Ticagrelor

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Ticagrelor Anticoagulant Ka Ntlong 28984  

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Ka morao

Ticagrelor ke mohanyetsi oa lipale tsa mokamohelo oa P2Y12 [1].

Ticagrelor ho tlalehiloe hore e thibela litlamorao tsa ADP ho platelet ka khahlano le kamohelo ea P2Y12. Ticagrelor e bonts'itse thibelo e felletseng ea platelet aggregation ex vivo. Ntle le moo Ticagrelor e khothalelitse thibelo e itšetlehileng ka tekanyetso ea palo ea li-platelet ho batho. Ntle le tsena, Ticagrelor e boetse e bonts'itse mohanyetsi ea tlamang ka molomo, ka mafolofolo le ka mokhoa o ts'oanang. Ho fapana le li-inhibitors tse ling, Ticagrelor le eona e tlalehile ho thibela mokelikeli oa P2Y12 ntle le phetoho ea metabolism. Ntle ho moo, Ticagrelor ke moemeli oa pele oa anti-platelet oa thienopyridine mme haholo-holo e sebelisoa ke CYP3A4 le CYP2C19 [1] [2].

Litšupiso:
[1] Zhou D1, Andersson lefuba, Grimm SW. Tlhahlobo ea in vitro ea litšebelisano tse ka bang teng tsa lithethefatsi le ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction, le phapang ea kinetics. Ho Laola Metab ea Lithethefatsi. 2011 Mmesa; 39 (4): 703-10.
[2] Li Y1, Landqvist C, Grimm SW. Boikutlo le metabolism ea ticagrelor, mohanyetsi oa li-receptor oa P2Y12, litoeba, likhoto le limmosets. Ho Laola Metab ea Lithethefatsi. 2011 Sep; 39 (9): 1555-67. doi: 10.1124 / dmd.111.039669. Epub 2011 Pherekhong 13.

Tlhaloso

Ticagrelor (AZD6140) ke mohanyetsi ea amohelang molomo oa P2Y12 bakeng sa kalafo ea pokello ea platelet.

Ka Vitro

Ticagrelor e khothaletsa thibelo e kholo ea adenosine 5'-diphosphate (ADP)-Ca2 + e hlohlellelitsoeng ka liplatelete tse hlatsoitsoeng khahlanong le bahanyetsi ba bang ba P2Y12R. Phello ena e eketsehileng ea ticagrelor ka nqane ho P2Y12R antagonism e karolo e le litlamorao tsa ticagrelor e thibelang equilibrative nucleoside transporter 1 (ENT1) ho liplatelete, e lebisang ho bokelleng ha adenosine ea kantle ho sele le ho kenya tšebetsong li-receptor tsa Gs-coupled adenosine A2A [1]. Lisele tsa B16-F10 li bonts'a ho fokotseha ha tšebelisano le liplatelete tse tsoang litoeba tse tšoaroang ke ticagrelor ha li bapisoa le litoeba tse tšoaroang ka letsoai [2].

Ho B16-F10 melanoma intravenous and intrasplenic metastasis models, litoeba tse alafiloeng ka tekanyetso ea bongaka ea ticagrelor (10 mg / kg) lipontšo tse fokotsang phokotso ea matšoafo (84%) le metastase ea sebete (86%). Ho feta moo, kalafo ea ticagrelor e ntlafatsa pholoho ha e bapisoa le liphoofolo tse tšoaroang ka letsoai. Phello e ts'oanang e bonoa mokhoeng oa mofets'e oa 4T1, ka phokotso ea matšoafo (55%) le 'moko oa masapo (87%) metastases kamora kalafo ea ticagrelor [2]. Tsamaiso e le 'ngoe ea molomo ea ticagrelor (1-10 mg / kg) e baka tšitiso e amanang le lethal dose ho platelet aggregation. Ticagrelor, ka tekanyo e phahameng ka ho fetisisa (10 mg / kg) e thibela haholo palo ea platelet ho 1 h kamora ho ts'oaroa mme tlhoro ea tlhoro e bonoa ho 4 h kamora ho teba.

Polokelo

4°C, sireletsa leseling, le bolokiloe tlasa naetrojene

* Ka tharollo: -80°C, likhoeli tse 6; -20°C, khoeli ea 1 (sireletsa ho leseli, le bolokiloe tlasa naetrojene)

Sebopeho sa lik'hemik'hale

Ticagrelor

NTHATISI

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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