Loading Pathway...
Error: Pathway image not found.
Hide
Pathway Description
Vorapaxar Action Pathway
Homo sapiens
Drug Action Pathway
Vorapaxar also known as Zontivity, is an inhibitor for platelet aggregation used to treat patients with a history of myocardial infarction or peripheral arterial disease to reduce the chance of thrombotic cardiovascular events. Vorapaxar inhibits protease-activated receptor 1 (PAR-1), which is a G protein-coupled receptor that is expressed on the platelet. Inhibition of PAR-1 prevents platelet aggregation and activation. Vorapaxar is administered orally and rapidly absorbs and travels through the bloodstream. It is metabolized to major metabolites M20 and M19 by CYP3A4 and CYP2J2. This is then eliminated primarily through feces and urine. Due to the anticoagulant and antiplatelet nature, herbs and supplements with similar activity should be avoided such as garlic, ginger, bilberry, danshen, piracetam and ginkgo biloba. St.John's Wort should also be avoided as it induces CYP3A metabolism and will reduce the concentration of Vorapaxar. Caution should be exercised with grapefruit products, as coadministration with strong inhibitors should be avoided.
References
Vorapaxar Pathway References
Ghosal A, Lu X, Penner N, Gao L, Ramanathan R, Chowdhury SK, Kishnani NS, Alton KB: Identification of human liver cytochrome P450 enzymes involved in the metabolism of SCH 530348 (Vorapaxar), a potent oral thrombin protease-activated receptor 1 antagonist. Drug Metab Dispos. 2011 Jan;39(1):30-8. doi: 10.1124/dmd.110.035493. Epub 2010 Oct 6.
Pubmed: 20926621
Lhermusier T, Baker NC, Waksman R: Overview of the 2014 Food and Drug Administration Cardiovascular and Renal Drugs Advisory Committee meeting regarding cangrelor. Am J Cardiol. 2015 Apr 15;115(8):1154-61. doi: 10.1016/j.amjcard.2015.01.551. Epub 2015 Feb 3.
Pubmed: 25728646
Tricoci P, Huang Z, Held C, Moliterno DJ, Armstrong PW, Van de Werf F, White HD, Aylward PE, Wallentin L, Chen E, Lokhnygina Y, Pei J, Leonardi S, Rorick TL, Kilian AM, Jennings LH, Ambrosio G, Bode C, Cequier A, Cornel JH, Diaz R, Erkan A, Huber K, Hudson MP, Jiang L, Jukema JW, Lewis BS, Lincoff AM, Montalescot G, Nicolau JC, Ogawa H, Pfisterer M, Prieto JC, Ruzyllo W, Sinnaeve PR, Storey RF, Valgimigli M, Whellan DJ, Widimsky P, Strony J, Harrington RA, Mahaffey KW: Thrombin-receptor antagonist vorapaxar in acute coronary syndromes. N Engl J Med. 2012 Jan 5;366(1):20-33. doi: 10.1056/NEJMoa1109719. Epub 2011 Nov 13.
Pubmed: 22077816
Cheng JW, Colucci V, Howard PA, Nappi JM, Spinler SA: Vorapaxar in atherosclerotic disease management. Ann Pharmacother. 2015 May;49(5):599-606. doi: 10.1177/1060028015571410. Epub 2015 Feb 13.
Pubmed: 25680760
Highlighted elements will appear in red.
Highlight Compounds
Highlight Proteins
Enter relative concentration values (without units). Elements will be highlighted in a color gradient where red = lowest concentration and green = highest concentration. For the best results, view the pathway in Black and White.
Visualize Compound Data
Visualize Protein Data
Downloads
Settings