Peringatan Keamanan

Eltrombopag may cause hepatotoxicity, especially if administered in combination with interferon and ribavirin in patients with chronic hepatitis C (may increase the risk of hepatic decompensation).

Eltrombopag

DB06210

small molecule approved

Deskripsi

Eltrombopag is used to treat low blood platelet counts in adults with chronic immune (idiopathic) thrombocytopenia (ITP), when certain other medicines, or surgery to remove the spleen, have not worked well enough. ITP is a condition that may cause unusual bruising or bleeding due to an abnormally low number of platelets in the blood. Eltrombopag has also been recently approved (late 2012) for the treatment of thrombocytopenia (low blood platelet counts) in patients with chronic hepatitis C to allow them to initiate and maintain interferon-based therapy.

Struktur Molekul 2D

Berat 442.4666
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) About 21-32 hours in healthy patients. About 26-35 hours in patients with idiopathic thrombocytopenic purpura.
Volume Distribusi Based on a radiolabel study, the concentration of eltrombopag in blood cells is approximately 50% to 79% of plasma concentrations.
Klirens (Clearance) -

Absorpsi

Peak absorption of Eltrombopag occurs around 2-6 hours following oral administration, and the total oral absorption of drug-related material following a 75 mg dose was estimated to be at least 52%.

Metabolisme

Eltrombopag is predominantly through pathways including cleavage, oxidation, and conjugation with glucuronic acid, glutathione, or cysteine. In vitro studies suggest that CYP1A2 and CYP2C8 are responsible for the oxidative metabolism of eltrombopag. UGT1A1 and UGT1A3 are responsible for the glucuronidation of eltrombopag.

Rute Eliminasi

Eltrombopag is eliminated primarily via the feces (59%), along with 31% being renally excreted.

Farmakogenomik

2 Varian
F5 (rs6025)

Patients who carry this polymorphism in F5 are associated with an increased risk of thromboembolism when treated with eltrombopag.

SERPINC1 (rs121909567)

Patients who carry this polymorphism in SERPINC1 are associated with antithrombin III deficiency and an increased risk of thromboembolism when treated with eltrombopag.

Interaksi Makanan

2 Data
  • 1. Avoid multivalent ions. Polyvalent cations in food or supplements will be chelated by eltrombopag; therefore, they should be separated by 4 hours before or 2 hours after taking eltrombopag.
  • 2. Take on an empty stomach. Separate the administration of eltrombopag from food by at least 1 hour before and 2 hours after eating.

Interaksi Obat

748 Data
Deferasirox The serum concentration of Eltrombopag can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Eltrombopag can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Eltrombopag can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Eltrombopag can be decreased when it is combined with Teriflunomide.
Irinotecan The risk or severity of neutropenia can be increased when Eltrombopag is combined with Irinotecan.
Calcium acetate The serum concentration of Eltrombopag can be decreased when it is combined with Calcium acetate.
Calcium glucoheptonate The serum concentration of Eltrombopag can be decreased when it is combined with Calcium glucoheptonate.
Calcium chloride The serum concentration of Eltrombopag can be decreased when it is combined with Calcium chloride.
Calcium The serum concentration of Eltrombopag can be decreased when it is combined with Calcium.
Calcium carbonate The serum concentration of Eltrombopag can be decreased when it is combined with Calcium carbonate.
Calcium citrate The serum concentration of Eltrombopag can be decreased when it is combined with Calcium citrate.
Calcium gluconate The serum concentration of Eltrombopag can be decreased when it is combined with Calcium gluconate.
Calcium Phosphate The serum concentration of Eltrombopag can be decreased when it is combined with Calcium Phosphate.
Calcium lactate The serum concentration of Eltrombopag can be decreased when it is combined with Calcium lactate.
Calcium lactate gluconate The serum concentration of Eltrombopag can be decreased when it is combined with Calcium lactate gluconate.
Calcium pangamate The serum concentration of Eltrombopag can be decreased when it is combined with Calcium pangamate.
Calcium polycarbophil The serum concentration of Eltrombopag can be decreased when it is combined with Calcium polycarbophil.
Deferiprone The serum concentration of Deferiprone can be increased when it is combined with Eltrombopag.
Mifepristone The serum concentration of Eltrombopag can be increased when it is combined with Mifepristone.
Sucralfate Sucralfate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bentoquatam Bentoquatam can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium sulfate Magnesium sulfate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium Aluminium can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium oxide Magnesium oxide can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium salicylate Magnesium salicylate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Kaolin Kaolin can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc Zinc can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc trihydroxide Zinc trihydroxide can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc Substituted Heme C Zinc Substituted Heme C can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum hydroxide Aluminum hydroxide can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magaldrate Magaldrate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Potassium alum Potassium alum can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium hydroxide Magnesium hydroxide can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Polaprezinc Polaprezinc can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium trisilicate Magnesium trisilicate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc oxide Zinc oxide can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc sulfate Zinc sulfate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium chloride Magnesium chloride can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium carbonate Magnesium carbonate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Talc Talc can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum chloride Aluminum chloride can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium citrate Magnesium citrate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc citrate Zinc citrate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc picolinate Zinc picolinate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum sulfate Aluminum sulfate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc gluconate Zinc gluconate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bentonite Bentonite can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium silicate Magnesium silicate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium acetoacetate Aluminium acetoacetate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Hydrotalcite Hydrotalcite can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium aspartate Magnesium aspartate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium peroxide Magnesium peroxide can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium glycinate Aluminium glycinate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aloglutamol Aloglutamol can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Montmorillonite Montmorillonite can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium gluconate Magnesium gluconate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium orotate Magnesium orotate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetylcysteine zinc Acetylcysteine zinc can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc ascorbate Zinc ascorbate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc acetate Zinc acetate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc glycinate Zinc glycinate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium Magnesium can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium levulinate Magnesium levulinate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium lactate Magnesium lactate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium phosphate Aluminium phosphate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc chloride Zinc chloride can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc sulfate, unspecified form Zinc sulfate, unspecified form can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zinc cation Zinc cation can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum oxide Aluminum oxide can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Nelfinavir The metabolism of Eltrombopag can be increased when combined with Nelfinavir.
Desogestrel The metabolism of Eltrombopag can be increased when combined with Desogestrel.
Zidovudine The metabolism of Eltrombopag can be increased when combined with Zidovudine.
Lamotrigine The metabolism of Eltrombopag can be increased when combined with Lamotrigine.
Efavirenz The metabolism of Eltrombopag can be increased when combined with Efavirenz.
Tipranavir The metabolism of Eltrombopag can be increased when combined with Tipranavir.
Ethinylestradiol The metabolism of Eltrombopag can be increased when combined with Ethinylestradiol.
Testosterone propionate The metabolism of Eltrombopag can be increased when combined with Testosterone propionate.
Rosuvastatin The serum concentration of Rosuvastatin can be increased when it is combined with Eltrombopag.
Iron Dextran Iron Dextran can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron Iron can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Prussian blue Prussian blue can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron sucrose Iron sucrose can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric pyrophosphate Ferric pyrophosphate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric ammonium citrate Ferric ammonium citrate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferumoxsil Ferumoxsil can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferumoxides Ferumoxides can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric sulfate Ferric sulfate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous bisglycinate Ferrous bisglycinate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Gleptoferron Gleptoferron can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric oxide Ferric oxide can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Perflubutane Perflubutane can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous sulfate anhydrous Ferrous sulfate anhydrous can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sodium feredetate Sodium feredetate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric hydroxide Ferric hydroxide can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric cation Ferric cation can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous gluconate Ferrous gluconate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous succinate Ferrous succinate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferrous fumarate Ferrous fumarate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tetraferric tricitrate decahydrate Tetraferric tricitrate decahydrate can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric oxyhydroxide Ferric oxyhydroxide can cause a decrease in the absorption of Eltrombopag resulting in a reduced serum concentration and potentially a decrease in efficacy.

Target Protein

Thrombopoietin receptor MPL

Referensi & Sumber

Synthesis reference: http://doc.sciencenet.cn/upload/file/2011531154034454.pdf
Artikel (PubMed)
  • PMID: 18366111
    Zekry A, Freiman J: Eltrombopag: Is this "24 karat gold platelet" treatment for thrombocytopenia in cirrhosis associated with hepatitis C? Hepatology. 2008 Apr;47(4):1418-21. doi: 10.1002/hep.22300.
  • PMID: 18433923
    Mondelli MU: Eltrombopag: an effective remedy for thrombocytopaenia? J Hepatol. 2008 Jun;48(6):1030-2. doi: 10.1016/j.jhep.2008.03.008. Epub 2008 Mar 31.
  • PMID: 23492914
    Tarantino MD, Fogarty P, Mayer B, Vasey SY, Brainsky A: Efficacy of eltrombopag in management of bleeding symptoms associated with chronic immune thrombocytopenia. Blood Coagul Fibrinolysis. 2013 Apr;24(3):284-96. doi: 10.1097/MBC.0b013e32835fac99.
  • PMID: 15781124
    Kiang TK, Ensom MH, Chang TK: UDP-glucuronosyltransferases and clinical drug-drug interactions. Pharmacol Ther. 2005 Apr;106(1):97-132. Epub 2005 Jan 12.
  • PMID: 21646437
    Deng Y, Madatian A, Wire MB, Bowen C, Park JW, Williams D, Peng B, Schubert E, Gorycki F, Levy M, Gorycki PD: Metabolism and disposition of eltrombopag, an oral, nonpeptide thrombopoietin receptor agonist, in healthy human subjects. Drug Metab Dispos. 2011 Sep;39(9):1734-46. doi: 10.1124/dmd.111.040170. Epub 2011 Jun 6.
  • PMID: 23821332
    Kuter DJ: The biology of thrombopoietin and thrombopoietin receptor agonists. Int J Hematol. 2013 Jul;98(1):10-23. doi: 10.1007/s12185-013-1382-0. Epub 2013 Jul 3.
Attachment

Contoh Produk & Brand

Produk: 38 • International brands: 2
Produk
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  • Alvaiz
    Tablet, film coated • 54 mg/1 • Oral • US • Approved
  • Apo-eltrombopag
    Tablet • 25 mg • Oral • Canada • Generic • Approved
  • Apo-eltrombopag
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Promacta
    Tablet, film coated • 25 mg/1 • Oral • US • Approved
  • Promacta
    Tablet, film coated • 50 mg/1 • Oral • US • Approved
Menampilkan 8 dari 38 produk.
International Brands
  • Promacta
  • Revolade

Sekuens Gen/Protein (FASTA)

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