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Synonyms: SCH 530348 | SCH-530348 | SCH530348 | Zontivity®
vorapaxar is an approved drug (FDA (2014))
Compound class: Synthetic organic
Comment: Vorapaxar is an orally active thrombin receptor (PAR1) antagonist based on the natural product himbacine , that is used as an anti-thrombosis drug.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: vorapaxar
|No information available.|
|Summary of Clinical Use|
|Approved to reduce the risk of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or with peripheral arterial disease (PAD).
SARS-CoV-2 and COVID-19: Antagonism of PAR1 and the resulting anti-thrombotic action may be applicable to the management of pathological thrombosis and endotheliitis in patients with severe COVID-19 .
|Mechanism Of Action and Pharmacodynamic Effects|
|Vorapaxar is an antagonist of the protease-activated receptor-1 (PAR1) expressed on platelets. The effect is to inhibit thrombin-induced and thrombin receptor agonist peptide (TRAP)-induced platelet aggregation. Drug action reduces the formation of blood clots and reduces the risk of cardiovascular events and stroke. Due to its long receptor dissociation half-life of (~20 hours) it acts effectively in an irreversible fashion. Its very long elimination half-life, means it is long-acting, displaying significant inhibition of platelet aggregation for up to 4 weeks after discontinuation .|
For extended ADME data see the following: