Peringatan Keamanan

The oral lowest published toxic dose (Toxic Dose Low, TDLo) is 2.84 mg/kg/21D (intermittent).L44582 The oral LD50 of sorafenib tosylate in rats is >2000 mg/kg.L44607

The adverse reactions observed at 800 mg sorafenib twice daily (twice the recommended dose) were primarily diarrhea and dermatologic. No information is available on symptoms of acute overdose in animals because of the saturation of absorption in oral acute toxicity studies conducted in animals. The prescribing information recommends the discontinuation of sorafenib treatment and initiation of supportive care in cases of suspected overdose.L9341

Sorafenib

DB00398

small molecule approved investigational

Deskripsi

Sorafenib is a bi-aryl urea and an oral multikinase inhibitor. It targets cell surface tyrosine kinase receptors and downstream intracellular kinases that are implicated in tumour cell proliferation and tumour angiogenesis.A255852 First approved by the FDA and European Commission in 2007 for the treatment of hepatocellular carcinoma, sorafenib is also indicated to treat renal carcinoma and differentiated thyroid carcinoma.A14794

Struktur Molekul 2D

Berat 464.825
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 elimination half-life of sorafenib was approximately 25 to 48 hours.[L9341]
Volume Distribusi Sorafenib is widely distributed to tissues, indicating that it is lipophilic.[A255852]
Klirens (Clearance) -

Absorpsi

The administration of multiple doses for seven days resulted in a 2.5- to 7-fold accumulation compared to a single dose. Steady-state concentrations were achieved within seven days, with a peak-to-trough ratio of mean concentrations of less than 2. Mean Cmax and AUC increased less than proportionally beyond oral doses of 400 mg administered twice daily. The Tmax is approximately three hours.L9341 The mean relative bioavailability was 38–49% following the administration of oral sorafenib tablets. A high-fat meal reduced bioavailability by 29%.L9341

Metabolisme

Sorafenib undergoes oxidative metabolism by CYP3A4 in the liver, as well as glucuronidation by UGT1A9 in the liver and kidneys.A255852,L9341 At steady-state, sorafenib accounts for 70-85% of the circulating analytes in plasma.A255852 About eight metabolites of sorafenib have been identified, of which five were detected in plasma. The main circulating metabolite was the pyridine N-oxide form, which comprises approximately 9–16% of the total circulating dose at steady-state: the pharmacological activity of this metabolite was comparable to the parent drug.L9341

Rute Eliminasi

Following oral administration of a 100 mg dose of sorafenib, about 96% of the dose was recovered within 14 days, with 77% of the dose being excreted in feces and 19% of the dose being excreted in urine as glucuronidated metabolites. Unchanged sorafenib accounted for 51% of the dose excreted in feces.L9341

Interaksi Makanan

4 Data
  • 1. Do not take with or immediately after a high-fat meal. Take sorafenib at least 1 hour before or 2 hours after a high-fat meal, as sorafenib absorption can be reduced by a high-fat meal.
  • 2. Exercise caution with grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum levels of sorafenib.
  • 3. Exercise caution with St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce serum levels of sorafenib.
  • 4. Take on an empty stomach. Take sorafenib at least one hour before or two hours after a meal.

Interaksi Obat

1944 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Sorafenib.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Sorafenib.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Sorafenib.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Sorafenib.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Sorafenib.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Sorafenib.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Sorafenib.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Sorafenib.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Sorafenib.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Sorafenib.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Sorafenib.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Sorafenib.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Sorafenib.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Sorafenib.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Sorafenib.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Sorafenib.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Sorafenib.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Sorafenib.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Sorafenib.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Sorafenib.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Sorafenib.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Sorafenib.
Cladribine Sorafenib may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Sorafenib.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Sorafenib.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Sorafenib.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Sorafenib.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Sorafenib.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Sorafenib.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Sorafenib.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Sorafenib.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Sorafenib.
Streptozocin The risk or severity of adverse effects can be increased when Sorafenib is combined with Streptozocin.
Trifluridine The risk or severity of adverse effects can be increased when Sorafenib is combined with Trifluridine.
Lenalidomide The risk or severity of adverse effects can be increased when Sorafenib is combined with Lenalidomide.
Altretamine The risk or severity of adverse effects can be increased when Sorafenib is combined with Altretamine.
Cisplatin The risk or severity of adverse effects can be increased when Sorafenib is combined with Cisplatin.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Sorafenib.
Pentostatin The risk or severity of adverse effects can be increased when Sorafenib is combined with Pentostatin.
Linezolid The risk or severity of adverse effects can be increased when Sorafenib is combined with Linezolid.
Clofarabine The risk or severity of adverse effects can be increased when Sorafenib is combined with Clofarabine.
Prednisone The risk or severity of adverse effects can be increased when Sorafenib is combined with Prednisone.
Pemetrexed The risk or severity of adverse effects can be increased when Sorafenib is combined with Pemetrexed.
Fludrocortisone The risk or severity of adverse effects can be increased when Sorafenib is combined with Fludrocortisone.
Sulfasalazine The risk or severity of adverse effects can be increased when Sorafenib is combined with Sulfasalazine.
Temozolomide The risk or severity of adverse effects can be increased when Sorafenib is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Sorafenib is combined with Penicillamine.
Mechlorethamine The risk or severity of adverse effects can be increased when Sorafenib is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Sorafenib is combined with Azacitidine.
Azathioprine The risk or severity of adverse effects can be increased when Sorafenib is combined with Azathioprine.
Hydroxyurea The risk or severity of adverse effects can be increased when Sorafenib is combined with Hydroxyurea.
Mercaptopurine The risk or severity of adverse effects can be increased when Sorafenib is combined with Mercaptopurine.
Thalidomide The metabolism of Sorafenib can be increased when combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Sorafenib is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Sorafenib is combined with Fludarabine.
Procarbazine The risk or severity of adverse effects can be increased when Sorafenib is combined with Procarbazine.
Arsenic trioxide The risk or severity of QTc prolongation can be increased when Arsenic trioxide is combined with Sorafenib.
Idarubicin The risk or severity of adverse effects can be increased when Sorafenib is combined with Idarubicin.
Estramustine The risk or severity of adverse effects can be increased when Sorafenib is combined with Estramustine.
Lomustine The risk or severity of adverse effects can be increased when Sorafenib is combined with Lomustine.
Eculizumab The risk or severity of adverse effects can be increased when Sorafenib is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Sorafenib is combined with Decitabine.
Nelarabine The risk or severity of adverse effects can be increased when Sorafenib is combined with Nelarabine.
Ciclesonide The risk or severity of adverse effects can be increased when Sorafenib is combined with Ciclesonide.
Stepronin The risk or severity of adverse effects can be increased when Sorafenib is combined with Stepronin.
Castanospermine The risk or severity of adverse effects can be increased when Sorafenib is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Sorafenib is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Sorafenib is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Sorafenib is combined with Brequinar.
Aldosterone The risk or severity of adverse effects can be increased when Sorafenib is combined with Aldosterone.
Pirfenidone The risk or severity of adverse effects can be increased when Sorafenib is combined with Pirfenidone.
Interferon alfa The risk or severity of adverse effects can be increased when Sorafenib is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Sorafenib is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Sorafenib is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Sorafenib is combined with Human interferon omega-1.
Mepolizumab The risk or severity of adverse effects can be increased when Sorafenib is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Sorafenib is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Sorafenib is combined with Belatacept.
Pralatrexate The risk or severity of adverse effects can be increased when Sorafenib is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Sorafenib is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Sorafenib is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Sorafenib is combined with Belimumab.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Sorafenib is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Sorafenib is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Sorafenib is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Sorafenib is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Sorafenib is combined with Dinutuximab.
Vilanterol The risk or severity of QTc prolongation and ventricular arrhythmias can be increased when Vilanterol is combined with Sorafenib.
Tixocortol The risk or severity of adverse effects can be increased when Sorafenib is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Sorafenib is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Sorafenib is combined with Antilymphocyte immunoglobulin (horse).
Fluprednisolone The risk or severity of adverse effects can be increased when Sorafenib is combined with Fluprednisolone.
Tepoxalin The risk or severity of adverse effects can be increased when Sorafenib is combined with Tepoxalin.
Melengestrol The risk or severity of adverse effects can be increased when Sorafenib is combined with Melengestrol.
Ixekizumab The risk or severity of adverse effects can be increased when Sorafenib is combined with Ixekizumab.
Ravulizumab The risk or severity of adverse effects can be increased when Sorafenib is combined with Ravulizumab.
Pirarubicin The risk or severity of adverse effects can be increased when Sorafenib is combined with Pirarubicin.
Voclosporin The risk or severity of adverse effects can be increased when Sorafenib is combined with Voclosporin.
Peficitinib The risk or severity of adverse effects can be increased when Sorafenib is combined with Peficitinib.
Brodalumab The risk or severity of adverse effects can be increased when Sorafenib is combined with Brodalumab.

Target Protein

Serine/threonine-protein kinase B-raf BRAF
Epidermal growth factor receptor EGFR
RAF proto-oncogene serine/threonine-protein kinase RAF1
Vascular endothelial growth factor receptor 3 FLT4
Vascular endothelial growth factor receptor 2 KDR
Vascular endothelial growth factor receptor 1 FLT1
Receptor-type tyrosine-protein kinase FLT3 FLT3
Platelet-derived growth factor receptor beta PDGFRB
Mast/stem cell growth factor receptor Kit KIT
Fibroblast growth factor receptor 1 FGFR1
Proto-oncogene tyrosine-protein kinase receptor Ret RET

Referensi & Sumber

Synthesis reference: Ales Gavenda, Alexandr Jegorov, Pierluigi Rossetto, Peter Lindsay MacDonald, Augusto Canavesi, "POLYMORPHS OF SORAFENIB TOSYLATE AND SORAFENIB HEMI-TOSYLATE, AND PROCESSES FOR PREPARATION THEREOF." U.S. Patent US20090192200, issued July 30, 2009.
Artikel (PubMed)
  • PMID: 20586710
    Iyer R, Fetterly G, Lugade A, Thanavala Y: Sorafenib: a clinical and pharmacologic review. Expert Opin Pharmacother. 2010 Aug;11(11):1943-55. doi: 10.1517/14656566.2010.496453.
  • PMID: 28299600
    Keating GM: Sorafenib: A Review in Hepatocellular Carcinoma. Target Oncol. 2017 Apr;12(2):243-253. doi: 10.1007/s11523-017-0484-7.
  • PMID: 19228077
    Keating GM, Santoro A: Sorafenib: a review of its use in advanced hepatocellular carcinoma. Drugs. 2009;69(2):223-40. doi: 10.2165/00003495-200969020-00006.
  • PMID: 16757355
    Adnane L, Trail PA, Taylor I, Wilhelm SM: Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Methods Enzymol. 2006;407:597-612.

Contoh Produk & Brand

Produk: 15 • International brands: 0
Produk
  • Apo-sorafenib
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Nexavar
    Tablet, film coated • 200 mg/1 • Oral • US • Approved
  • Nexavar
    Tablet, film coated • 200 mg/1 • Oral • US • Approved
  • Nexavar
    Tablet • 200 mg • Oral • Canada • Approved
  • Nexavar
    Tablet, film coated • 200 mg/1 • Oral • US • Approved
  • Nexavar
    Tablet, film coated • 200 mg • Oral • EU • Approved
  • Sorafenib
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • Approved
  • Sorafenib
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 15 produk.

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