Dabigatran - CAS 211914-51-1
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Not Intended for Therapeutic Use. For research use only.
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Dabigatran is a very potent anticoagulant, shows that the terminal phenyl can be substituted by the more hydrophilic 2-pyridyl group without substantial loss of activity.
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B0084-102023 250 mg $168 In stock
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BIBR 953
1.Management of bleeding complications in patients with cancer on DOACs.
Schulman S1, Shrum J2, Majeed A3. Thromb Res. 2016 Apr;140 Suppl 1:S142-7. doi: 10.1016/S0049-3848(16)30113-X.
There has been a concern that major bleeding events (MBE) on direct-acting oral anticoagulants (DOACs) will be more difficult to manage than on vitamin K antagonists. Patients with cancer and DOAC-associated bleeding may be even more of a challenge to manage. We therefore reviewed the literature on bleeding in patients with cancer on DOACs. In addition, we performed an analysis of individual patient data from 5 phase III trials on treatment with dabigatran with focus on those with cancer. In 6 randomized trials the risk of MBE in patients with cancer was similar on treatment with DOACs compared to vitamin K antagonists. Bleeding was in the majority of patients managed with supportive therapy alone. In the individual patient data analysis there were no significant differences in use of hemostatic products, transfusion of red cells, effectiveness of management, bleeding-related mortality or 30-day all-cause mortality between patients with cancer treated with dabigatran or with warfarin.
2.Laboratory determination of old and new targeted anticoagulant agents for prevention of bleeding and thrombotic events in cancer patients.
Harenberg J1. Thromb Res. 2016 Apr;140 Suppl 1:S165-7. doi: 10.1016/S0049-3848(16)30117-7.
A two-fold prolongation of activated partial thromboplastin time (APTT) is established as therapeutic range for therapy with unfractionated heparin, hirudin and argatroban. The international normalized ratio (INR) of 2 to 3 is required to maintain anticoagulation in the therapeutic range of vitamin K antagonists. The therapeutic range of anti-factor Xa activity during therapy with low-molecular weight heparins and danaparoid are less well and of direct oral anticoagulants (DOAC) poorly defined. The relation of aPTT and INR values to thrombotic and bleeding events are well established despite a large variation of values in affected patients. The relation of coagulation values of the other anticoagulants to clinical events is open. The value of determination in cancer patients is higher because of the increased risk for thrombotic and bleeding events of this patient group. Several activities are currently undertaken to certify methods for in vitro diagnostic testing for DAOCs.
3.Hypercoagulability causes atrial fibrosis and promotes atrial fibrillation.
Spronk HM1, De Jong AM2, Verheule S3, De Boer HC4, Maass AH2, Lau DH3, Rienstra M2, van Hunnik A3, Kuiper M3, Lumeij S3, Zeemering S3, Linz D5, Kamphuisen PW6, Ten Cate H1, Crijns HJ7, Van Gelder IC2, van Zonneveld AJ4, Schotten U8. Eur Heart J. 2016 Apr 12. pii: ehw119. [Epub ahead of print]
AIMS: Atrial fibrillation (AF) produces a hypercoagulable state. Stimulation of protease-activated receptors by coagulation factors provokes pro-fibrotic, pro-hypertrophic, and pro-inflammatory responses in a variety of tissues. We studied the effects of thrombin on atrial fibroblasts and tested the hypothesis that hypercoagulability contributes to the development of a substrate for AF.
4.Specific antidotes against direct oral anticoagulants: A comprehensive review of clinical trials data.
Tummala R1, Kavtaradze A1, Gupta A2, Ghosh RK3. Int J Cardiol. 2016 Mar 28;214:292-298. doi: 10.1016/j.ijcard.2016.03.056. [Epub ahead of print]
The Vitamin K antagonist warfarin was the only oral anticoagulant available for decades for the treatment of thrombosis and prevention of thromboembolism until Direct Oral Anticoagulants (DOACs); a group of new oral anticoagulants got approved in the last few years. Direct thrombin inhibitor: dabigatran and factor Xa inhibitors: apixaban, rivaroxaban, and edoxaban directly inhibit the coagulation cascade. DOACs have many advantages over warfarin. However, the biggest drawback of DOACs has been the lack of specific antidotes to reverse the anticoagulant effect in emergency situations. Activated charcoal, hemodialysis, and activated Prothrombin Complex Concentrate (PCC) were amongst the nonspecific agents used in a DOAC associated bleeding but with limited success. Idarucizumab, the first novel antidote against direct thrombin inhibitor dabigatran was approved by US FDA in October 2015. It comprehensively reversed dabigatran-induced anticoagulation in a phase I study.
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CAS 211914-51-1 Dabigatran

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