Drug intelligence / Profile preview

dabigatran etexilate + ticagrelor

Development stage
Phase 4
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **combination of dabigatran etexilate**, a direct oral anticoagulant (DOAC) that acts as a reversible, direct thrombin inhibitor, and **ticagrelor**, an oral antiplatelet drug that acts as a P2Y12 receptor antagonist.\n- **Dabigatran etexilate** is hydrolyzed to dabigatran, which inhibits thrombin (factor IIa), preventing the conversion of fibrinogen to fibrin and consequently inhibiting blood clot formation.\n- **Ticagrelor** inhibits the P2Y12 receptor on platelets, preventing ADP-mediated platelet activation and aggregation, thus reducing thrombosis.\nThis **combination is used in clinical practice, but is not marketed as a unique co-formulated product**—both agents are prescribed together when enhanced antithrombotic therapy is needed, for example in selected cardiovascular conditions.\nThis pairing increases antithrombotic effect but also raises bleeding risk. Pharmacokinetic and pharmacodynamic interaction exists: ticagrelor increases dabigatran exposure and bleeding risk; this is due to ticagrelor’s weak inhibition of P-glycoprotein (P-gp), which affects dabigatran disposition[1][2][5].

Other names
dabigatran etexilateBrilique (for ticagrelor in some regions)
02

Targets

P2Y12 (Purinergic P2Y12 receptor)F2 (Thrombin)

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