Apixaban

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Orukọ API Itọkasi Sipesifikesonu US DMF EU DMF CEP
Apixaban VTE Ninu Ile

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Lẹhin

Apixaban jẹ yiyan ti o ga julọ ati onidena iparọ ti Factor Xa pẹlu awọn iye Ki ti 0.08 nM ati 0.17 nM ninu eniyan ati ehoro, lẹsẹsẹ [1].

Ifosiwewe X, ti a tun mọ nipasẹ eponym Stuart – Prower ifosiwewe, jẹ enzymu ti kasulu coagulation. Ti mu ifosiwewe X ṣiṣẹ, nipasẹ hydrolysis, sinu ifosiwewe Xa nipasẹ ifosiwewe IX mejeeji. Ifosiwewe Xa jẹ fọọmu ti a mu ṣiṣẹ ti ifosiwewe coagulationthrombokinase. Idinamọ ifosiwewe Xa le funni ni ọna miiran fun anticoagulation. Awọn oludena Direct Xa jẹ awọn egboogi egboogi ti o gbajumọ [2].

In vitro: Apixabanhas ṣe afihan agbara giga, yiyan, ati ipa lori Factor Xa pẹlu Ki ti 0.08 nM ati 0.17 nM fun Ifosiwewe Eniyan Xa ati Ehoro ifosiwewe Xa, lẹsẹsẹ [1]. Apixaban pẹ awọn akoko didi ti pilasima eniyan deede pẹlu awọn ifọkansi (EC2x) ti 3.6, 0.37, 7.4 ati 0.4 μM, eyiti o nilo ni atẹle lati ṣe ilọpo meji akoko prothrombin (PT), akoko prothrombin ti a tunṣe (mPT), ti ṣiṣẹ apakan akoko thromboplastin apakan ( APTT) ati HepTest. Yato si, Apixaban fihan agbara ti o ga julọ ninu pilasima eniyan ati ehoro, ṣugbọn agbara ti o kere si eku ati pilasima aja ni awọn ayẹwo PT ati APTT [3].

Ni vivo: Apixaban yọ awọn oogun-oogun ti o dara julọ pẹlu imukuro kekere pupọ (Cl: 0.02 L kg-1h-1), ati iwọn kekere ti pinpin (Vdss: 0.2 L / kg) ninu aja. Yato si, Apixaban tun fihan idaji-aye ti o dara pẹlu T1 / 2 ti awọn wakati 5.8 ati bioavailability ti o dara (F: 58%) [1]. Ninu iṣọn-ẹjẹ arteriovenous-shunt (AVST), thrombosis iṣọn-ẹjẹ (VT) ati awọn awoṣe ehoro ti o ni ilaja eleto itanna (ECAT), Apixaban ṣe awọn ipa antithrombotic pẹlu EC50 ti 270 nM, 110 nM ati 70 nM ni ọna igbẹkẹle iwọn lilo [3 ]. Apixaban dawọle idiwọ ifosiwewe iṣẹ Xa pẹlu IC50 ti 0.22 μM ni ehoro ex vivo [4]. Ni chimpanzee, Apixaban tun fihan iwọn kekere ti pinpin (Vdss: 0.17 L kg-1), kiliaransi eto eleyi (Cl: 0.018 L kg-1h-1), ati bioavailability ti o dara (F: 59%) [5].

Awọn itọkasi:
Pinto DJP, Orwat MJ, Koch S, et al. Awari ti 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), agbara ti o ga julọ, yiyan, imunadoko, ati onidena bioavailable bioa ti ifosiwewe coagulation ẹjẹ Xa [J]. Iwe akosile ti kemistri ti oogun, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Awọn oludena bi Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, ẹnu, taara ati ifosiwewe yiyan yiyan Xa onidena: in vitro, antithrombotic ati antihemostaticstudies [J]. Iwe akosile ti Thrombosis ati Haemostasis, 2008, 6 (5): 820-829.
Zhang D, Oun K, Raghavan N, et al. Iṣelọpọ, ilana oogun ati ilana oogun ti ifosiwewe Xa onidena apixaban ninu awọn ehoro [J]. Iwe akọọlẹ ti thrombosis ati thrombolysis, 2010, 29 (1): 70-80.
Oun K, Luettgen JM, Zhang D, et al. Iṣeduro oogun iṣaaju ati oogun-oogun ti apixaban, ifosiwewe ti o lagbara ati ti o yan Xa onidena [J]. Iwe iroyin European ti iṣelọpọ ti oogun ati oogun-oogun, 2011, 36 (3): 129-139.

Apixaban jẹ yiyan ti o ga julọ ati onidena iparọ ti Factor Xa pẹlu awọn iye Ki ti 0.08 nM ati 0.17 nM ninu eniyan ati ehoro, lẹsẹsẹ [1].

Ifosiwewe X, ti a tun mọ nipasẹ eponym Stuart – Prower ifosiwewe, jẹ enzymu ti kasulu coagulation. Ti mu ifosiwewe X ṣiṣẹ, nipasẹ hydrolysis, sinu ifosiwewe Xa nipasẹ ifosiwewe IX mejeeji. Ifosiwewe Xa jẹ fọọmu ti a mu ṣiṣẹ ti ifosiwewe coagulationthrombokinase. Idinamọ ifosiwewe Xa le funni ni ọna miiran fun anticoagulation. Awọn oludena Direct Xa jẹ awọn egboogi egboogi ti o gbajumọ [2].

In vitro: Apixabanhas ṣe afihan agbara giga, yiyan, ati ipa lori Factor Xa pẹlu Ki ti 0.08 nM ati 0.17 nM fun Ifosiwewe Eniyan Xa ati Ehoro ifosiwewe Xa, lẹsẹsẹ [1]. Apixaban pẹ awọn akoko didi ti pilasima eniyan deede pẹlu awọn ifọkansi (EC2x) ti 3.6, 0.37, 7.4 ati 0.4 μM, eyiti o nilo ni atẹle lati ṣe ilọpo meji akoko prothrombin (PT), akoko prothrombin ti a tunṣe (mPT), ti ṣiṣẹ apakan akoko thromboplastin apakan ( APTT) ati HepTest. Yato si, Apixaban fihan agbara ti o ga julọ ninu pilasima eniyan ati ehoro, ṣugbọn agbara ti o kere si eku ati pilasima aja ni awọn ayẹwo PT ati APTT [3].

Ni vivo: Apixaban yọ awọn oogun-oogun ti o dara julọ pẹlu imukuro kekere pupọ (Cl: 0.02 L kg-1h-1), ati iwọn kekere ti pinpin (Vdss: 0.2 L / kg) ninu aja. Yato si, Apixaban tun fihan idaji-aye ti o dara pẹlu T1 / 2 ti awọn wakati 5.8 ati bioavailability ti o dara (F: 58%) [1]. Ninu iṣọn-ẹjẹ arteriovenous-shunt (AVST), thrombosis iṣọn-ẹjẹ (VT) ati awọn awoṣe ehoro ti o ni ilaja eleto itanna (ECAT), Apixaban ṣe awọn ipa antithrombotic pẹlu EC50 ti 270 nM, 110 nM ati 70 nM ni ọna igbẹkẹle iwọn lilo [3 ]. Apixaban dawọle idiwọ ifosiwewe iṣẹ Xa pẹlu IC50 ti 0.22 μM ni ehoro ex vivo [4]. Ni chimpanzee, Apixaban tun fihan iwọn kekere ti pinpin (Vdss: 0.17 L kg-1), kiliaransi eto eleyi (Cl: 0.018 L kg-1h-1), ati bioavailability ti o dara (F: 59%) [5].

Awọn itọkasi:
Pinto DJP, Orwat MJ, Koch S, et al. Awari ti 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), agbara ti o ga julọ, yiyan, imunadoko, ati onidena bioavailable bioa ti ifosiwewe coagulation ẹjẹ Xa [J]. Iwe akosile ti kemistri ti oogun, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Awọn oludena bi Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, ẹnu, taara ati ifosiwewe yiyan yiyan Xa onidena: in vitro, antithrombotic ati antihemostaticstudies [J]. Iwe akosile ti Thrombosis ati Haemostasis, 2008, 6 (5): 820-829.
Zhang D, Oun K, Raghavan N, et al. Iṣelọpọ, ilana oogun ati ilana oogun ti ifosiwewe Xa onidena apixaban ninu awọn ehoro [J]. Iwe akọọlẹ ti thrombosis ati thrombolysis, 2010, 29 (1): 70-80.
Oun K, Luettgen JM, Zhang D, et al. Iṣeduro oogun iṣaaju ati oogun-oogun ti apixaban, ifosiwewe ti o lagbara ati ti o yan Xa onidena [J]. Iwe iroyin European ti iṣelọpọ ti oogun ati oogun-oogun, 2011, 36 (3): 129-139.

Ilana kemikali

Apixaban

Iwe-ẹri

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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