China China Factory for Sacubitril Hemicalcium - Dabigatran Etexilate Mesylate – CPF manufacturers and suppliers

China Factory for Sacubitril Hemicalcium - Dabigatran Etexilate Mesylate – CPF

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China Factory for Sacubitril Hemicalcium - Dabigatran Etexilate Mesylate – CPF Detail:

Description

Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active prodrug of Dabigatran. Dabigatran etexilate mesylate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.

Background

Description: IC50 Value: 4.5nM (Ki); 10nM(Thrombin-induced platelet aggregation) [1] Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) undergoing advanced clinical development as its orally active prodrug,dabigatran etexilate. in vitro: Dabigatran selectively and reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC(50): 10 nM), while showing no inhibitory effect on other platelet-stimulating agents.Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC(50): 0.56 microM). Dabigatran demonstrated concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 microM, respectively [1]. in vivo: Dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively [1]. Patients treated with dabigatran etexilate experienced fewer ischaemic strokes (3.74 dabigatran etexilate vs 3.97 warfarin) and fewer combined intracranial haemorrhages and haemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2]. Clinical trial: An Evaluation of the Pharmacokinetics and Pharmacodynamics of Oral Dabigatran Etexilate in Hemodialysis Patients . Phase1

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02170792	Boehringer Ingelheim	Healthy	February 2001	Phase 1
NCT02170974	Boehringer Ingelheim	Healthy	July 2004	Phase 1
NCT02170831	Boehringer Ingelheim	Healthy	May 1999	Phase 1
NCT02170805	Boehringer Ingelheim	Healthy	April 2001	Phase 1
NCT02170610	Boehringer Ingelheim	Healthy	March 2002	Phase 1
NCT02170909	Boehringer Ingelheim	Healthy	December 2004	Phase 1
NCT02171000	Boehringer Ingelheim	Healthy	April 2005	Phase 1
NCT02170844	Boehringer Ingelheim	Healthy	June 2004	Phase 1
NCT02170584	Boehringer Ingelheim	Healthy	January 2001	Phase 1
NCT02170935	Boehringer Ingelheim	Venous Thromboembolism	April 2002	Phase 2
NCT02170636	Boehringer Ingelheim	Healthy	January 2002	Phase 1
NCT02170766	Boehringer Ingelheim	Healthy	October 2000	Phase 1
NCT02171442	Boehringer Ingelheim	Healthy	April 2002	Phase 1
NCT02170896	Boehringer Ingelheim	Healthy	October 2001	Phase 1
NCT02173730	Boehringer Ingelheim	Healthy	November 2002	Phase 1
NCT02170623	Boehringer Ingelheim	Healthy	February 2002	Phase 1
NCT02170116	Boehringer Ingelheim	Healthy	November 1998	Phase 1
NCT02170597	Boehringer Ingelheim	Healthy	August 2003	Phase 1
NCT01225822	Boehringer Ingelheim	Venous Thromboembolism	November 2002	Phase 2
NCT02170701	Boehringer Ingelheim	Venous Thromboembolism	October 2000	Phase 2
NCT02170740	Boehringer Ingelheim	Healthy	November 1999	Phase 1
NCT02170922	Boehringer Ingelheim	Healthy	July 1999	Phase 1