Peringatan Keamanan

Data regarding fedratinib in overdose is not readily available.L8090 Patients given 680mg/day experienced a greater incidence and severity of adverse effects including anemia, thrombocytopenia, gastrointestinal toxicity, hepatic toxicity, and elevated amylase and lipase.A183185 These effects were treated symptomatically as well as by reducing the dose or temporarily stopping fedratinib.A183185,L8090

Fedratinib

DB12500

small molecule approved investigational

Deskripsi

Fedratinib, also known as SAR302503 and TG101348, is a tyrosine kinase inhibitor used to treat intermediate-2 and high risk primary and secondary myelofibrosis.A183176,L8090 It is an anilinopyrimidine derivative.A183188

Fedratinib was granted FDA approval on August 16, 2019.L8090

Struktur Molekul 2D

Berat 524.678
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of fedratinib is 41 hours with a terminal half life of 114 hours.[L8090]
Volume Distribusi The apparent volume of distribution is 1770L.[L8090]
Klirens (Clearance) The clearance of fedratinib is 13L/h.[L8090]

Absorpsi

A 400mg oral dose results in a Cmax of 1804ng/mL and an AUC of 26,870ng/*hr/mL.L8090 Fedratinib has a Tmax of 1.75-3 hours.A183182,L8090 A high fat breakfast does not significantly affect the absorption of fedratinib.A183179

Metabolisme

Fedratinib is metabolized by CYP3A4, CYP2C19, and flavin-containing monooxygenase 3.L8090 Beyond that, data regarding the metabolism of fedratinib is not readily available.

Rute Eliminasi

An oral dose of fedratinib is 77% eliminated in the feces with 23% as unchanged drug.L8090 5% is eliminated in the urine, with 3% as unchanged drug.L8090

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of fedratinib. Dose reduction may be necessary.
  • 2. Avoid St. John's Wort. This herb induces the CYP3A metabolism of fedratinib and may reduce its serum concentration.
  • 3. Take with or without food. Food may help reduce adverse effects of fedratinib such as nausea and vomiting.

Interaksi Obat

1245 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Fedratinib.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Fedratinib.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Fedratinib.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Fedratinib.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Fedratinib.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Fedratinib.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Fedratinib.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Fedratinib.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Fedratinib.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Fedratinib.
Silodosin The excretion of Silodosin can be decreased when combined with Fedratinib.
Topotecan Fedratinib may decrease the excretion rate of Topotecan which could result in a higher serum level.
Dabrafenib The serum concentration of Fedratinib can be decreased when it is combined with Dabrafenib.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Fedratinib.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Fedratinib.
Luliconazole The serum concentration of Fedratinib can be increased when it is combined with Luliconazole.
Acetaminophen The serum concentration of Acetaminophen can be increased when it is combined with Fedratinib.
Propacetamol The serum concentration of Propacetamol can be increased when it is combined with Fedratinib.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Fedratinib.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Fedratinib.
Vincristine The serum concentration of Vincristine can be increased when it is combined with Fedratinib.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Fedratinib.
Lumacaftor The serum concentration of Fedratinib can be decreased when it is combined with Lumacaftor.
Fluvoxamine The serum concentration of Fluvoxamine can be increased when it is combined with Fedratinib.
Isoniazid The metabolism of Fedratinib can be decreased when combined with Isoniazid.
Miconazole The metabolism of Fedratinib can be decreased when combined with Miconazole.
Ticlopidine The serum concentration of Ticlopidine can be increased when it is combined with Fedratinib.
Chloramphenicol The metabolism of Fedratinib can be decreased when combined with Chloramphenicol.
Lansoprazole The serum concentration of Lansoprazole can be increased when it is combined with Fedratinib.
Fluoxetine The serum concentration of Fluoxetine can be increased when it is combined with Fedratinib.
Zafirlukast The metabolism of Fedratinib can be decreased when combined with Zafirlukast.
Gemfibrozil The serum concentration of Gemfibrozil can be increased when it is combined with Fedratinib.
Eslicarbazepine acetate The metabolism of Fedratinib can be decreased when combined with Eslicarbazepine acetate.
Betrixaban The serum concentration of Betrixaban can be increased when it is combined with Fedratinib.
Vemurafenib The serum concentration of Fedratinib can be increased when it is combined with Vemurafenib.
Apalutamide The serum concentration of Fedratinib can be decreased when it is combined with Apalutamide.
Pitolisant The serum concentration of Fedratinib can be decreased when it is combined with Pitolisant.
Isavuconazole The serum concentration of Isavuconazole can be increased when it is combined with Fedratinib.
Isavuconazonium The serum concentration of Isavuconazonium can be increased when it is combined with Fedratinib.
Folic acid Fedratinib may decrease the excretion rate of Folic acid which could result in a higher serum level.
Pravastatin Fedratinib may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Conjugated estrogens The serum concentration of Conjugated estrogens can be increased when it is combined with Fedratinib.
Gefitinib The serum concentration of Gefitinib can be increased when it is combined with Fedratinib.
Sorafenib The serum concentration of Sorafenib can be increased when it is combined with Fedratinib.
Allopurinol Fedratinib may decrease the excretion rate of Allopurinol which could result in a higher serum level.
Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Fedratinib.
Teniposide The serum concentration of Teniposide can be increased when it is combined with Fedratinib.
Prazosin Fedratinib may decrease the excretion rate of Prazosin which could result in a higher serum level.
Raloxifene Fedratinib may decrease the excretion rate of Raloxifene which could result in a higher serum level.
Celecoxib The serum concentration of Celecoxib can be increased when it is combined with Fedratinib.
Zidovudine The serum concentration of Zidovudine can be increased when it is combined with Fedratinib.
Oxaliplatin Fedratinib may decrease the excretion rate of Oxaliplatin which could result in a higher serum level.
Fluorouracil Fedratinib may decrease the excretion rate of Fluorouracil which could result in a higher serum level.
Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Fedratinib.
Ivermectin The serum concentration of Ivermectin can be increased when it is combined with Fedratinib.
Imatinib The serum concentration of Imatinib can be increased when it is combined with Fedratinib.
Testosterone The serum concentration of Testosterone can be increased when it is combined with Fedratinib.
Clofarabine Fedratinib may decrease the excretion rate of Clofarabine which could result in a higher serum level.
Sumatriptan Fedratinib may decrease the excretion rate of Sumatriptan which could result in a higher serum level.
Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be increased when it is combined with Fedratinib.
Daunorubicin Fedratinib may decrease the excretion rate of Daunorubicin which could result in a higher serum level.
Nitrofurantoin Fedratinib may decrease the excretion rate of Nitrofurantoin which could result in a higher serum level.
Lamivudine Fedratinib may decrease the excretion rate of Lamivudine which could result in a higher serum level.
Riluzole Fedratinib may decrease the excretion rate of Riluzole which could result in a higher serum level.
Irinotecan The serum concentration of Irinotecan can be increased when it is combined with Fedratinib.
Sulfasalazine Fedratinib may decrease the excretion rate of Sulfasalazine which could result in a higher serum level.
Donepezil The serum concentration of Donepezil can be increased when it is combined with Fedratinib.
Ezetimibe Fedratinib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Glyburide The serum concentration of Glyburide can be increased when it is combined with Fedratinib.
Tegaserod The serum concentration of Tegaserod can be increased when it is combined with Fedratinib.
Leflunomide Fedratinib may decrease the excretion rate of Leflunomide which could result in a higher serum level.
Rosuvastatin The serum concentration of Rosuvastatin can be increased when it is combined with Fedratinib.
Mitoxantrone Fedratinib may decrease the excretion rate of Mitoxantrone which could result in a higher serum level.
Alvocidib Fedratinib may decrease the excretion rate of Alvocidib which could result in a higher serum level.
Camptothecin Fedratinib may decrease the excretion rate of Camptothecin which could result in a higher serum level.
Apixaban The serum concentration of Apixaban can be increased when it is combined with Fedratinib.
Teriflunomide Fedratinib may decrease the excretion rate of Teriflunomide which could result in a higher serum level.
Dolutegravir Fedratinib may decrease the excretion rate of Dolutegravir which could result in a higher serum level.
Riociguat The serum concentration of Riociguat can be increased when it is combined with Fedratinib.
Sofosbuvir Fedratinib may decrease the excretion rate of Sofosbuvir which could result in a higher serum level.
Palbociclib The serum concentration of Palbociclib can be increased when it is combined with Fedratinib.
Lenvatinib Fedratinib may decrease the excretion rate of Lenvatinib which could result in a higher serum level.
Fimasartan Fedratinib may decrease the excretion rate of Fimasartan which could result in a higher serum level.
Ombitasvir Fedratinib may decrease the excretion rate of Ombitasvir which could result in a higher serum level.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Fedratinib.
Velpatasvir The serum concentration of Velpatasvir can be increased when it is combined with Fedratinib.
Delafloxacin Fedratinib may decrease the excretion rate of Delafloxacin which could result in a higher serum level.
Duvelisib The serum concentration of Duvelisib can be increased when it is combined with Fedratinib.
Glasdegib The serum concentration of Glasdegib can be increased when it is combined with Fedratinib.
Voxilaprevir The serum concentration of Voxilaprevir can be increased when it is combined with Fedratinib.
Brigatinib The serum concentration of Brigatinib can be increased when it is combined with Fedratinib.
Rucaparib The serum concentration of Rucaparib can be increased when it is combined with Fedratinib.
Lusutrombopag Fedratinib may decrease the excretion rate of Lusutrombopag which could result in a higher serum level.
Pibrentasvir Fedratinib may decrease the excretion rate of Pibrentasvir which could result in a higher serum level.
Glecaprevir Fedratinib may decrease the excretion rate of Glecaprevir which could result in a higher serum level.
Testosterone cypionate The serum concentration of Testosterone cypionate can be increased when it is combined with Fedratinib.
Testosterone enanthate The serum concentration of Testosterone enanthate can be increased when it is combined with Fedratinib.
Darolutamide The serum concentration of Darolutamide can be increased when it is combined with Fedratinib.
Tazemetostat The serum concentration of Tazemetostat can be increased when it is combined with Fedratinib.
Selumetinib The serum concentration of Selumetinib can be increased when it is combined with Fedratinib.

Target Protein

Tyrosine-protein kinase JAK2 JAK2
Receptor-type tyrosine-protein kinase FLT3 FLT3
Tyrosine-protein kinase JAK1 JAK1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 26181658
    Pardanani A, Harrison C, Cortes JE, Cervantes F, Mesa RA, Milligan D, Masszi T, Mishchenko E, Jourdan E, Vannucchi AM, Drummond MW, Jurgutis M, Kuliczkowski K, Gheorghita E, Passamonti F, Neumann F, Patki A, Gao G, Tefferi A: Safety and Efficacy of Fedratinib in Patients With Primary or Secondary Myelofibrosis: A Randomized Clinical Trial. JAMA Oncol. 2015 Aug;1(5):643-51. doi: 10.1001/jamaoncol.2015.1590.
  • PMID: 26357842
    Jamieson C, Hasserjian R, Gotlib J, Cortes J, Stone R, Talpaz M, Thiele J, Rodig S, Pozdnyakova O: Effect of treatment with a JAK2-selective inhibitor, fedratinib, on bone marrow fibrosis in patients with myelofibrosis. J Transl Med. 2015 Sep 10;13:294. doi: 10.1186/s12967-015-0644-4.
  • PMID: 27136912
    Zhang M, Xu C, Ma L, Shamiyeh E, Yin J, von Moltke LL, Smith WB: Effect of food on the bioavailability and tolerability of the JAK2-selective inhibitor fedratinib (SAR302503): Results from two phase I studies in healthy volunteers. Clin Pharmacol Drug Dev. 2015 Jul;4(4):315-21. doi: 10.1002/cpdd.161. Epub 2014 Oct 27.
  • PMID: 24165976
    Zhang M, Xu CR, Shamiyeh E, Liu F, Yin JY, von Moltke LL, Smith WB: A randomized, placebo-controlled study of the pharmacokinetics, pharmacodynamics, and tolerability of the oral JAK2 inhibitor fedratinib (SAR302503) in healthy volunteers. J Clin Pharmacol. 2014 Apr;54(4):415-21. doi: 10.1002/jcph.218. Epub 2013 Nov 16.
  • PMID: 21220608
    Pardanani A, Gotlib JR, Jamieson C, Cortes JE, Talpaz M, Stone RM, Silverman MH, Gilliland DG, Shorr J, Tefferi A: Safety and efficacy of TG101348, a selective JAK2 inhibitor, in myelofibrosis. J Clin Oncol. 2011 Mar 1;29(7):789-96. doi: 10.1200/JCO.2010.32.8021. Epub 2011 Jan 10.
  • PMID: 27473820
    Roskoski R Jr: Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases. Pharmacol Res. 2016 Sep;111:784-803. doi: 10.1016/j.phrs.2016.07.038. Epub 2016 Jul 26.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Inrebic
    Capsule • 100 mg/1 • Oral • US • Approved
  • Inrebic
    Capsule • 100 mg • Oral • EU • Approved
  • Inrebic
    Capsule • 100 mg • Oral • Canada • Approved

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