Dabigatran etexilate Basic information
Indications and Usage Mechanisms of Action Clinical Research Warnings and Precautions
Product Name: Dabigatran etexilate
Synonyms: BIBR-1048(Dabigatran etexilate);N-[2-[4-[N-(Hexyloxycarbonyl)aMidino]phenylaMinoMethyl]-1-Methyl-1H-benziMidazol-5-ylcarbonyl]-N-(2-;BIBR 1048;BIBR-1048;Prazaxa;N-[[2-[[[4-[[[(Hexyloxy)carbonyl]aMidino]iMinoMethyl]phenyl]aMino]Methyl]-1-Methyl-1H-benziMidazol-5-yl]carbonyl]-N-2-pyridyl-beta-alanine,ethyl ester;Pradaxa (dabigatran);Dabigatran Etexilate (free base)
CAS: 211915-06-9
MF: C34H41N7O5
MW: 627.74
EINECS: 1592732-453-0
Product Categories: Pharmaceutical intermediate;API;Dabigatran etexilate;Other APIs
Mol File: 211915-06-9.mol
Dabigatran etexilate Structure
Dabigatran etexilate Chemical Properties
Melting point 128-129°
Safety Information
MSDS Information
Dabigatran etexilate Usage And Synthesis
Indications and Usage Dabigatran is the newest generation of oral anticoagulant drugs – direct thrombin inhibitors (DTIs), belonging to non-peptide thrombin inhibitors and instead specifically and selectively blocks the thrombin activity (free or bound) to prevent coagulation. Dabigatran targets the preventative and clinical treatment needs of acute and chronic thromboembolic disease.
Mechanisms of Action It achieves anticoagulant effects through specific and selective inhibition of blood enzymes (free or bound). After oral ingestion and absorption through the digestive system, Dabigatran turns into Dabiga groups that have the direct anticoagulant abilities. By binding to thrombin in fibrin specific binding sites, Dabigatran stops fibrinogen from cleaving into fibrin, thus interrupting the blood clotting network and consequently thrombosis. Dabiga groups can also dissociate from the fibrin-thrombin coagulate and have an anticoagulating effect. Different from vitamin K antagonists, which affect different coagulants, Dabigatran can provide effective, predictable and stable anticoagulant effects. It will also have minimal reactions to other drugs or food, and does not require frequent monitoring or dosage adjustment.
Clinical Research Compared to the control group treated with Warfarin, Dabigatran can significantly decrease the risk of stroke and embolic disease (including hemorrhagic stroke), greatly reduce the occurrence of bleeding (including fatal bleeding and intracranial hemorrhage), and greatly lower vascular mortality rate. Dabigatran provides effective and stable anticoagulant effects and does not require constant monitoring of anticoagulant functions or dosage adjustments.
Warnings and Precautions 1. Dabigatran is not to be used by patients with severe kidney damage (CrCl<30ml/min).
2. Patients with high bleeding risk should also not use Dabigatran.
3. Patients must be tested and monitored for signs of lack of bleeding or anemia; if there is severe bleeding, cease use of Dabigatran and identify the bleeding area.
4. Dabigatran is not suitable for patients with significant manifestations of rheumatic valvar heart disease or patients with artificial heart valves.
Uses BIBR-1048 (Dabigatran) is an anticoagulant from the class of the direct thrombin inhibitors. It is being studied for various clinical indications and in many cases it offers an alternative to warfarin as the preferred orally administered blood thinner sin
Definition ChEBI: An aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-{N'-[(hexyloxy)carbonyl]carbamimidoyl}phenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amino group of thyl N-pyridin-2-yl-beta-alaninate. A prodrug for dabigatran, a thrombin inhibitor and anticoagulant which is used for the prevention of stroke and systemic embolism.