Peringatan Keamanan

The most common adverse reactions reported in at least 3% of patients were pyrexia, abdominal pain, nausea, headache, fatigue, and peripheral edema.L2822,L49941 Hyponatremia was also a rare serious adverse effect of this drug, seen in only 2 patients in the treatment group .L49941 Adverse reactions resulting in discontinuation of this drug have been anemia, pyrexia, and myalgia.L49941

Atrombopag is a thrombopoietin (TPO) receptor agonist, and TPO receptor agonists have been associated with thrombotic and thromboembolic complications in patients with chronic liver disease. Portal venous thrombosis occurrence has been reported in patients with chronic liver disease who are treated with TPO receptor agonists.L49941

Avatrombopag

DB11995

small molecule approved investigational

Deskripsi

Avatrombopag (Doptelet), is an orally administered, small molecule thrombopoietin receptor (c-Mpl) agonist that increases platelet number without increasing platelet activation,A33097,L2824 thereby decreasing the need for blood transfusions.L2824 Patients with thrombocytopenia and chronic liver disease often require platelet transfusions before surgical procedures to decrease the risk of bleeding.A33095 Thrombocytopenia is a common complication in patients suffering from chronic liver disease, occurring as a result of liver disease or a consequence of interferon-based antiviral therapy.F95

Avatrombopag was first approved by the FDA in May 2018 for use in adults with chronic liver disease who are scheduled to undergo a procedure.L2931 It is administered orally as the salt form avatrombopag maleate.L2927 Doptelet (Avatrombopag) is the first orally administered treatment option for patients with chronic liver disease, allowing a large population of patients to avoid a platelet transfusion before a procedure by increasing platelet counts to the optimal level ?50,000 per microliter.L2932

Struktur Molekul 2D

Berat 649.65
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean plasma elimination half-life (%CV) of avatrombopag is approximately 19 hours (19%).[L49941]
Volume Distribusi Avatrombopag has an estimated mean volume of distribution (%CV) of 180 L (25%).[L49941]
Klirens (Clearance) The mean (%CV) of the clearance of avatrombopag is estimated to be 6.9 L/hr (29%).[L49941]

Absorpsi

Following single dosing under fasted and fed conditions, mean peak concentrations occurred at 5-8 hours and declined with a half-life of 16-18 hours in Japanese and white subjects. Administration with food did not have an effect on the rate or extent of avatrombopag absorption, however, significantly reduced pharmacokinetic variability relative to the fasting state.A33097 Avatrombopag showed dose-proportional pharmacokinetics after single doses from 10 mg (0.25-times the lowest approved dosage) to 80 mg (1.3-times the highest recommended dosage). Healthy subjects administered 40 mg of avatrombopag showed a geometric mean (%CV) maximal concentration (Cmax) of 166 (84%) ng/mL and area under the time-concentration curve, extrapolated to infinity (AUC0-inf) of 4198 (83%) ng.hr/mL. The pharmacokinetics of avatrombopag are similar in both healthy subjects and the chronic liver disease population.L49941

Metabolisme

Avatrombopag is primarily metabolized by CYP2C9 and CYP3A4.L49941

Rute Eliminasi

Fecal excretion accounted for 88% of the administered dose, with 34% of the dose excreted as unchanged avatrombopag. Only 6% of the administered dose was found in urine.L49941

Interaksi Makanan

1 Data
  • 1. Take with food.

Interaksi Obat

392 Data
Phenytoin The metabolism of Avatrombopag can be increased when combined with Phenytoin.
Pentobarbital The metabolism of Avatrombopag can be increased when combined with Pentobarbital.
Carbamazepine The metabolism of Avatrombopag can be increased when combined with Carbamazepine.
Mitotane The metabolism of Avatrombopag can be increased when combined with Mitotane.
Primidone The metabolism of Avatrombopag can be increased when combined with Primidone.
Rifampin The metabolism of Avatrombopag can be increased when combined with Rifampicin.
Phenobarbital The metabolism of Avatrombopag can be increased when combined with Phenobarbital.
Rifapentine The metabolism of Avatrombopag can be increased when combined with Rifapentine.
Dexamethasone The metabolism of Avatrombopag can be increased when combined with Dexamethasone.
Fosphenytoin The metabolism of Avatrombopag can be increased when combined with Fosphenytoin.
St. John's Wort The metabolism of Avatrombopag can be increased when combined with St. John's Wort.
Midostaurin The metabolism of Avatrombopag can be decreased when combined with Midostaurin.
Enzalutamide The serum concentration of Avatrombopag can be decreased when it is combined with Enzalutamide.
Lumacaftor The metabolism of Avatrombopag can be increased when combined with Lumacaftor.
Apalutamide The serum concentration of Avatrombopag can be decreased when it is combined with Apalutamide.
Cyclosporine The metabolism of Avatrombopag can be decreased when combined with Cyclosporine.
Fluvoxamine The metabolism of Avatrombopag can be decreased when combined with Fluvoxamine.
Fluconazole The metabolism of Avatrombopag can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Avatrombopag can be increased when it is combined with Erythromycin.
Ziprasidone The metabolism of Avatrombopag can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Avatrombopag can be decreased when combined with Isradipine.
Diltiazem The metabolism of Avatrombopag can be decreased when combined with Diltiazem.
Clozapine The metabolism of Avatrombopag can be decreased when combined with Clozapine.
Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Avatrombopag.
Ciprofloxacin The metabolism of Avatrombopag can be decreased when combined with Ciprofloxacin.
Voriconazole The metabolism of Avatrombopag can be decreased when combined with Voriconazole.
Nicardipine The metabolism of Avatrombopag can be decreased when combined with Nicardipine.
Verapamil The metabolism of Avatrombopag can be decreased when combined with Verapamil.
Aprepitant The metabolism of Avatrombopag can be decreased when combined with Aprepitant.
Isoniazid The metabolism of Avatrombopag can be decreased when combined with Isoniazid.
Primaquine The metabolism of Avatrombopag can be decreased when combined with Primaquine.
Miconazole The metabolism of Avatrombopag can be decreased when combined with Miconazole.
Danazol The metabolism of Avatrombopag can be decreased when combined with Danazol.
Fusidic acid The metabolism of Avatrombopag can be decreased when combined with Fusidic acid.
Zimelidine The metabolism of Avatrombopag can be decreased when combined with Zimelidine.
Dronedarone The metabolism of Avatrombopag can be decreased when combined with Dronedarone.
Milnacipran The metabolism of Avatrombopag can be decreased when combined with Milnacipran.
Simeprevir The metabolism of Avatrombopag can be decreased when combined with Simeprevir.
Isavuconazonium The metabolism of Avatrombopag can be decreased when combined with Isavuconazonium.
Desvenlafaxine The metabolism of Avatrombopag can be decreased when combined with Desvenlafaxine.
Nilvadipine The metabolism of Avatrombopag can be decreased when combined with Nilvadipine.
Seproxetine The metabolism of Avatrombopag can be decreased when combined with Seproxetine.
Linagliptin The metabolism of Avatrombopag can be decreased when combined with Linagliptin.
Indalpine The metabolism of Avatrombopag can be decreased when combined with Indalpine.
Netupitant The metabolism of Avatrombopag can be decreased when combined with Netupitant.
Barnidipine The metabolism of Avatrombopag can be decreased when combined with Barnidipine.
Benidipine The metabolism of Avatrombopag can be decreased when combined with Benidipine.
Venetoclax The metabolism of Avatrombopag can be decreased when combined with Venetoclax.
Isavuconazole The metabolism of Avatrombopag can be decreased when combined with Isavuconazole.
Fosnetupitant The metabolism of Avatrombopag can be decreased when combined with Fosnetupitant.
Berotralstat The metabolism of Avatrombopag can be decreased when combined with Berotralstat.
Nelfinavir The metabolism of Avatrombopag can be decreased when combined with Nelfinavir.
Indinavir The metabolism of Avatrombopag can be decreased when combined with Indinavir.
Terfenadine The metabolism of Avatrombopag can be decreased when combined with Terfenadine.
Ritonavir The serum concentration of Avatrombopag can be increased when it is combined with Ritonavir.
Efavirenz The metabolism of Avatrombopag can be decreased when combined with Efavirenz.
Ergotamine The metabolism of Avatrombopag can be decreased when combined with Ergotamine.
Amprenavir The metabolism of Avatrombopag can be decreased when combined with Amprenavir.
Delavirdine The metabolism of Avatrombopag can be decreased when combined with Delavirdine.
Methimazole The metabolism of Avatrombopag can be decreased when combined with Methimazole.
Conivaptan The metabolism of Avatrombopag can be decreased when combined with Conivaptan.
Tipranavir The metabolism of Avatrombopag can be decreased when combined with Tipranavir.
Telithromycin The metabolism of Avatrombopag can be decreased when combined with Telithromycin.
Ketoconazole The metabolism of Avatrombopag can be decreased when combined with Ketoconazole.
Atazanavir The metabolism of Avatrombopag can be decreased when combined with Atazanavir.
Amiodarone The metabolism of Avatrombopag can be decreased when combined with Amiodarone.
Nefazodone The metabolism of Avatrombopag can be decreased when combined with Nefazodone.
Itraconazole The metabolism of Avatrombopag can be decreased when combined with Itraconazole.
Clarithromycin The metabolism of Avatrombopag can be decreased when combined with Clarithromycin.
Saquinavir The metabolism of Avatrombopag can be decreased when combined with Saquinavir.
Posaconazole The metabolism of Avatrombopag can be decreased when combined with Posaconazole.
Darunavir The metabolism of Avatrombopag can be decreased when combined with Darunavir.
Lopinavir The metabolism of Avatrombopag can be decreased when combined with Lopinavir.
Ditiocarb The metabolism of Avatrombopag can be decreased when combined with Ditiocarb.
Nilotinib The metabolism of Avatrombopag can be decreased when combined with Nilotinib.
Telaprevir The metabolism of Avatrombopag can be decreased when combined with Telaprevir.
Levoketoconazole The metabolism of Avatrombopag can be decreased when combined with Levoketoconazole.
Lonafarnib The metabolism of Avatrombopag can be decreased when combined with Lonafarnib.
Boceprevir The metabolism of Avatrombopag can be decreased when combined with Boceprevir.
Elvitegravir The metabolism of Avatrombopag can be decreased when combined with Elvitegravir.
Stiripentol The metabolism of Avatrombopag can be decreased when combined with Stiripentol.
Curcumin The metabolism of Avatrombopag can be decreased when combined with Curcumin.
Ribociclib The metabolism of Avatrombopag can be decreased when combined with Ribociclib.
Danoprevir The metabolism of Avatrombopag can be decreased when combined with Danoprevir.
Troleandomycin The metabolism of Avatrombopag can be decreased when combined with Troleandomycin.
Troglitazone The metabolism of Avatrombopag can be decreased when combined with Troglitazone.
Valproic acid The metabolism of Avatrombopag can be decreased when combined with Valproic acid.
Fluoxetine The metabolism of Avatrombopag can be decreased when combined with Fluoxetine.
Imatinib The metabolism of Avatrombopag can be decreased when combined with Imatinib.
Mifepristone The metabolism of Avatrombopag can be decreased when combined with Mifepristone.
Quinidine The metabolism of Avatrombopag can be decreased when combined with Quinidine.
Felbamate The metabolism of Avatrombopag can be decreased when combined with Felbamate.
Sulfinpyrazone The metabolism of Avatrombopag can be decreased when combined with Sulfinpyrazone.
Iproniazid The metabolism of Avatrombopag can be decreased when combined with Iproniazid.
Medical Cannabis The metabolism of Avatrombopag can be decreased when combined with Medical Cannabis.
Dabrafenib The serum concentration of Avatrombopag can be decreased when it is combined with Dabrafenib.
Floxuridine The metabolism of Avatrombopag can be decreased when combined with Floxuridine.
Capecitabine The serum concentration of Avatrombopag can be increased when it is combined with Capecitabine.
Gemfibrozil The metabolism of Avatrombopag can be decreased when combined with Gemfibrozil.
Sulfaphenazole The metabolism of Avatrombopag can be decreased when combined with Sulfaphenazole.

Target Protein

Thrombopoietin receptor MPL

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29778606
    Terrault N, Chen YC, Izumi N, Kayali Z, Mitrut P, Tak WY, Allen LF, Hassanein T: Avatrombopag Before Procedures Reduces Need for Platelet Transfusion in Patients With Chronic Liver Disease and Thrombocytopenia. Gastroenterology. 2018 May 17. pii: S0016-5085(18)34545-1. doi: 10.1053/j.gastro.2018.05.025.
  • PMID: 27800187
    Qureshi K, Patel S, Meillier A: The Use of Thrombopoietin Receptor Agonists for Correction of Thrombocytopenia prior to Elective Procedures in Chronic Liver Diseases: Review of Current Evidence. Int J Hepatol. 2016;2016:1802932. doi: 10.1155/2016/1802932. Epub 2016 Oct 9.
  • PMID: 28339166
    Nomoto M, Pastino G, Rege B, Aluri J, Ferry J, Han D: Pharmacokinetics, Pharmacodynamics, Pharmacogenomics, Safety, and Tolerability of Avatrombopag in Healthy Japanese and White Subjects. Clin Pharmacol Drug Dev. 2018 Feb;7(2):188-195. doi: 10.1002/cpdd.349. Epub 2017 Mar 24.
  • PMID: 27403440
    Yun SH, Sim EH, Goh RY, Park JI, Han JY: Platelet Activation: The Mechanisms and Potential Biomarkers. Biomed Res Int. 2016;2016:9060143. doi: 10.1155/2016/9060143. Epub 2016 Jun 15.
  • PMID: 24802775
    Bussel JB, Kuter DJ, Aledort LM, Kessler CM, Cuker A, Pendergrass KB, Tang S, McIntosh J: A randomized trial of avatrombopag, an investigational thrombopoietin-receptor agonist, in persistent and chronic immune thrombocytopenia. Blood. 2014 Jun 19;123(25):3887-94. doi: 10.1182/blood-2013-07-514398. Epub 2014 May 6.

Contoh Produk & Brand

Produk: 5 • International brands: 0
Produk
  • Doptelet
    Tablet, film coated • 20 mg • Oral • EU • Approved
  • Doptelet
    Tablet, film coated • 20 mg • Oral • EU • Approved
  • Doptelet
    Tablet, film coated • 20 mg • Oral • EU • Approved
  • Doptelet
    Tablet, film coated • 20 mg/1 • Oral • US • Approved
  • Doptelet
    Tablet • 20 mg • Oral • Canada • Approved

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