Drug intelligence / Profile preview

acetylsalicylic acid + clopidogrel + acenocoumarol

Development stage
Unknown
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

The combination of acetylsalicylic acid, clopidogrel, and acenocoumarol is used in specific cardiovascular conditions where both antiplatelet and anticoagulant effects are needed. This combination therapy is primarily used in patients with acute coronary syndrome, particularly after procedures like percutaneous coronary intervention (PCI). ## Mechanism of Action This is a triple combination therapy with complementary mechanisms: - **Acetylsalicylic acid (Aspirin)** blocks the enzyme prostaglandin cyclo-oxygenase, reducing thromboxane production which normally helps clots form by attaching platelets together[5]. - **Clopidogrel** blocks ADP from attaching to receptors on platelet surfaces, preventing platelets from becoming "sticky" and reducing blood clot formation risk[5]. It's a platelet inhibitor that works by preventing platelets from clumping together in the blood[8]. - **Acenocoumarol** is an anticoagulant that inhibits vitamin K reductase, depleting the reduced form of vitamin K (vitamin KH2). This limits the gamma-carboxylation and subsequent activation of vitamin K-dependent coagulant proteins (factors II, VII, IX, and X)[3]. ## Clinical Use The triple combination has been studied in patients after PCI and in those with unstable angina[1]. In one study, aspirin and clopidogrel were indicated in 36 patients after PCI, and in 7 for unstable angina, with acenocoumarol added for anticoagulation[1]. ## Safety Considerations The combination carries an increased risk of bleeding complications. Monitoring parameters typically include hematocrit, hemoglobin, international normalized ratio (INR), and liver function tests[3]. The risk or severity of bleeding can be increased when these medications are used together[4]. ## Alternative Combinations For many cardiovascular conditions, dual antiplatelet therapy with aspirin and clopidogrel is more common than the triple therapy that includes acenocoumarol. The dual combination has been shown to be more effective at preventing events such as heart attacks than acetylsalicylic acid alone[2].

02

Targets

VKORC1 (Vitamin K epoxide reductase complex subunit 1)P2Y12 (Purinergic P2Y12 receptor)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PGHS-1 (Prostaglandin G/H Synthase 1)

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