Target intelligence / Profile preview

Ticagrelor, Apixaban, and Rivaroxaban

Molecular classification
P2Y12 receptor antagonist, Factor Xa inhibitor, Small molecule
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Overview

Ticagrelor, Apixaban, and Rivaroxaban are three distinct pharmacological agents used in antithrombotic therapy, rather than a single biological target. Ticagrelor is a cyclopentyltriazolopyrimidine that acts as a reversible, direct-acting P2Y12 receptor antagonist, inhibiting adenosine diphosphate-induced platelet aggregation (StatPearls, 2023). In contrast, Apixaban and Rivaroxaban are direct oral anticoagulants (DOACs) that selectively and reversibly inhibit Coagulation Factor Xa, which is the rate-limiting step in the coagulation cascade for thrombin production (NIH, 2022; PubMed, 2021). These drugs are clinically indicated for the prevention of stroke in non-valvular atrial fibrillation and the treatment of venous thromboembolism, while Ticagrelor is specifically used for acute coronary syndrome (FDA, 2021). Because this entry combines an antiplatelet agent with two anticoagulants that target different proteins (P2Y12 and Factor Xa), it represents a collection of drugs rather than a specific molecular target. Consequently, this grouping is considered incorrect for the purpose of single-target identification.

Other names
BrilintaEliquisXareltoP2Y12 inhibitors and Factor Xa inhibitors
02

Mechanism of action

Ticagrelor is a P2Y12 receptor antagonist; Apixaban and Rivaroxaban are direct Factor Xa inhibitors.

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Biological functions

Platelet aggregationBlood coagulationHemostasisThrombin generation
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Disease associations

Cardiovascular diseaseThrombosisAtrial fibrillationAcute coronary syndromeStroke
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Safety considerations

Major bleedingGastrointestinal hemorrhageIntracranial hemorrhageDrug-drug interactions with CYP3A4 inhibitors/inducers
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Interacting drugs

Ticagrelor

2 more in the full profile.

07

Biomarkers

Anti-Xa activityPlatelet reactivity units (PRU)Prothrombin time (PT)

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