Drug intelligence / Profile preview

dabigatran etexilate + amiodarone

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

Overview

**dabigatran etexilate + amiodarone** is a combination of two pharmaceutical agents: dabigatran etexilate, a direct oral anticoagulant (DOAC) that acts as a reversible direct thrombin inhibitor, and amiodarone, a Class III antiarrhythmic that inhibits several cardiac ion channels and is a potent inhibitor of P-glycoprotein (P-gp) transporters. While no fixed-dose combination product exists, these drugs may be used concurrently in clinical practice, especially in patients with atrial fibrillation for stroke prevention and rhythm control. Concomitant use significantly increases dabigatran plasma concentrations—by about 50–58%—due to amiodarone's inhibition of P-gp, raising both efficacy and bleeding risk, particularly in elderly populations. Dabigatran etexilate is a prodrug hydrolyzed to dabigatran, which directly inhibits the conversion of fibrinogen to fibrin by thrombin, while amiodarone works by prolonging cardiac action potentials and refractory periods in myocardial tissue.

02

Targets

CaV (Voltage-gated calcium channel protein complex)Kir (Inward-rectifier potassium channels)F2 (Thrombin)NaV (Voltage-gated sodium channels)ABCB1 (P-glycoprotein)

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