [1].

Factor X, inozivikanwawo neiyo eponym Stuart-Prower factor, ndiyo enzyme yeiyo coagulation cascade. Chinhu X chinoshandiswa, nehydrolysis, kuita factor Xa nezvose zviri zviviri IX. Factor Xa ndiyo fomu yakamisikidzwa yecoagulation factorthrombokinase, Inhibiting Factor Xa inogona kupa imwe nzira yeanodzivirira. Direct Xa inhibitors inozivikanwa anticoagulants [2].

In vitro: Apixabanhas yakaratidza huwandu hwesimba, kusarudza, uye kushanda paFactor Xa neKi ye0.08 nM uye 0.17 nM yeHuman Factor Xa uye Rabbit Factor Xa, zvichiteerana [1]. Apixaban yakawedzera nguva dzekugwamba dzeyakajairika plasma yemunhu pamwe nemabatiro (EC2x) e3.6, 0.37, 7.4 uye 0.4 μM, ayo anodikanwa zvakateedzana kuti awedzere iyo prothrombin nguva (PT), yakagadziridzwa prothrombin nguva (mPT), yakamisirwa chikamu chetromboplastin nguva ( APTT) uye HepTest. Kunze kwezvo, Apixaban yakaratidza simba rakakwirira kwazvo muplasma yemunhu uye yetsuro, asi shoma potency mumakonzo nembwa yeplasma mune zvese PT uye APTT zviyero [3].

Mu vivo: Apixaban akaratidzira yakanakisa pharmacokinetics ine yakadzika kwazvo clearance (Cl: 0.02 L kg-1h-1), uye yakaderera vhoriyamu yekuparadzira (Vdss: 0.2 L / kg) imbwa. Kunze kwezvo, Apixaban akaratidzawo zvine mwero hafu-yehupenyu neT1 / 2 maawa 5.8 uye yakanaka yemuromo bioavailability (F: 58%) [1]. Mune arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) uye nemagetsi anogadziriswa carotid arterial thrombosis (ECAT) mhando dzetsuro, Apixaban yakaburitsa antithrombotic mhedzisiro neEC50 ye270 nM, 110 nM uye 70 nM munzira inotarisirwa nedosi [3 ]. Apixaban zvakanyanya kudzivirirwa chinhu Xa chiitiko neIC50 ye0.22 μM muhuro ex vivo [4]. Mune chimpanzi, Apixaban zvakare yakaratidza diki vhoriyamu yekuparadzira (Vdss: 0.17 L kg-1), yakaderera systemic clearance (Cl: 0.018 L kg-1h-1), uye yakanaka yemuromo bioavailability (F: 59%) [5].

Zvinyorwa:
Pinto DJP, Orwat MJ, Koch S, uye al. Kuwanika 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 kwazvo, inosarudza, inoshanda, uye nemuromo isingawanikwe inhibitor yeropa coagulation factor Xa [J]. Zvinyorwa zvemishonga chemistry, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors seAnticoagulants [J].
PC yeWong, Crain EJ, Xin B, et al. Apixaban, yemuromo, yakanangana uye inonyanya kusarudza chinhu Xa inhibitor: in vitro, antithrombotic uye antihemostaticstudies [J]. Zvinyorwa zveThrombosis uye Haemostasis, 2008, 6 (5): 820-829.
Zhang D, Iye K, Raghavan N, et al. Metabolism, pharmacokinetics uye pharmacodynamics yechinhu Xa inhibitor apixaban mumatsuro [J]. Zvinyorwa zve thrombosis uye thrombolysis, 2010, 29 (1): 70-80.
Iye K, Luettgen JM, Zhang D, et al. Preclinical pharmacokinetics uye pharmacodynamics yeapixaban, ine simba uye inosarudza chinhu Xa inhibitor [J]. European magazine yezvinodhaka metabolism uye pharmacokinetics, 2011, 36 (3): 129-139.

Chimiro chemakemikari

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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