I-Dabigatran Etexilate Mesylate

Incazelo emfushane:

Igama le-API Inkomba Ukucaciswa I-US DMF I-EU DMF CEP
I-Dabigatran Etexilate Mesylate I-Anticoagulant Endlini      


Imininingwane Yomkhiqizo

Omaka bomkhiqizo

IMINININGWANE YOMKHIQIZO

Incazelo

I-Dabigatran etexilate mesylate (BIBR 1048MS) iyisidakamizwa esisebenza ngomlomo se-Dabigatran.I-Dabigatran etexilate mesylate inemiphumela ye-anticoagulant futhi isetshenziselwa ukuvimbela i-venousthromboembolism kanye ne-stroke ngenxa ye-atrial fibrillation.

Ingemuva

Incazelo: IC50 Inani: 4.5nM (Ki);I-10nM(i-Thrombin-induced platelet aggregation) [1] I-Dabigatran iyisivimbeli esibuyisela emuva emuva nesikhethayo, esiqondile se-thrombin inhibitor (DTI) esithuthuke kakhulu emtholampilo njenge-prodrug esebenza ngomlomo, i-dabigatran etexilate.in vitro: I-Dabigatran evinjelwa ngokukhetha nangokubuyisela emuva i-thrombin yomuntu (Ki: 4.5 nM) kanye ne-thrombin-induced platelet aggregation (IC(50): 10 nM), kuyilapho ingabonisi umthelela ovimbelayo kwamanye ama-agent avuselela i-platelet.Isizukulwane se-Thrombin ku-platelet -i-plasma empofu (i-PPP), elinganiswa njenge-endogenous thrombin potential (ETP) yayivinjelwe ukugxila-okuncike (IC(50): 0.56 microM).I-Dabigatran ibonise imiphumela ye-anticoagulant encike ekugxiliseni ezinhlotsheni ezihlukahlukene ze-vitro, iphinda kabili isikhathi esicushiwe se-thromboplastin (aPTT), isikhathi se-prothrombin (PT) nesikhathi se-ecarin clotting (ECT) ku-PPP yomuntu ekugxilweni kwe-0.23, 0.83 kanye ne-0.18 microM, ngokulandelana [ 1].ku-vivo: I-Dabigatran yelula umthamo we-aPTT ngokuncika ngemva kokuphathwa ngomthambo wamagundane (0.3, 1 kanye no-3 mg/kg) nezinkawu ze-rhesus (0.15, 0.3 kanye no-0.6 mg/kg).Imiphumela ye-anticoagulant encike kumthamo nesikhathi yabonwa nge-dabigatran etexilate elawulwa ngomlomo kumagundane aqaphile (10, 20 kanye ne-50 mg / kg) noma izinkawu ze-rhesus (1, 2.5 noma 5 mg / kg), nemiphumela ephezulu ebonwa phakathi kwe-30 ne-120 iminithi ngemuva kokuphatha, ngokulandelana [1].Iziguli ezelashwa nge-dabigatran etexilate zaba nokushaywa kwe-ischemic okumbalwa (3.74 dabigatran etexilate vs 3.97 warfarin) kanye nokopha okuhlanganisiwe kwe-intracranial kanye nemivimbo ene-hemorrhagic (0.43 dabigatran etexilate vs 0.99 isiguli se-warfarin] ngonyaka we-10) ngonyaka we-10.Isilingo somtholampilo: Ukuhlolwa kwe-Pharmacokinetics kanye ne-Pharmacodynamics ye-Oral Dabigatran Etexilate ku-Hemodialysis Patients.Isigaba1

Isitoreji

Impushana

-20°C

3 iminyaka
 

4°C

iminyaka engu-2
Ku-solvent

-80°C

6 izinyanga
 

-20°C

Inyanga engu-1

Ukuhlolwa Komtholampilo

Inombolo ye-NCT Umxhasi Isimo Usuku okuqalwa ngalo

Isigaba

I-NCT02170792 Boehringer Ingelheim Unempilo February 2001

Isigaba 1

I-NCT02170974 Boehringer Ingelheim Unempilo Julayi 2004

Isigaba 1

I-NCT02170831 Boehringer Ingelheim Unempilo Meyi 1999

Isigaba 1

I-NCT02170805 Boehringer Ingelheim Unempilo Ephreli 2001

Isigaba 1

I-NCT02170610 Boehringer Ingelheim Unempilo Mashi 2002

Isigaba 1

I-NCT02170909 Boehringer Ingelheim Unempilo Disemba 2004

Isigaba 1

I-NCT02171000 Boehringer Ingelheim Unempilo Ephreli 2005

Isigaba 1

I-NCT02170844 Boehringer Ingelheim Unempilo Juni 2004

Isigaba 1

I-NCT02170584 Boehringer Ingelheim Unempilo Januwari 2001

Isigaba 1

I-NCT02170935 Boehringer Ingelheim I-venous thromboembolism Ephreli 2002

Isigaba 2

I-NCT02170636 Boehringer Ingelheim Unempilo Januwari 2002

Isigaba 1

I-NCT02170766 Boehringer Ingelheim Unempilo Okthoba 2000

Isigaba 1

I-NCT02171442 Boehringer Ingelheim Unempilo Ephreli 2002

Isigaba 1

I-NCT02170896 Boehringer Ingelheim Unempilo Okthoba 2001

Isigaba 1

I-NCT02173730 Boehringer Ingelheim Unempilo Novemba 2002

Isigaba 1

I-NCT02170623 Boehringer Ingelheim Unempilo February 2002

Isigaba 1

I-NCT02170116 Boehringer Ingelheim Unempilo Novemba 1998

Isigaba 1

I-NCT02170597 Boehringer Ingelheim Unempilo Agasti 2003

Isigaba 1

I-NCT01225822 Boehringer Ingelheim I-venous thromboembolism Novemba 2002

Isigaba 2

I-NCT02170701 Boehringer Ingelheim I-venous thromboembolism Okthoba 2000

Isigaba 2

I-NCT02170740 Boehringer Ingelheim Unempilo Novemba 1999

Isigaba 1

I-NCT02170922 Boehringer Ingelheim Unempilo Julayi 1999

Isigaba 1

Isakhiwo samakhemikhali

Dabigatran Etexilate Mesylate

ISItifiketi

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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