Peringatan Keamanan

Betrixaban presents a minimal hepatotoxicity, which is the main adverse effect found in this class of drugs. Some of the major adverse effects of Betrixaban are bleeding or hypersensitivity A27287.

Betrixaban

DB12364

small molecule approved investigational

Deskripsi

Betrixaban is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa A7708. It was selected among all lead compounds due to its low hERG channel affinity while sustaining its factor Xa inhibition capacity A27286. Betrixaban, now developed by Portola Pharmaceuticals Inc., is prescribed as a venous thromboembolism (VTE) prophylactic for adult patients with moderate to severe restricted motility or with other risks for VTE A27285. VTE can be manifested as deep vein thrombosis or pulmonary embolism and it is a leading cause of preventable death in hospitalized patients A27287.

Struktur Molekul 2D

Berat 451.91
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Betrixaban presents a long half-life of between 19-27 hours [A7708].
Volume Distribusi The apparent volume of distribution os 32 L/kg [FDA label].
Klirens (Clearance) Betrixaban presents a minimal renal clearance (being 5-7% of the administered dose) [A27287].

Absorpsi

Betrixaban presents a rapid absorption at a dose of 80 mg. Its peak plasma concentration is registered within 3-4 hours after oral administration in healthy humans. The oral bioavailability is 34%, and it can be reduced with the consumption of foodA27287. Specifically, the Cmax and AUC is reduced by an average of 70% and 61% with a low-fat meal, and 50% and 48% with a high-fat meal compared to the fasted state, an effect which is apparent up to six hours following food intake.FDA label

Metabolisme

One of the major characteristics of Betrixaban is its minimal hepatic metabolism (< 1%), preventing potential accumulation with liver impariment. Unchanged Betrixaban is the main form found in human plasma, followed by two hydolitic CYP-independent inactive metabolites (15-18%). The minimal hepatic metabolism produces an unlikely drug-to-drug interaction with inhibitors or agonists of CYP450 A27287.

Rute Eliminasi

Betrixaban is reported to present mainly a gastrointestinal elimination route, it has been shown that even 85% of it gets disposed in the feces and only 11% of it can be found in the urine A7708.

Interaksi Makanan

3 Data
  • 1. Avoid herbs and supplements with anticoagulant/antiplatelet activity. These herbs may increase the risk of bleeding. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • 2. Take at the same time every day.
  • 3. Take with food. Betrixaban should be taken with food. The Cmax and AUC of betrixaban are decreased by approximately 60% and 55% when administered together with a 900 calorie meal.

Interaksi Obat

837 Data
Apixaban Apixaban may increase the anticoagulant activities of Betrixaban.
Dabigatran etexilate Dabigatran etexilate may increase the anticoagulant activities of Betrixaban.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Betrixaban.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Betrixaban is combined with Deferasirox.
Ursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Cholic Acid.
Glycocholic acid The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Deoxycholic acid.
Obeticholic acid The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Hyodeoxycholic Acid.
Taurocholic acid The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Taurocholic acid.
Edoxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Betrixaban.
Ibrutinib The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Betrixaban.
Obinutuzumab The risk or severity of bleeding and hemorrhage can be increased when Betrixaban is combined with Obinutuzumab.
Rivaroxaban Betrixaban may increase the anticoagulant activities of Rivaroxaban.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Betrixaban is combined with Sugammadex.
Tibolone Tibolone may increase the anticoagulant activities of Betrixaban.
Urokinase Urokinase may increase the anticoagulant activities of Betrixaban.
Vitamin E Vitamin E may increase the anticoagulant activities of Betrixaban.
Vorapaxar The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Betrixaban.
Ranolazine The serum concentration of Betrixaban can be increased when it is combined with Ranolazine.
Ginkgo biloba Ginkgo biloba may increase the anticoagulant activities of Betrixaban.
Ifosfamide The risk or severity of bleeding can be increased when Ifosfamide is combined with Betrixaban.
Pentoxifylline The therapeutic efficacy of Betrixaban can be increased when used in combination with Pentoxifylline.
Pentosan polysulfate Pentosan polysulfate may increase the anticoagulant activities of Betrixaban.
Levocarnitine The therapeutic efficacy of Betrixaban can be increased when used in combination with Levocarnitine.
Diethylstilbestrol Diethylstilbestrol may decrease the anticoagulant activities of Betrixaban.
Chlorotrianisene Chlorotrianisene may decrease the anticoagulant activities of Betrixaban.
Conjugated estrogens Conjugated estrogens may decrease the anticoagulant activities of Betrixaban.
Mestranol The risk or severity of adverse effects can be increased when Mestranol is combined with Betrixaban.
Estrone sulfate Estrone sulfate may decrease the anticoagulant activities of Betrixaban.
Quinestrol Quinestrol may decrease the anticoagulant activities of Betrixaban.
Hexestrol Hexestrol may decrease the anticoagulant activities of Betrixaban.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may decrease the anticoagulant activities of Betrixaban.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may decrease the anticoagulant activities of Betrixaban.
Polyestradiol phosphate Polyestradiol phosphate may decrease the anticoagulant activities of Betrixaban.
Esterified estrogens Esterified estrogens may decrease the anticoagulant activities of Betrixaban.
Zeranol Zeranol may decrease the anticoagulant activities of Betrixaban.
Equol Equol may decrease the anticoagulant activities of Betrixaban.
Methallenestril Methallenestril may decrease the anticoagulant activities of Betrixaban.
Epimestrol Epimestrol may decrease the anticoagulant activities of Betrixaban.
Moxestrol Moxestrol may decrease the anticoagulant activities of Betrixaban.
Estradiol acetate Estradiol acetate may decrease the anticoagulant activities of Betrixaban.
Estradiol benzoate Estradiol benzoate may decrease the anticoagulant activities of Betrixaban.
Estradiol cypionate Estradiol cypionate may decrease the anticoagulant activities of Betrixaban.
Estradiol valerate Estradiol valerate may decrease the anticoagulant activities of Betrixaban.
Biochanin A Biochanin A may decrease the anticoagulant activities of Betrixaban.
Formononetin Formononetin may decrease the anticoagulant activities of Betrixaban.
Estriol Estriol may decrease the anticoagulant activities of Betrixaban.
Limaprost The risk or severity of adverse effects can be increased when Limaprost is combined with Betrixaban.
Omacetaxine mepesuccinate The risk or severity of bleeding can be increased when Betrixaban is combined with Omacetaxine mepesuccinate.
Omega-3 fatty acids Omega-3 fatty acids may increase the anticoagulant activities of Betrixaban.
Tositumomab The risk or severity of bleeding and hemorrhage can be increased when Betrixaban is combined with Tositumomab.
Collagenase clostridium histolyticum The risk or severity of adverse effects can be increased when Betrixaban is combined with Collagenase clostridium histolyticum.
Carbimazole Carbimazole may increase the anticoagulant activities of Betrixaban.
Propylthiouracil Propylthiouracil may increase the anticoagulant activities of Betrixaban.
Methimazole Methimazole may increase the anticoagulant activities of Betrixaban.
3,5-Diiodotyrosine 3,5-Diiodotyrosine may increase the anticoagulant activities of Betrixaban.
Potassium Iodide Potassium Iodide may increase the anticoagulant activities of Betrixaban.
Dibromotyrosine Dibromotyrosine may increase the anticoagulant activities of Betrixaban.
Potassium perchlorate Potassium perchlorate may increase the anticoagulant activities of Betrixaban.
Methylthiouracil Methylthiouracil may increase the anticoagulant activities of Betrixaban.
Benzylthiouracil Benzylthiouracil may increase the anticoagulant activities of Betrixaban.
Octylphenoxy polyethoxyethanol The therapeutic efficacy of Betrixaban can be decreased when used in combination with Octylphenoxy polyethoxyethanol.
Trestolone The therapeutic efficacy of Betrixaban can be decreased when used in combination with Trestolone.
Ulipristal The therapeutic efficacy of Betrixaban can be decreased when used in combination with Ulipristal.
Cloprostenol The therapeutic efficacy of Betrixaban can be decreased when used in combination with Cloprostenol.
Gossypol The therapeutic efficacy of Betrixaban can be decreased when used in combination with Gossypol.
Progesterone The therapeutic efficacy of Betrixaban can be decreased when used in combination with Progesterone.
Etonogestrel The therapeutic efficacy of Betrixaban can be decreased when used in combination with Etonogestrel.
Dydrogesterone Dydrogesterone may decrease the anticoagulant activities of Betrixaban.
Allylestrenol Allylestrenol may decrease the anticoagulant activities of Betrixaban.
Norelgestromin The therapeutic efficacy of Betrixaban can be decreased when used in combination with Norelgestromin.
Hydroxyprogesterone caproate The therapeutic efficacy of Betrixaban can be decreased when used in combination with Hydroxyprogesterone caproate.
Medrogestone Medrogestone may decrease the anticoagulant activities of Betrixaban.
Altrenogest Altrenogest may decrease the anticoagulant activities of Betrixaban.
Nomegestrol The therapeutic efficacy of Betrixaban can be decreased when used in combination with Nomegestrol.
Gestonorone Gestonorone may decrease the anticoagulant activities of Betrixaban.
Methylestrenolone Methylestrenolone may decrease the anticoagulant activities of Betrixaban.
Promegestone Promegestone may decrease the anticoagulant activities of Betrixaban.
Etynodiol The therapeutic efficacy of Betrixaban can be decreased when used in combination with Etynodiol.
Hydroxyprogesterone Hydroxyprogesterone may decrease the anticoagulant activities of Betrixaban.
Quingestanol acetate Quingestanol acetate may decrease the anticoagulant activities of Betrixaban.
Aminosalicylic acid The risk or severity of bleeding can be increased when Aminosalicylic acid is combined with Betrixaban.
Bismuth subsalicylate The risk or severity of bleeding can be increased when Bismuth subsalicylate is combined with Betrixaban.
Dersalazine The risk or severity of bleeding can be increased when Dersalazine is combined with Betrixaban.
Phenyl aminosalicylate The risk or severity of bleeding can be increased when Phenyl aminosalicylate is combined with Betrixaban.
Methyl salicylate The risk or severity of bleeding can be increased when Methyl salicylate is combined with Betrixaban.
Trolamine salicylate The risk or severity of bleeding can be increased when Trolamine salicylate is combined with Betrixaban.
Aloxiprin The risk or severity of bleeding can be increased when Aloxiprin is combined with Betrixaban.
Choline salicylate The risk or severity of bleeding can be increased when Choline salicylate is combined with Betrixaban.
Thiosalicylic acid The risk or severity of bleeding can be increased when Thiosalicylic acid is combined with Betrixaban.
Abciximab The risk or severity of bleeding can be increased when Abciximab is combined with Betrixaban.
Eptifibatide The risk or severity of bleeding can be increased when Eptifibatide is combined with Betrixaban.

Target Protein

Coagulation factor X F10

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18096568
    Turpie AG: New oral anticoagulants in atrial fibrillation. Eur Heart J. 2008 Jan;29(2):155-65. Epub 2007 Dec 19.
  • PMID: 23487517
    Connolly SJ, Eikelboom J, Dorian P, Hohnloser SH, Gretler DD, Sinha U, Ezekowitz MD: Betrixaban compared with warfarin in patients with atrial fibrillation: results of a phase 2, randomized, dose-ranging study (Explore-Xa). Eur Heart J. 2013 May;34(20):1498-505. doi: 10.1093/eurheartj/eht039. Epub 2013 Mar 13.
  • PMID: 19297154
    Zhang P, Huang W, Wang L, Bao L, Jia ZJ, Bauer SM, Goldman EA, Probst GD, Song Y, Su T, Fan J, Wu Y, Li W, Woolfrey J, Sinha U, Wong PW, Edwards ST, Arfsten AE, Clizbe LA, Kanter J, Pandey A, Park G, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY: Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenz amide, a highly potent, selective, and orally efficacious factor Xa inhibitor. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2179-85. doi: 10.1016/j.bmcl.2009.02.111. Epub 2009 Mar 3.
  • PMID: 26170684
    Chan NC, Bhagirath V, Eikelboom JW: Profile of betrixaban and its potential in the prevention and treatment of venous thromboembolism. Vasc Health Risk Manag. 2015 Jun 26;11:343-51. doi: 10.2147/VHRM.S63060. eCollection 2015.
  • PMID: 25673997
    Cabral KP, Ansell JE: The role of factor Xa inhibitors in venous thromboembolism treatment. Vasc Health Risk Manag. 2015 Jan 30;11:117-23. doi: 10.2147/VHRM.S39726. eCollection 2015.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Bevyxxa
    Capsule, gelatin coated • 80 mg/1 • Oral • US • Approved
  • Bevyxxa
    Capsule, gelatin coated • 40 mg/1 • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

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