Drug intelligence / Profile preview

dabigatran etexilate + verapamil

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

Overview

**dabigatran etexilate + verapamil** is a combination of two small molecule drugs: dabigatran etexilate, an oral prodrug of dabigatran, and verapamil. Dabigatran etexilate is a direct thrombin inhibitor that impairs the conversion of fibrinogen to fibrin, thus preventing blood clot formation. Verapamil is a calcium channel blocker used primarily for cardiac indications, but also acts as an inhibitor of P-glycoprotein (P-gp). When administered together, verapamil increases the bioavailability of dabigatran etexilate by inhibiting its P-gp-mediated extrusion at sites of intestinal absorption, leading to higher plasma concentrations of dabigatran. This interaction does not significantly change the functional relationship between dabigatran concentration and anticoagulation effect, but it markedly increases the risk of bleeding events due to elevated dabigatran exposure. The combination raises specific safety concerns, and dose timing can influence the magnitude of the interaction—administering dabigatran etexilate at least 2 hours before verapamil reduces the interaction. The combination is not formulated as a single product and is used off-label when both drugs are co-prescribed in clinical practice for patients with indications requiring both anticoagulation and cardiac management[1][3][5][7].

Other names
dabigatran + verapamil
02

Targets

F2 (Thrombin)ABCB1 (P-glycoprotein)

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