Delving into the Latest Updates on Darexaban Maleate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Darexaban, Darexaban maleate (JAN)

+ [2]

Target

factor Xa

Mechanism

factor Xa inhibitors(Factor Xa inhibitors)

Therapeutic Areas

Cardiovascular DiseasesNervous System Diseases

Active Indication-

Inactive Indication

Acute Coronary SyndromeAtrial FibrillationStroke+ [3]

Originator Organization

Astellas Pharma, Inc.

Active Organization-

Inactive Organization

Astellas Pharma Europe Ltd.

Astellas Pharma, Inc.Astellas Tokai KK

+ [2]

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

Regulation-

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Structure

Molecular FormulaC31H34N4O8

InChIKeyWHMPMUVISXATBH-BTJKTKAUSA-N

CAS Registry365462-24-4

View All Structures (2)

The primary objective of this study is to determine the effect of rifampicin on the way the body handles darexaban and its metabolites (drug degradation products). The secondary objective of the study is to evaluate the safety and tolerability of a single dose of darexaban alone and when administered together with rifampicin.

Start Date01 Jan 2010

Sponsor / Collaborator

Astellas Pharma, Inc.

100 Clinical Results associated with Darexaban Maleate

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100 Translational Medicine associated with Darexaban Maleate

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100 Patents (Medical) associated with Darexaban Maleate

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72

Literatures (Medical) associated with Darexaban Maleate

13 Jan 2023·Medicine

Efficacy of 11 anticoagulants for the prevention of venous thromboembolism after total hip or knee arthroplasty: A systematic review and network meta-analysis

Review

Author: Xu, Dan ; Zhao, Pengfei ; Huang, Zhihao ; Xu, Xinru ; Zou, Miao

Background:To systematically review the efficacy of 11 anticoagulants in the treatment of venous thromboembolism (VTE) after total hip or knee arthroplasty.Methods:PubMed, Cochrane Library, Embase, Web of Science, China National Knowledge Infrastructure, Wanfang Data, VIP, and China Biology Medicine databases were electronically searched for studies assessing the efficacy of different anticoagulants for the prevention of VTE after total hip or knee arthroplasty from January 1, 2010, to January 27, 2022. Two reviewers independently screened the literature, extracted data, and graded the evidence using Confidence in Network Meta-Analysis. The network meta-analysis was then performed using Stata 16.0 software and R 4.1.0 software.Results:A total of 61 articles were included. The results of network meta-analysis showed that apixaban, edoxaban, fondaparinux, rivaroxaban, and darexaban were the most effective anticoagulants for the prevention of deep vein thrombosis in patients undergoing total hip or knee arthroplasty (P < .05), while there was no difference in the efficacy among the anticoagulants for the prevention of pulmonary embolism (P > .05).Conclusion:Apixaban, edoxaban, fondaparinux, rivaroxaban, and darexaban have the best efficacy for the prevention of VTE after total hip or knee arthroplasty.

01 Apr 2021·Pharmacological ResearchQ2 · MEDICINE

Ranking the efficacy of anticoagulants for the prevention of venous thromboembolism after total hip or knee arthroplasty: A systematic review and a network meta-analysis

Q2 · MEDICINE

Review

Author: Feng, Weili ; Huang, Daoqiang ; Wang, Xiaoping ; Lu, Anqi

BACKGROUNDAnticoagulants are essential in the prevention of venous thromboembolism. However, the effectiveness and safety of different anticoagulants have always been controversial. Therefore, we aimed to expand the sample of anticoagulant results and rank the efficacy and safety of 19 anticoagulants in the prevention of venous thromboembolism when total knee or total hip arthroplasty procedure is performed.METHODSA systematic review and network meta-analysis of randomized trials of adult patients undergoing total hip or knee arthroplasty were conducted. The trials were identified from PubMed, Web of Science, Cochrane Library, and Embase databases, in which anticoagulants were used as interventions randomized controlled trial. The incidence of venous embolism and bleeding are the key outcomes of assessing the efficacy of intervention drugs. We used the Physical Therapy Evidence Database (PEDro) to assess risk bias and used pairwise comparison and network meta-analysis with random effects to estimate the summary relative risk. The study has been registered with PROSPERO, number CRD42020200747.RESULTSFrom the 4083 identified manuscripts, 45,067 participants from 53 randomized trials were included in the analysis and randomly assigned to 19 anticoagulants. With Enoxaparin as a control, Rivaroxaban (risk difference 0.07, 95 % credible interval 0.06 to 0.08), Edoxaban (RD 0.09, 95 % CrI 0.08 to 0.11), and Apixaban (RD 0.05, 95 % CrI 0.04 to 0.06) had the best effect in preventing VTE. However, in terms of comprehensive bleeding rate, Apixaban, Edoxaban, and Darexaban were the most effective and stable. Although effective in preventing VTE, bleeding remains relatively high in Rivaroxaban. Enoxaparin is low-molecular-weight heparin that is widely used in clinics, and although its overall efficacy is not the best, its efficacy and safety are very stable.CONCLUSIONAccording to the available data, Apixaban, Edoxaban, and Darexaban are better than any anticoagulants in the prevention of VTE and bleeding during total knee or total hip arthroplasty. In our study, Fondaparinux, Eribaxaban, Dalteparin, Betrixaban, Bemiparin, Reviparin, Acenocoumarol, and Tinzaparin were scarce in the included studies, therefore, more evidence is needed to prove their efficacy and safety.

01 Jan 2021·Thrombosis ResearchQ3 · MEDICINE

Twice- or Once-Daily Dosing of Direct Oral Anticoagulants, a systematic review and meta-analysis

Q3 · MEDICINE

Review

Author: Nony, P ; Cucherat, M ; Durieu, I ; Mainbourg, S ; Mismetti, P ; Laporte, S ; Grange, C ; Bertoletti, L ; Lega, J-C ; Provencher, S ; Grenet, G ; Kilo, R ; Gueyffier, F

AIMThe direct oral anticoagulants (DOAC) have similar half-lives, but the dosing regimen varies between once daily (QD) or twice daily (BID). For some prescribers, the QD regimen improves compliance. Others prefer BID regimens to promote better stability of plasma concentrations, particularly in the event of missed doses. Limited level of evidence provides guidance about the best treatment strategy. The purpose of this study was to compare the treatment effect of QD vs. BID administration of DOACs in major orthopedic surgery (MOS), non-valvular atrial fibrillation (NVAF), venous thromboembolism (VTE), and acute coronary syndrome (ACS).METHODSWe conducted a systematic review up to April 2020. We included phase II clinical trials comparing DOAC QD vs BID with same daily dose. We extracted data for the occurrence of major thrombosis (proximal deep vein thrombosis, pulmonary embolism, myocardial infarction, ischemic stroke) and major hemorrhage (ISTH criteria and recommendations of the European Medicines Agency for surgical patients). Relative risks (RR) were combined using a fixed and random effects weighted meta-analysis.RESULTSTwelve randomized, controlled, phase II trials were included (10,716 patients), representing 24 dosing regimen comparisons of apixaban, darexaban, edoxaban, rivaroxaban, letaxaban, and dabigatran. There was no difference for major thrombotic event (RR_BID/QD = 1.06, 95%IC 0.86-1.30) nor for major bleeding (RR_BID/QD = 1.02, 95%IC 0.84-1.23) between the BID vs QD regimens, without heterogeneity (I² = 0%).CONCLUSIONOur study does not support a global difference in term of efficacy and safety of the BID and QD regimens of DOAC in MOS, NVAF, VTE and ACS.

100 Deals associated with Darexaban Maleate

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External Link

KEGG	Wiki	ATC	Drug Bank
D09817	Darexaban Maleate	-	DB12289

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Venous Thromboembolism	Phase 3	RU	Astellas Pharma Europe Ltd.	01 Apr 2009
Venous Thromboembolism	Phase 3	UA	Astellas Pharma Europe Ltd.	01 Apr 2009
Venous Thromboembolism	Phase 3	SE	Astellas Pharma Europe Ltd.	01 Apr 2009
Venous Thromboembolism	Phase 3	PR	Astellas Pharma Europe Ltd.	01 Apr 2009
Venous Thromboembolism	Phase 3	ZA	Astellas Pharma Europe Ltd.	01 Apr 2009
Venous Thromboembolism	Phase 3	CZ	Astellas Pharma Europe Ltd.	01 Apr 2009
Venous Thromboembolism	Phase 3	AT	Astellas Pharma Europe Ltd.	01 Apr 2009
Venous Thromboembolism	Phase 3	BR	Astellas Pharma Europe Ltd.	01 Apr 2009
Venous Thromboembolism	Phase 3	US	Astellas Pharma Europe Ltd.	01 Apr 2009
Venous Thromboembolism	Phase 3	IN	Astellas Pharma Europe Ltd.	01 Apr 2009

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00942435 (Pubmed \| J Heart Lung Transplant)	Phase 3	-	156	Darexaban 15 mg bid	(ehutaxigmk) = wumcnmlqua ssknnnvtkr (oxmjxsejyn ) View more	-	01 Sep 2012
				Darexaban (YM150) (Mechanical prophylaxis)	(ehutaxigmk) = jopsbiwgyb ssknnnvtkr (oxmjxsejyn ) View more
ONYX-2 (Pubmed \| J Thromb Haemost)	Not Applicable	Venous Thromboembolism	1,017	YM150 5 mg	tksiceewsi(zloktpquki) = wpqvaasvol eotoriedxh (oqzwdmuftz )	-	01 Apr 2010
				YM150 10 mg	tksiceewsi(zloktpquki) = qymcbyhkgj eotoriedxh (oqzwdmuftz )