ximelagatran (Exanta)

prodrug (via hydroxylation) of melagatran & a direct thrombin inhibitor; liver toxicity concerns so AZD0837 being developed to replace this

Also Known As:

Exanta; H 376 95; H 376-95; glycine, N-((1)1-cyclohexyl-2-((2)-((((4-(amino(hydroxyimino)methyl)phenyl)methyl)amino)carbonyl)-1-azetidinyl)2-oxoethyl)-ethyl ester; glycine, N-((1R)1-cyclohexyl-2-((2S)-((((4-(amino(hydroxyimino)methyl)phenyl)methyl)amino)carbonyl)-1-azetidinyl)2-oxoethyl)-ethyl ester; xi-melagatran

Networked: 239 relevant articles (39 outcomes, 123 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Experts

1.	Eriksson, Ulf G: 16 articles (04/2012 - 02/2002)
2.	Frison, Lars: 10 articles (11/2008 - 02/2002)
3.	Wåhlander, Karin: 9 articles (04/2012 - 08/2002)
4.	Halperin, Jonathan L: 9 articles (08/2009 - 09/2003)
5.	Bylock, Anders: 8 articles (02/2008 - 02/2002)
6.	Eriksson, Henry: 8 articles (04/2006 - 08/2002)
7.	Eriksson, Bengt I: 7 articles (01/2006 - 02/2002)
8.	Wolzt, Michael: 6 articles (04/2012 - 02/2003)
9.	Lip, Gregory Y H: 6 articles (09/2010 - 12/2004)
10.	Grind, Margaretha: 6 articles (06/2007 - 03/2003)

Related Diseases

1.	Stroke (Strokes) 02/01/2008 - "Ximelagatran reduced the risk of death, MI, or stroke by 70% (hazard ratio 0.30, 95% CI 0.12-0.74). " 02/01/2008 - "Of 101 patients with AF treated with ximelagatran 7 (6.9%) had either death, MI, or stroke, compared with 15 (20.6%) in 73 patients allocated to placebo. " 08/01/2005 - "Given the consistency of response, the favorable overall benefit-risk ratio and the convenience of fixed oral dosing, ximelagatran may increase the number of patients with AF eligible for anticoagulation and amplify the potential for prophylaxis against stroke." 06/15/2005 - "Cost-effectiveness of ximelagatran for stroke prevention." 01/01/2005 - "With its positive benefit-risk ratio, ximelagatran may increase the population of eligible patients for anticoagulation with AF and maximize the potential of anticoagulation in the prevention of stroke."
2.	Atrial Fibrillation 08/01/2005 - "The low potential for drug:drug interactions with ximelagatran is also supported by an analysis of the pharmacokinetic data from clinical studies in patients with atrial fibrillation receiving long-term treatment with oral ximelagatran. " 01/01/2005 - "Ximelagatran has also been evaluated in two Phase III trials in patients with atrial fibrillation. " 09/01/2004 - "The pharmacology of ximelagatran and clinical trials with its use in atrial fibrillation is reviewed." 03/01/2003 - "Using an open, group-matched study design, the effects of ximelagatran (36 mg twice daily for 5 days) were studied in 12 patients with permanent nonvalvular atrial fibrillation and in 12 healthy controls. " 09/01/2004 - "Ximelagatran: a new antithrombotic option in atrial fibrillation."
3.	Venous Thromboembolism 01/01/2005 - "Safety and efficacy of ximelagatran: meta-analysis of the controlled randomized trials for the prophylaxis or treatment of venous thromboembolism." 03/01/2006 - "Incidence of recurrent venous thromboembolism of patients after termination of treatment with ximelagatran." 08/01/2005 - "Ximelagatran for the prevention of venous thromboembolism following elective hip or knee replacement surgery." 07/01/2005 - "Ximelagatran has already been approved in Europe for prophylaxis of venous thromboembolism in patients undergoing hip or knee surgery. " 01/01/2005 - "The role of ximelagatran in the treatment of venous thromboembolism."
4.	Hemorrhage 09/01/2005 - "The influence of potential prognostic factors on the risk of recurrent VTE or major and/or minor bleeding and their impact on ximelagatran treatment was evaluated in the THRIVE III study population. " 10/01/2004 - "The definitions of bleeding events used in clinical trials of ximelagatran are broadly consistent with those used in many other major trials. " 08/01/2002 - "Recent data derived from a dose-finding study and its open label continuous follow-up period are very encouraging with regard to the low incidence of bleeding complications and ximelagatran's clinical efficacy for the prevention of thromboembolic events. " 07/08/2014 - "One RCT comparing six months' extension of anticoagulation with 18 months of ximelagatran 24 mg twice daily versus no extended ximelagatran did not exclude beneficial or harmful effects for the outcomes of reduction in VTE, mortality, and minor bleeding. " 06/15/2011 - "One RCT comparing six months extension of anticoagulation with 18 months ximelagatran 24 mg twice daily versus placebo found a reduction in VTE (HR 0.16; 95% CI 0.09 to 0.30) but did not exclude beneficial or harmful effects for the outcomes of mortality and bleeding. "
5.	Venous Thrombosis (Deep-Vein Thrombosis) 07/01/2007 - "Ximelagatran for treatment and prophylaxis of recurrent events in deep vein thrombosis." 04/01/2005 - "Pharmacokinetics of ximelagatran and relationship to clinical response in acute deep vein thrombosis." 07/23/2004 - "[Prevention and treatment of deep vein thrombosis with ximelagatran]." 11/01/2005 - "Ximelagatran, an oral direct thrombin inhibitor, has also been shown to effective for treatment and prevention of venous thrombosis. " 07/01/2007 - "The efficacy and safety of treatment of patients with acute deep venous thrombosis who received 2 infinity 36 mg ximelagatran was not inferior to that of patients who received a conventional anticoagulant for prophylaxis of recurrent events over 6 months. "

Related Drugs and Biologics

1.	Warfarin (Coumadin)
2.	Antithrombins
3.	Thrombin
4.	Anticoagulants
5.	Enoxaparin (Lovenox)
6.	Low-Molecular-Weight Heparin (Heparin, Low Molecular Weight)
7.	melagatran
8.	Aspirin (Acetylsalicylic Acid)
9.	Vitamin K
10.	idraparinux

Related Therapies and Procedures

1.	Therapeutics
2.	Knee Replacement Arthroplasty (Total Knee Replacement)
3.	Secondary Prevention
4.	Orthopedic Procedures
5.	Operative Surgical Procedures