ndabere

Apixaban bụ onye na-ahọrọ nke ukwuu na onye na-emegharị ihe nke Factor Xa na ụkpụrụ Ki nke 0.08 nM na 0.17 nM na mmadụ na oke bekee, n'otu n'otu [1].

Factor X, makwaara site na eponym Stuart-Prower factor, bụ enzyme nke coagulation cascade. Factor X na-arụ ọrụ, site na hydrolysis, n'ime ihe Xa site na ihe abụọ IX. Factor Xa bụ ụdị arụ ọrụ nke coagulation factor thrombokinase. Inhibiting Factor Xa nwere ike inye ụzọ ọzọ maka mgbochi ọrịa obi. Direct Xa inhibitors bụ ọgwụ mgbochi ọrịa na-ewu ewu [2].

Na vitro: Apixabanhas gosipụtara ọkwa dị elu nke ike, nhọrọ, na arụmọrụ na Factor Xa na Ki nke 0.08 nM na 0.17 nM maka Human Factor Xa na Rabbit Factor Xa, n'otu n'otu [1]. Apixaban na-agbatị oge clotting nke plasma mmadụ nkịtị na ntinye uche (EC2x) nke 3.6, 0.37, 7.4 na 0.4 μM, nke achọrọ iji okpukpu abụọ oge prothrombin (PT), oge prothrombin gbanwere (mPT), oge thromboplastin na-arụ ọrụ. APTT) na HepTest. E wezụga nke ahụ, Apixaban gosipụtara ike kachasị elu na plasma mmadụ na oke bekee, mana obere ike na plasma oke na nkịta na ma nyocha PT na APTT [3].

Na vivo: Apixaban gosipụtara ezigbo pharmacokinetics na nkwụsị dị ala (Cl: 0.02 L kg-1h-1), na obere nkesa nkesa (Vdss: 0.2 L / kg) na nkịta. E wezụga nke ahụ, Apixaban gosikwara ọkara ndụ na T1 / 2 nke 5.8 awa na ezigbo bioavailability ọnụ (F: 58%) [1]. Na thrombosis arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) na ọkụ eletrik na-eme ka carotid arterial thrombosis (ECAT) rabbit ụdị, Apixaban mepụtara mmetụta antithrombotic na EC50 nke 270 nM, 110 nM na 70 nM n'ụzọ dabere na dose [3] ]. Apixaban mechibidoro ọrụ Xa na IC50 nke 0.22 μM na oke bekee ex vivo[4]. Na chimpanzee, Apixaban gosikwara obere nkesa nkesa (Vdss: 0.17 L kg-1), nkwụsịtụ usoro dị ala (Cl: 0.018 L kg-1h-1), na ezigbo bioavailability ọnụ (F: 59%) [5].

Ntụaka:
Pinto DJP, Orwat MJ, Koch S, et al. Nchọpụta nke 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), ike dị ukwuu, nhọrọ, dị irè, na ọnụ ọnụ. bioavailable inhibitor nke ọbara coagulation factor Xa[J]. Akwụkwọ akụkọ chemistry ọgwụ, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors dị ka Anticoagulants[J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, ihe na-emechi ọnụ, kpọmkwem na nke ukwuu nhọrọ Xa inhibitor: in vitro, antithrombotic na antihemostatics [J]. Akwụkwọ akụkọ nke Thrombosis na Hemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics na pharmacodynamics nke ihe Xa inhibitor apixaban na rabbits[J]. Akwụkwọ akụkọ nke thrombosis na thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. Preclinical pharmacokinetics na pharmacodynamics nke apixaban, ihe nwere ike na nhọrọ Xa inhibitor[J]. Akwụkwọ akụkọ Europe nke ọgwụ metabolism na pharmacokinetics, 2011, 36 (3): 129-139.

Apixaban bụ onye na-ahọrọ nke ukwuu na onye na-emegharị ihe nke Factor Xa na ụkpụrụ Ki nke 0.08 nM na 0.17 nM na mmadụ na oke bekee, n'otu n'otu [1].

Factor X, makwaara site na eponym Stuart-Prower factor, bụ enzyme nke coagulation cascade. Factor X na-arụ ọrụ, site na hydrolysis, n'ime ihe Xa site na ihe abụọ IX. Factor Xa bụ ụdị arụ ọrụ nke coagulation factor thrombokinase. Inhibiting Factor Xa nwere ike inye ụzọ ọzọ maka mgbochi ọrịa obi. Direct Xa inhibitors bụ ọgwụ mgbochi ọrịa na-ewu ewu [2].

Na vitro: Apixabanhas gosipụtara ọkwa dị elu nke ike, nhọrọ, na arụmọrụ na Factor Xa na Ki nke 0.08 nM na 0.17 nM maka Human Factor Xa na Rabbit Factor Xa, n'otu n'otu [1]. Apixaban na-agbatị oge clotting nke plasma mmadụ nkịtị na ntinye uche (EC2x) nke 3.6, 0.37, 7.4 na 0.4 μM, nke achọrọ iji okpukpu abụọ oge prothrombin (PT), oge prothrombin gbanwere (mPT), oge thromboplastin na-arụ ọrụ. APTT) na HepTest. E wezụga nke ahụ, Apixaban gosipụtara ike kachasị elu na plasma mmadụ na oke bekee, mana obere ike na plasma oke na nkịta na ma nyocha PT na APTT [3].

Na vivo: Apixaban gosipụtara ezigbo pharmacokinetics na nkwụsị dị ala (Cl: 0.02 L kg-1h-1), na obere nkesa nkesa (Vdss: 0.2 L / kg) na nkịta. E wezụga nke ahụ, Apixaban gosikwara ọkara ndụ na T1 / 2 nke 5.8 awa na ezigbo bioavailability ọnụ (F: 58%) [1]. Na thrombosis arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) na ọkụ eletrik na-eme ka carotid arterial thrombosis (ECAT) rabbit ụdị, Apixaban mepụtara mmetụta antithrombotic na EC50 nke 270 nM, 110 nM na 70 nM n'ụzọ dabere na dose [3] ]. Apixaban mechibidoro ọrụ Xa na IC50 nke 0.22 μM na oke bekee ex vivo[4]. Na chimpanzee, Apixaban gosikwara obere nkesa nkesa (Vdss: 0.17 L kg-1), nkwụsịtụ usoro dị ala (Cl: 0.018 L kg-1h-1), na ezigbo bioavailability ọnụ (F: 59%) [5].

Ntụaka:
Pinto DJP, Orwat MJ, Koch S, et al. Nchọpụta nke 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), ike dị ukwuu, nhọrọ, dị irè, na ọnụ ọnụ. bioavailable inhibitor nke ọbara coagulation factor Xa[J]. Akwụkwọ akụkọ chemistry ọgwụ, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors dị ka Anticoagulants[J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, ihe na-emechi ọnụ, kpọmkwem na nke ukwuu nhọrọ Xa inhibitor: in vitro, antithrombotic na antihemostatics [J]. Akwụkwọ akụkọ nke Thrombosis na Hemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics na pharmacodynamics nke ihe Xa inhibitor apixaban na rabbits[J]. Akwụkwọ akụkọ nke thrombosis na thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al. Preclinical pharmacokinetics na pharmacodynamics nke apixaban, ihe nwere ike na nhọrọ Xa inhibitor[J]. Akwụkwọ akụkọ Europe nke ọgwụ metabolism na pharmacokinetics, 2011, 36 (3): 129-139.

Ọdịdị chemical