Defibrotide

DB04932

biotech approved investigational

Deskripsi

Defibrotide is the sodium salt of a mixture of single-stranded oligodeoxyribonucleotides derived from porcine mucosal DNA. It has been shown to have antithrombotic, anti-inflammatory and anti-ischemic properties (but without associated significant systemic anticoagulant effects). It is marketed under the brand names Dasovas (FM), Noravid, and Prociclide in a variety of countries. In the USA it is was approved in March, 2016 as Defitelio.

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) t1/2-alpha = minutes (10-20 minutes in rat); t1/2-beta = a few hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Bioavailability is 58-70% following oral administration, compared to parenteral forms (i.v. and i.m. = 100%).

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

1 Data
  • 1. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Interaksi Obat

646 Data
Apixaban Apixaban may increase the anticoagulant activities of Defibrotide.
Dabigatran etexilate Dabigatran etexilate may increase the anticoagulant activities of Defibrotide.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Defibrotide.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Defibrotide is combined with Deferasirox.
Edoxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Defibrotide.
Ibrutinib The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Defibrotide.
Rivaroxaban Defibrotide may increase the anticoagulant activities of Rivaroxaban.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Defibrotide is combined with Sugammadex.
Tibolone Tibolone may increase the anticoagulant activities of Defibrotide.
Urokinase Urokinase may increase the anticoagulant activities of Defibrotide.
Vorapaxar The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Defibrotide.
Aprotinin The therapeutic efficacy of Defibrotide can be decreased when used in combination with Aprotinin.
Ursodeoxycholic acid The risk or severity of adverse effects can be increased when Defibrotide is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of adverse effects can be increased when Defibrotide is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of adverse effects can be increased when Defibrotide is combined with Cholic Acid.
Glycocholic acid The risk or severity of adverse effects can be increased when Defibrotide is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of adverse effects can be increased when Defibrotide is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of adverse effects can be increased when Defibrotide is combined with Taurocholic acid.
Obeticholic acid The risk or severity of adverse effects can be increased when Defibrotide is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of adverse effects can be increased when Defibrotide is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of adverse effects can be increased when Defibrotide is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of adverse effects can be increased when Defibrotide is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of adverse effects can be increased when Defibrotide is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of adverse effects can be increased when Defibrotide is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of adverse effects can be increased when Defibrotide is combined with Hyodeoxycholic Acid.
Glucosamine Glucosamine may increase the antiplatelet activities of Defibrotide.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Defibrotide is combined with Ibritumomab tiuxetan.
Obinutuzumab The risk or severity of adverse effects can be increased when Defibrotide is combined with Obinutuzumab.
Tipranavir Tipranavir may increase the antiplatelet activities of Defibrotide.
Vitamin E Vitamin E may increase the antiplatelet activities of Defibrotide.
Ginkgo biloba Ginkgo biloba may increase the anticoagulant activities of Defibrotide.
Ifosfamide The risk or severity of bleeding can be increased when Ifosfamide is combined with Defibrotide.
Quinine The therapeutic efficacy of Defibrotide can be increased when used in combination with Quinine.
Quinidine The therapeutic efficacy of Defibrotide can be increased when used in combination with Quinidine.
Tamoxifen The risk or severity of bleeding can be increased when Tamoxifen is combined with Defibrotide.
Toremifene The risk or severity of bleeding can be increased when Toremifene is combined with Defibrotide.
Pentoxifylline The therapeutic efficacy of Defibrotide can be increased when used in combination with Pentoxifylline.
Pentosan polysulfate The risk or severity of adverse effects can be increased when Pentosan polysulfate is combined with Defibrotide.
Levocarnitine The therapeutic efficacy of Defibrotide can be increased when used in combination with Levocarnitine.
Diethylstilbestrol Diethylstilbestrol may decrease the anticoagulant activities of Defibrotide.
Chlorotrianisene Chlorotrianisene may decrease the anticoagulant activities of Defibrotide.
Conjugated estrogens Conjugated estrogens may decrease the anticoagulant activities of Defibrotide.
Mestranol The risk or severity of adverse effects can be increased when Mestranol is combined with Defibrotide.
Estrone sulfate Estrone sulfate may decrease the anticoagulant activities of Defibrotide.
Quinestrol Quinestrol may decrease the anticoagulant activities of Defibrotide.
Hexestrol Hexestrol may decrease the anticoagulant activities of Defibrotide.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may decrease the anticoagulant activities of Defibrotide.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may decrease the anticoagulant activities of Defibrotide.
Polyestradiol phosphate Polyestradiol phosphate may decrease the anticoagulant activities of Defibrotide.
Esterified estrogens Esterified estrogens may decrease the anticoagulant activities of Defibrotide.
Zeranol Zeranol may decrease the anticoagulant activities of Defibrotide.
Equol Equol may decrease the anticoagulant activities of Defibrotide.
Methallenestril Methallenestril may decrease the anticoagulant activities of Defibrotide.
Epimestrol Epimestrol may decrease the anticoagulant activities of Defibrotide.
Moxestrol Moxestrol may decrease the anticoagulant activities of Defibrotide.
Estradiol acetate Estradiol acetate may decrease the anticoagulant activities of Defibrotide.
Estradiol benzoate Estradiol benzoate may decrease the anticoagulant activities of Defibrotide.
Estradiol cypionate Estradiol cypionate may decrease the anticoagulant activities of Defibrotide.
Estradiol valerate Estradiol valerate may decrease the anticoagulant activities of Defibrotide.
Biochanin A Biochanin A may decrease the anticoagulant activities of Defibrotide.
Formononetin Formononetin may decrease the anticoagulant activities of Defibrotide.
Estriol Estriol may decrease the anticoagulant activities of Defibrotide.
Icosapent The risk or severity of bleeding and hemorrhage can be increased when Icosapent is combined with Defibrotide.
Mesalazine The risk or severity of bleeding can be increased when Mesalazine is combined with Defibrotide.
Indomethacin The risk or severity of bleeding and hemorrhage can be increased when Indomethacin is combined with Defibrotide.
Nabumetone The risk or severity of bleeding and hemorrhage can be increased when Nabumetone is combined with Defibrotide.
Ketorolac The risk or severity of bleeding and hemorrhage can be increased when Ketorolac is combined with Defibrotide.
Tenoxicam The risk or severity of bleeding and hemorrhage can be increased when Tenoxicam is combined with Defibrotide.
Celecoxib The risk or severity of bleeding and hemorrhage can be increased when Celecoxib is combined with Defibrotide.
Tolmetin The risk or severity of bleeding and hemorrhage can be increased when Tolmetin is combined with Defibrotide.
Rofecoxib The risk or severity of bleeding and hemorrhage can be increased when Rofecoxib is combined with Defibrotide.
Piroxicam The risk or severity of bleeding and hemorrhage can be increased when Piroxicam is combined with Defibrotide.
Fenoprofen The risk or severity of bleeding and hemorrhage can be increased when Fenoprofen is combined with Defibrotide.
Valdecoxib The risk or severity of bleeding and hemorrhage can be increased when Valdecoxib is combined with Defibrotide.
Diclofenac The risk or severity of bleeding and hemorrhage can be increased when Diclofenac is combined with Defibrotide.
Sulindac The risk or severity of bleeding and hemorrhage can be increased when Sulindac is combined with Defibrotide.
Flurbiprofen The risk or severity of bleeding and hemorrhage can be increased when Flurbiprofen is combined with Defibrotide.
Etodolac The risk or severity of bleeding and hemorrhage can be increased when Etodolac is combined with Defibrotide.
Mefenamic acid The risk or severity of bleeding and hemorrhage can be increased when Mefenamic acid is combined with Defibrotide.
Naproxen The risk or severity of bleeding and hemorrhage can be increased when Naproxen is combined with Defibrotide.
Sulfasalazine The risk or severity of bleeding and hemorrhage can be increased when Sulfasalazine is combined with Defibrotide.
Phenylbutazone The risk or severity of bleeding and hemorrhage can be increased when Phenylbutazone is combined with Defibrotide.
Meloxicam The risk or severity of bleeding and hemorrhage can be increased when Meloxicam is combined with Defibrotide.
Carprofen The risk or severity of bleeding and hemorrhage can be increased when Carprofen is combined with Defibrotide.
Diflunisal The risk or severity of bleeding and hemorrhage can be increased when Diflunisal is combined with Defibrotide.
Salicylic acid The risk or severity of bleeding and hemorrhage can be increased when Salicylic acid is combined with Defibrotide.
Meclofenamic acid The risk or severity of bleeding and hemorrhage can be increased when Meclofenamic acid is combined with Defibrotide.
Oxaprozin The risk or severity of bleeding and hemorrhage can be increased when Oxaprozin is combined with Defibrotide.
Ketoprofen The risk or severity of bleeding and hemorrhage can be increased when Ketoprofen is combined with Defibrotide.
Balsalazide The risk or severity of bleeding and hemorrhage can be increased when Balsalazide is combined with Defibrotide.
Olsalazine The risk or severity of bleeding can be increased when Olsalazine is combined with Defibrotide.
Lumiracoxib The risk or severity of bleeding and hemorrhage can be increased when Lumiracoxib is combined with Defibrotide.
Magnesium salicylate The risk or severity of bleeding and hemorrhage can be increased when Magnesium salicylate is combined with Defibrotide.
Salsalate The risk or severity of bleeding and hemorrhage can be increased when Salsalate is combined with Defibrotide.
Choline magnesium trisalicylate The risk or severity of bleeding and hemorrhage can be increased when Choline magnesium trisalicylate is combined with Defibrotide.
Antrafenine The risk or severity of bleeding and hemorrhage can be increased when Antrafenine is combined with Defibrotide.
Aminophenazone The risk or severity of bleeding and hemorrhage can be increased when Aminophenazone is combined with Defibrotide.
Antipyrine The risk or severity of bleeding and hemorrhage can be increased when Antipyrine is combined with Defibrotide.
Tiaprofenic acid The risk or severity of bleeding and hemorrhage can be increased when Tiaprofenic acid is combined with Defibrotide.
Etoricoxib The risk or severity of bleeding and hemorrhage can be increased when Etoricoxib is combined with Defibrotide.

Target Protein

Adenosine receptor A1 ADORA1
Adenosine receptor A2a ADORA2A
Adenosine receptor A2b ADORA2B

Referensi & Sumber

Artikel (PubMed)
  • PMID: 3754833
    Noseda G, Fragiacomo C, Ferrari D: Pharmacokinetics of defibrotide in healthy volunteers. Haemostasis. 1986;16 Suppl 1:26-30.
  • PMID: 7681375
    Palmer KJ, Goa KL: Defibrotide. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in vascular disorders. Drugs. 1993 Feb;45(2):259-94.
  • PMID: 8511753
    Fisher J, Johnston AM, Holland TK, McCallum J, Pescador R, Mantovani M, Prino G: Pharmacokinetics, absorption, distribution and disposition of 125I-defibrotide following intravenous or oral administration in the rat. Thromb Res. 1993 Apr 1;70(1):77-90.
  • PMID: 17495522
    Koehl GE, Geissler EK, Iacobelli M, Frei C, Burger V, Haffner S, Holler E, Andreesen R, Schlitt HJ, Eissner G: Defibrotide: an endothelium protecting and stabilizing drug, has an anti-angiogenic potential in vitro and in vivo. Cancer Biol Ther. 2007 May;6(5):686-90. Epub 2007 Feb 3.
  • PMID: 16584299
    Kornblum N, Ayyanar K, Benimetskaya L, Richardson P, Iacobelli M, Stein CA: Defibrotide, a polydisperse mixture of single-stranded phosphodiester oligonucleotides with lifesaving activity in severe hepatic veno-occlusive disease: clinical outcomes and potential mechanisms of action. Oligonucleotides. 2006 Spring;16(1):105-14.
  • PMID: 8807733
    Pescador R, Porta R, Ferro L: An integrated view of the activities of defibrotide. Semin Thromb Hemost. 1996;22 Suppl 1:71-5.

Contoh Produk & Brand

Produk: 2 • International brands: 3
Produk
  • Defitelio
    Injection, solution • 80 mg/1mL • Intravenous • US • Approved
  • Defitelio
    Solution • 80 mg / mL • Intravenous • Canada • Approved
International Brands
  • Dasovas
  • Noravid
  • Prociclide

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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