Drug intelligence / Profile preview

dabigatran etexilate + dronedarone

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

Dabigatran etexilate is an oral anticoagulant prodrug that is hydrolyzed to the active form, dabigatran, a direct and reversible thrombin inhibitor. It prevents the conversion of fibrinogen to fibrin, thereby impairing clot formation and reducing the risk of thromboembolic events such as stroke in patients with atrial fibrillation or after hip/knee replacement surgery. Dronedarone is an antiarrhythmic agent structurally related to amiodarone; it works by blocking multiple cardiac ion channels (calcium, potassium, sodium) and has antiadrenergic effects. Dronedarone slows nerve impulses in heart tissue to help maintain normal heart rhythm in patients with atrial fibrillation. When used together, there is a pharmacokinetic interaction due to dronedarone’s inhibition of P-glycoprotein (P-gp), which increases exposure to dabigatran[1][2][3][6]. Both drugs are approved for use in nonvalvular atrial fibrillation but require careful monitoring when co-administered due to increased bleeding risk.

Brand names
PradaxaMultaq
Other names
dabigatrandabigatran etexilate mesylate
02

Targets

SCN5A (Sodium channel protein type 5 subunit alpha)ABCB1 (P-glycoprotein)KCNH2 (Voltage-gated potassium channel subfamily H member 2)F2 (Thrombin)ADRB1 (β1)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)

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