Ticagrelor

Short Bayani:

Sunan API Nuni Musammantawa US DMF  EU DMF  CEP
Ticagrelor Anticoagulant Cikin-Gida 28984  

Bayanin Samfura

Alamar samfur

CIKAKKEN BAYANI

Bayan Fage

Ticagrelor abokin gaba ne na mai karɓar mai karɓar P2Y12 [1].

An ruwaito Ticagrelor don hana tasirin prothrombotic na ADP akan platelet ta hanyar karɓar mai karɓar P2Y12. Ticagrelor ya nuna cikakken hanawar tarawar platelet ex vivo. Bugu da kari Ticagrelor ya ba da shawarar hana dogaro da ƙwayar platelet a cikin ɗan adam. Baya ga waɗannan, Ticagrelor ya kuma nuna magana ta baki, mai ƙarfi, mai rikitarwa mai rikitarwa. Ba kamar sauran masu hanawa ba, Ticagrelor ya kuma bayar da rahoton hana mai karɓar P2Y12 ba tare da canjin rayuwa ba. Bayan wannan, Ticagrelor shine wakili na farko na maganin platelet na tayenopyridine kuma yawanci CYP3A4 da CYP2C19 ne suka inganta shi.

Nassoshi:
[1] Zhou D1, Andersson TB, Grimm SW. In vitro kimantawa na yiwuwar hulɗar miyagun ƙwayoyi-hulɗa da miyagun ƙwayoyi tare da ticagrelor: cytochrome P450 reaction phenotyping, hanawa, shigar da abu, da bambancin jijiyoyin jiki. Magungunan ƙwayoyi na Metab. 2011 Apr; 39 (4): 703-10.
[2] Li Y1, Landqvist C, Grimm SW. Bayyanawa da haɓaka metabolism na ticagrelor, wani ɗan littafin mai karɓar mai karɓar P2Y12, a cikin ɓeraye, beraye, da marmosets. Magungunan ƙwayoyi na Metab. 2011 Satumba; 39 (9): 1555-67. Doi: 10.1124 / dmd.111.039669. Epub 2011 Jun 13.

Bayani

Ticagrelor (AZD6140) shine mai karɓar mai karɓar mai karɓa na P2Y12 don maganin tarawar platelet.

A cikin Vitro

Ticagrelor yana haɓaka mafi girman hana adenosine 5'-diphosphate (ADP)-jawo Ca2 + saki a cikin platelet plateed da sauran masu adawa da P2Y12R. Wannan ƙarin tasirin ticagrelor fiye da antagonism na P2Y12R yana cikin ɓangare sakamakon sakamakon ticagrelor yana hana jigilar jigilar mahaifa 1 (ENT1) a kan platelet, wanda ke haifar da tarin adenosine da kunnawa na Gs-hade adenosine A2A masu karɓa [1]. Kwayoyin B16-F10 suna nuna raguwar mu'amala da platelets daga berayen da aka yiwa maganin ticagrelor idan aka kwatanta da berayen da aka yiwa maganin gishiri [2].

A cikin B16-F10 melanoma na cikin kwarjinin ciki da ƙananan ƙwayoyin cuta, ɓeraye waɗanda aka yi wa magani na ticagrelor (10 mg / kg) suna nuna ragin raguwa a cikin huhu (84%) da hanta (86%) metastases. Bugu da ƙari kuma, maganin ticagrelor yana inganta rayuwa idan aka kwatanta da dabbobin da aka kula da su. An lura da irin wannan tasirin a cikin tsarin cutar sankarar mama 4T1, tare da raguwa a cikin huhu (55%) da kuma kashin ƙashi (87%) na metastases bayan bin ticagrelor [2]. Gudanar da maganganu guda ɗaya na ticagrelor (1-10 mg / kg) yana haifar da tasirin hana tasirin kwayar cutar akan tarin platelet. Ticagrelor, a mafi girman kashi (10 mg / kg) yana hana tarawar platelet a 1 h bayan yin allurai kuma ana lura da ƙyamar ganiya a 4 h bayan anayi.

Ma'aji

4°C, kariya daga haske, adana ƙarƙashin nitrogen

* A cikin sauran ƙarfi: -80°C, watanni 6; -20°C, wata 1 (kariya daga haske, adana ƙarƙashin nitrogen)

Tsarin sunadarai

Ticagrelor

TABBATARWA

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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