Ticagrelor

Faʻamatalaga puʻupuʻu:

Igoa ole API Faailoga Faʻamatalaga US DMF  EU DMF  CEP
Ticagrelor Anticoagulant Totonu o le Fale 28984  

Oloa Faʻamatalaga

Pine o oloa

FAʻAMATALAGA FAʻAMATALAGA

Talaʻaga

Ticagrelor o se tala tetee i le taliaina P2Y12 [1].

Ticagrelor ua lipotia e taofia le prothrombotic aafiaga o le ADP i luga o le ipu e faasaga i le P2Y12 taliaina. Ticagrelor ua faʻaalia le taofiofia atoa o le platelet aggregation ex vivo. I se faʻaopopoga Ticagrelor ua fautuaina se inumaga-faʻalagolago taofiofia o faʻamaʻaina faʻavaeina i tagata soifua. E ese mai i nei, ua faʻailoa mai foi e le Ticagrelor se tagata tautala i le tautala, faʻagaeʻetia, ma feliuaʻi. E le pei o isi mea taofi, Ticagrelor ua lipotia foi e taofia le P2Y12 talimalo e aunoa ma le suia o le metabolic. E le gata i lena, o le Ticagrelor o le muamua lea o le thienopyridine anti-platelet agents ma e tele na gaosia e CYP3A4 ma CYP2C19 [1] [2].

Faʻamatalaga:
[1] Zhou D1, Andersson TB, Grimm SW. In vitro iloiloina o gaioiga faʻatonu-fualaʻau faʻafitauli ma ticagrelor: cytochrome P450 tali phenotyping, taofiofia, faʻatonutonuina, ma eseesega kinetics. Fualaʻau Faʻasaina o Metab. 2011 Ape; 39 (4): 703-10.
[2] Li Y1, Landqvist C, Grimm SW. Disposition ma metabolism o le ticagrelor, o se tala fou P2Y12 talimalo talimalo, i isumu, isumu, ma marmosets. Fualaʻau Faʻasaina o Metab. 2011 Sep; 39 (9): 1555-67. faia: 10.1124 / dmd.111.039669. Epub 2011 Jun 13.

Faʻamatalaga

Ticagrelor (AZD6140) o se fesuiaʻi gofie P2Y12 talimalo talimalo talimalo mo le togafitia o faʻamaopoopo faaputuputuina.

I Vitro

Ticagrelor faalauiloaina se sili atu taofiofia o adenosine 5'-diphosphate (ADP)-faʻamalosia Ca2 + faʻasaʻolotoina i totonu o lapisi lapisi ma isi P2Y12R tagata tetee. O lenei faʻaopopo aʻafiaga o le ticagrelor i tala atu o le P2Y12R antagonism o se vaega o se faʻaiuga o le ticagrelor taofiofia le tutusa tutusa nucleoside transporter 1 (ENT1) i luga o peleti, e mafua ai le faʻaputuputuga o extracellular adenosine ma le faʻagaoioia o Gs-soʻofaʻatasi adenosine A2A taliaina [1]. O sela o le B16-F10 o loʻo faʻaalia ai le faʻaititia o paʻu mai i isumu na togafitia e le ticagreloror peʻa faʻatusatusa i isumu na togafitia i saline.

I le B16-F10 melanoma intravenous ma intrasplenic metastasis models, isumu togafitia ma se togafitiga fualaʻau o le ticagrelor (10 mg / kg) faʻaalia faʻaititia faʻaititia i mama (84%) ma ate (86%) metastases. Ma le isi, togafitiga ticagrelor faʻaleleia le ola faʻatusatusa i saline-togafitia manu. O se tutusa aafiaga o loo maitauina i le 4T1 susu kanesa faʻataʻitaʻiga, ma le faʻaititia o mama (55%) ma ponaivi gaʻo (87%) metastases mulimuli i togafitiga ticagrelor [2]. Nofofua gutu pulega o ticagrelor (1-10 mg / kg) mafua ai fualaʻau-fesoʻotaʻiga aafiaga i luga o faaputuga faaputuputuina. Ticagrelor, i le maualuga o vailaʻau (10 mg / kg) matua taofia le faʻaputuputuina o le lapisi ile 1 h i le maeʻa ai o vailaʻau ma le tumutumu taofi e matauina ile 4 h pe a maeʻa.

Teuina o Meaai

4°C, puipuia mai le malamalama, teu i lalo ole nitrogen

* I le solvent: -80°C, 6 masina; -20°C, 1 masina (puipuia mai le malamalama, teu i lalo o le nitrogen)

Fausaga o vailaʻau

Ticagrelor

FAUTUAINA

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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