ʻO Ticagrelor

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Ka inoa o API Hōʻike Hoakaka US DMF  EU DMF  CEP
ʻO Ticagrelor Anticoagulant Ma-Hale 28984  

ʻIke kikoʻī

Nā huahana huahana

ʻIkepili Huahana

Papa kāʻei kua

ʻO Ticagrelor kahi mea hakakā antagonist o ka mea loaʻa iā P2Y12 [1].

Ua hōʻike ʻia ʻo Ticagrelor e kāohi i nā hopena prothrombotic o ADP ma ka paukū e kūʻē i ka mea loaʻa iā P2Y12. Ua hōʻike ʻo Ticagrelor i ka pāpā piha o ka platelet hōʻuluʻulu ex vivo. Hoʻohui ʻia ua ʻōlelo ʻo Ticagrelor i kahi lāʻau kūpaʻa hilinaʻi i ka hōʻuluʻulu platelet i ke kanaka. Ma waho o kēia, ua hōʻike ʻo Ticagrelor i kahi mea antagonist hoʻopaʻa waha. ʻAʻole like me nā mea kāohi ʻē aʻe, ua hōʻike pū ʻo Ticagrelor e kāohi i ka mea loaʻa iā P2Y12 me ka loli ʻole o ka metabolic. Ma waho aʻe o kēlā, ʻo Ticagrelor ka thienopyridine anti-platelet agents mua a metabolised ʻia e CYP3A4 a me CYP2C19 [1] [2].

Nā kūmole:
[1] Zhou D1, Andersson TB, Grimm SW. ʻO ka loiloi in vitro o ka launa lāʻau lāʻau hiki ke hiki me ka ticagrelor: cytochrome P450 react phenotyping, kaohi ʻana, ka hoʻokomo ʻana, a me nā kinetics ʻokoʻa. ʻO ka hoʻolei Metab lāʻau lāʻau. 2011 ʻAropa; 39 (4): 703-10.
[2] Li Y1, Landqvist C, Grimm SW. ʻO ka dispose a me ka metabolism o ticagrelor, kahi antagonist receptor P2Y12 novel, i nāʻiole, nā ʻiole, a me nā marmosets. ʻO ka hoʻolei Metab lāʻau lāʻau. 2011 Sep; 39 (9): 1555-67. hana: 10.1124 / dmd.111.039669. Epub 2011 Jun 13.

Wehewehe

ʻO Ticagrelor (AZD6140) kahi P2Y12 receptor antagonist loea i hoʻohuli ʻia no ka mālama ʻana i ka hōʻuluʻulu platelet.

I Vitro

Paipai ʻo Ticagrelor i kahi pāpā nui o adenosine 5'-diphosphate (ADP)-hoʻokuʻu ʻia ʻo Ca2 + i loko o nā pā i makemake ʻia me nā mea hoʻouka P2Y12R ʻē aʻe. ʻO kēia hopena hou o ka ticagrelor ma ʻō aku o P2Y12R antagonism ma kahi ʻāpana ma ke ʻano he hopena o ticagrelor e kāohi ana i ka equilibrative nucleoside transporter 1 (ENT1) ma nā platelet, e alakaʻi ana i ka hōʻiliʻili ʻana o adenosine extracellular a me ka hoʻoulu ʻana o nā Gs i hui pū ʻia me adenosine A2A [1]. Hōʻike nā pūnaewele B16-F10 i ka hoʻoliʻiliʻi o ka launa pū ʻana me nā platelet mai nā ʻiole i mālama ʻia e ticagreloror i hoʻohālikelike ʻia me nā ʻiole i mālama ʻia i ka saline.

I ka B16-F10 melanoma intravenous a me intrasplenic metastasis models, nāʻiole i mālama ʻia me kahi lāʻau lapaʻau o ka ticagrelor (10 mg / kg) e hōʻike ana i nā hoʻoliʻiliʻi o nā māmā (84%) a me nā metastases ate (86%). Eia kekahi, hoʻomaikaʻi ke olakino ticagrelor i ke ola ke hoʻohālikelike ʻia i nā holoholona i mālama ʻia i ka saline. Kuhi ʻia kahi hopena e like me ke ʻano o ka maʻi ʻaʻai umauma 4T1, me ka hoʻēmi ʻana i ka māmā (55%) a me ka iwi iwi (87%) metastases ma hope o ka mālama ʻana i ka ticagrelor [2]. Hoʻokele waha hoʻokahi o ticagrelor (1-10 mg / kg) ke kumu o ka hopena o ka hopena pili i ka hopena ma ka hōʻiliʻili platelet. ʻO Ticagrelor, ma ka mahele lāʻau kiʻekiʻe loa (10 mg / kg) ka mea nui e kāohi i ka hōʻuluʻulu platelet ma 1 h ma hope o ka hana ʻana a ʻike ʻia ka pākī kiʻekiʻe ma 4 h ma hope o ka hana ʻana.

Waihona

4°C, pale mai ka mālamalama, mālama ʻia ma lalo o ka naikokene

* I ka hoʻoheheʻe: -80°C, 6 mahina; -20°C, 1 mahina (pale mai ka mālamalama, mālama ʻia ma lalo o ka naikokene)

ʻAno kemika

Ticagrelor

CERTIFICATE

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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