Dabigatran etexilate mesylate

Biological Activity

Dabigatran etexilate may provide a promising alternative for the treatment of postprocedural vision loss after ppv. A direct thrombin inhibitor, dabigatran etexilate (hereinafter referred to as dabigatran) was approved in the Russian Federation for prevention of thromboembolic complications in orthopaedic practice (2009), for prevention of ischaemic embologenic stroke in atrial fibrillation (2011) and for treatment of recurrent thrombosis of deep veins and pulmonary artery thromboembolism (2014). Additional administration of 2 × 110 mg dabigatran etexilate (Pradaxa(®)), a novel direct thrombin inhibitor, resulted in a prompt and marked improvement of visual acuity, which indicated improved blood flow in the central vessels of the optic nerve. Dabigatran etexilate appeared to have several pharmacokinetic and pharmacodynamic advantages over warfarin, as well as a favorable efficacy and safety profile being at least noninferior and often superior to warfarin in patients with non-valvular AF. The latter was shown in the clinical trials, meta-analyses and studies with 'real-world' data. Currently ongoing trials will expand the body of evidence on warfarin and will aid decision making in currently controversial areas. Important limitations of dabigatran etexilate include contraindications for its use in patients with prosthetic heart valves and end-stage chronic kidney disease.

Chemical Information

Molecular Weight	723.84
Formula	C35H45N7O8S
CAS Number	872728-81-9
Solubility (25°C)	DMSO
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

References

[1] Beliavskaia OO, et al. Angiol Sosud Khir. Laboratory assessment of haemostatic parameters in patients taking a direct thrombin inhibitor.

[2] Dzeshka MS, et al. Expert Opin Drug Saf. Warfarin versus dabigatran etexilate: an assessment of efficacy and safety in patients with atrial fibrillation.

[3] Schönfeld CL, et al. Case Rep Ophthalmol. Recovery of visual function after administration of dabigatran etexilate.