Peringatan Keamanan

There is an increased risk of bleeding and intracranial hemorrhage (ICH), which is why the use of vorapaxar is contraindicated in patients with a history of stroke, trans-ischemic attack (TIA), ICH, or active pathological bleeding such as peptic ulcer. Animal studies have suggested that there is a low probability of embryo/fetal toxicities, however there are no adequate and well-controlled studies describing use in pregnant women. Vorapaxar should also be avoided during breastfeeding as it is unknown whether vorapaxar or its metabolites are excreted in human milk, however it has been shown to be actively secreted in the milk of rats.

Vorapaxar

DB09030

small molecule approved

Deskripsi

Vorapaxar is a tricyclic himbacine-derived selective inhibitor of protease activated receptor (PAR-1) indicated for reducing the incidence of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or with peripheral arterial disease (PAD). By inhibiting PAR-1, a thrombin receptor expressed on platelets, vorapaxar prevents thrombin-related platelet aggregation.

Struktur Molekul 2D

Berat 492.5817
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Vorapaxar has an effective half life of 3-4 days and an apparent terminal half life of 8 days.
Volume Distribusi 424 L
Klirens (Clearance) -

Absorpsi

After oral administration, vorapaxar is rapidly absorbed and peak concentrations occur at a median tmax of 1 hour under faster conditions. Vorapaxar may be taken with or without food as ingestion with a high-fat meal did not result in meaningful changes in AUC. The mean absolute bioavailability is 100%.

Metabolisme

Vorapaxar is metabolized to its major circulating metabolite, M20, and its predominant metabolite excreted into feces, M19, by CYP3A4 and CYP 2J2.

Rute Eliminasi

Vorapaxar is primarily eliminated as its metabolite M19 through the feces (91.5%), and partially eliminated in the urine (8.5%).

Interaksi Makanan

4 Data
  • 1. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Additive antiplatelet activity may increase the risk of bleeding. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • 2. Avoid St. John's Wort. This herb induces the CYP3A metabolism of vorapaxar and may reduce its serum concentration.
  • 3. Exercise caution with grapefruit products. Coadministration of vorapaxar with moderate CYP3A4 inhibitors does not require intervention, but coadministration with strong inhibitors should be avoided.
  • 4. Take with or without food.

Interaksi Obat

1118 Data
Apixaban Apixaban may increase the anticoagulant activities of Vorapaxar.
Dabigatran etexilate Dabigatran etexilate may increase the anticoagulant activities of Vorapaxar.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Vorapaxar.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Vorapaxar is combined with Deferasirox.
Edoxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Vorapaxar.
Ibrutinib The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Vorapaxar.
Rivaroxaban Vorapaxar may increase the anticoagulant activities of Rivaroxaban.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Sugammadex.
Tibolone Tibolone may increase the anticoagulant activities of Vorapaxar.
Urokinase Urokinase may increase the anticoagulant activities of Vorapaxar.
Lepirudin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Lepirudin.
Bivalirudin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Bivalirudin.
Alteplase The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Alteplase.
Reteplase The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Reteplase.
Anistreplase The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Anistreplase.
Tenecteplase The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Tenecteplase.
Abciximab The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Abciximab.
Drotrecogin alfa The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Drotrecogin alfa.
Streptokinase The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Streptokinase.
Dicoumarol The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Dicoumarol.
Argatroban The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Argatroban.
Ardeparin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Ardeparin.
Phenindione The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Phenindione.
Fondaparinux The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Fondaparinux.
Warfarin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Warfarin.
Pentosan polysulfate The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Pentosan polysulfate.
Phenprocoumon The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Phenprocoumon.
Dipyridamole The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Dipyridamole.
Heparin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Heparin.
Enoxaparin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Enoxaparin.
Epoprostenol The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Epoprostenol.
Acenocoumarol The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Coumarin.
Ximelagatran The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Ximelagatran.
Desmoteplase The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Desmoteplase.
Defibrotide The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Defibrotide.
Ancrod The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Ancrod.
Beraprost The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Beraprost.
Prasugrel The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Prasugrel.
Sulodexide The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Sulodexide.
Semuloparin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Semuloparin.
Idraparinux The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Idraparinux.
Cangrelor The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Cangrelor.
Astaxanthin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Astaxanthin.
Otamixaban The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Otamixaban.
Amediplase The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Amediplase.
Danaparoid The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Danaparoid.
Dalteparin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Dalteparin.
Tinzaparin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Tinzaparin.
(R)-warfarin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Ethyl biscoumacetate.
Nadroparin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Nadroparin.
Triflusal The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Triflusal.
Ticagrelor The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Ticagrelor.
Ditazole The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Ditazole.
Sodium citrate The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Sodium citrate.
Dextran The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Dextran.
Bemiparin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Bemiparin.
Parnaparin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Parnaparin.
Desirudin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Desirudin.
Antithrombin Alfa The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Antithrombin Alfa.
Protein C The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Protein C.
Antithrombin III human The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Antithrombin III human.
Letaxaban The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Letaxaban.
Darexaban The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Darexaban.
Betrixaban The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Betrixaban.
Nafamostat The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Nafamostat.
Monteplase The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Monteplase.
Gabexate The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Gabexate.
Fluindione The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Fluindione.
Protein S human The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Protein S human.
Brinase The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Brinase.
Clorindione The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Clorindione.
Diphenadione The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Diphenadione.
Tioclomarol The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Tioclomarol.
Melagatran The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Melagatran.
Saruplase The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Saruplase.
(S)-Warfarin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with (S)-Warfarin.
Tocopherylquinone The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Tocopherylquinone.
Dabigatran The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Dabigatran.
Edetic acid The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Edetic acid.
Troxerutin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Troxerutin.
Reviparin The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Reviparin.
Dermatan sulfate The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Dermatan sulfate.
SR-123781A The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with SR-123781A.
Ursodeoxycholic acid The risk or severity of adverse effects can be increased when Vorapaxar is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of adverse effects can be increased when Vorapaxar is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of adverse effects can be increased when Vorapaxar is combined with Cholic Acid.
Glycocholic acid The risk or severity of adverse effects can be increased when Vorapaxar is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of adverse effects can be increased when Vorapaxar is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of adverse effects can be increased when Vorapaxar is combined with Taurocholic acid.
Obeticholic acid The risk or severity of adverse effects can be increased when Vorapaxar is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of adverse effects can be increased when Vorapaxar is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of adverse effects can be increased when Vorapaxar is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of adverse effects can be increased when Vorapaxar is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of adverse effects can be increased when Vorapaxar is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of adverse effects can be increased when Vorapaxar is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of adverse effects can be increased when Vorapaxar is combined with Hyodeoxycholic Acid.
Glucosamine Glucosamine may increase the antiplatelet activities of Vorapaxar.

Target Protein

Proteinase-activated receptor 1 F2R

Referensi & Sumber

Artikel (PubMed)
  • PMID: 20926621
    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.
  • PMID: 25728646
    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.
  • PMID: 22077816
    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.
  • PMID: 25680760
    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.

Contoh Produk & Brand

Produk: 4 • International brands: 0
Produk
  • Zontivity
    Tablet, film coated • 2.08 mg/1 • Oral • US • Approved
  • Zontivity
    Tablet, film coated • 2.08 mg/1 • Oral • US • Approved
  • Zontivity
    Tablet • 2.5 mg • Oral • Canada • Approved
  • Zontivity
    Tablet, film coated • 2.08 mg/1 • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

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