Investigation of Solid-State Hydrate-Anhydrous Phase Transformations of Dabigatran Etexilate Hemi-Edisylate

The Discovery of Dabigatran Etexilate

Thromboembolic disease is a major cause of mortality and morbidity in the developed world and is caused by an excessive stimulation of coagulation. Thrombin is a key serine protease in the coagulation cascade and numerous efforts have been made to develop safe and effective orally active direct thrombin inhibitors (DTIs). Current anticoagulant therapy includes the use of indirect thrombin inhib...

Phase Transformations Preparation of Solid State Materials

Pradaxa, INN- dabigatran etexilate

Dabigatran etexilate tetra­hydrate

In the title compound, C34H41N7O5·4H2O (systematic name: ethyl 3-{[2-({4-[(Z)-amino-(hexyl-oxycarbonyl-imino)-meth-yl]anilino}meth-yl)-1-meth-yl-benzimidazole-5-carbon-yl]pyridin-2-yl-amino}-propano-ate tetra-hydrate), the benzene and pyridine rings form dihedral angles of 5.4 (1) and 43.8 (1)°, respectively, with the benzimidazole mean plane. The terminal butyl group is disordered over two con...

Dabigatran etexilate in atrial fibrillation.

Atrial fibrillation (AF) affects millions worldwide. Stroke is the most devastating complication of AF and is associated with a huge disease burden. As a preventive measure, anticoagulant therapy is recommended for most AF patients based on presence of stroke risk factors. For the past six decades warfarin remained the gold standard for stroke prevention in AF (SPAF). However, it is associated ...