Vorapaxar
Vorapaxar is a first-in-class protease-activated receptor 1 (PAR-1) antagonist that irreversibly blocks thrombin-mediated platelet activation at the PAR-1 receptor on platelet surfaces, reducing platelet aggregation without affecting other coagulation pathways. It is approved for reduction of thrombotic cardiovascular events in patients with established myocardial infarction or peripheral arterial disease, used as adjunctive antiplatelet therapy. Its novel mechanism complements ADP-receptor antagonists by targeting thrombin-mediated platelet activation.
分子量
492.6000 g/mol
LogP
5.30
TPSA
77.50 Ų
リピンスキーの五則
適合
治療領域
作用機序
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
2D構造
Cite this structure
Embed this structure
SMILES
CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1
InChI
InChI=1S/C29H33FN2O4/c1-3-35-29(34)32-23-10-11-24-20(14-23)15-26-27(17(2)36-28(26)33)25(24)12-9-22-8-7-19(16-31-22)18-5-4-6-21(30)13-18/h4-9,12-13,16-17,20,23-27H,3,10-11,14-15H2,1-2H3,(H,32,34)/b12-9+/t17-,20+,23-,24-,25+,26-,27+/m1/s1
Molecular Formula
C29H33FN2O4
HBD / HBA
1 / 6
回転可能結合数
6
重原子数
36
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
よくある質問
Vorapaxar is a first-in-class protease-activated receptor 1 (PAR-1) antagonist that irreversibly blocks thrombin-mediated platelet activation at the PAR-1 receptor on platelet surfaces, reducing platelet aggregation without affecting other coagulation pathways. It is approved for reduction of thrombotic cardiovascular events in patients with established myocardial infarction or peripheral arterial disease, used as adjunctive antiplatelet therapy. Its novel mechanism complements ADP-receptor antagonists by targeting thrombin-mediated platelet activation.
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Yes, Vorapaxar is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL493982. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 10077130. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
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