Peringatan Keamanan

The maximally tolerated dose for rat, mouse, and dog when given orally is greater than 500 mg/kg. The maximally tolerated dose of a non-human primate is greater 1200 mg/kg.

Sunitinib

DB01268

small molecule approved investigational

Deskripsi

Sunitinib is a small-molecule multi-targeted receptor tyrosine kinase (RTK) inhibitor. On January 26, 2006, the agent was formally approved by the US FDA for the indications of treating renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). For these purposes, sunitinib is generally available as an orally administered formulation. Sunitinib inhibits cellular signaling by targeting multiple RTKs. These include all platelet-derived growth factor receptors (PDGF-R) and vascular endothelial growth factor receptors (VEGF-R). Sunitinib also inhibits KIT (CD117), the RTK that drives the majority of GISTs. In addition, sunitinib inhibits other RTKs including RET, CSF-1R, and flt3.

Struktur Molekul 2D

Berat 398.4738
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following administration of a single oral dose in healthy volunteers, the terminal half-lives of sunitinib and its primary active metabolite are approximately 40 to 60 hours and 80 to 110 hours, respectively.
Volume Distribusi * 2230 L (apparent volume of distribution, Vd/F)
Klirens (Clearance) * 34 - 62 L/h [Total oral clearance]

Absorpsi

Maximum plasma concentrations (Cmax) of sunitinib are generally observed between 6 and 12 hours (Tmax) following oral administration. Food has no effect on the bioavailability of sunitinib. Sunitinib may be taken with or without food. The pharmacokinetics were similar in healthy volunteers and in the solid tumor patient populations tested, including patients with GIST and RCC.

Metabolisme

Sunitinib is metabolized primarily by the cytochrome P450 enzyme, CYP3A4, to produce its primary active metabolite, which is further metabolized by CYP3A4.

Rute Eliminasi

Sunitinib is metabolized primarily by the cytochrome P450 enzyme, CYP3A4, to produce its primary active metabolite, which is further metabolized by CYP3A4. Elimination is primarily via feces. In a human mass balance study of 14Csunitinib, 61% of the dose was eliminated in feces, with renal elimination accounting for 16% of the administered dose.

Farmakogenomik

1 Varian
CYP3A4 (rs4646437)

Patients with metastatic renal cell carcinoma who carry this polymorphism in CYP3A4 are at a higher risk of experiencing drug-induced hypertension when treated with sunitinib.

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products. Grapefruit may reduce the CYP3A4 metabolism of sunitinib.
  • 2. Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum concentration of sunitinib.
  • 3. Take with or without food.

Interaksi Obat

1513 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Sunitinib.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Sunitinib.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Sunitinib.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Sunitinib.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Sunitinib.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Sunitinib.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Sunitinib.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Sunitinib.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Sunitinib.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Sunitinib.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Sunitinib.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Sunitinib.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Sunitinib.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Sunitinib.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Sunitinib.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Sunitinib.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Sunitinib.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Sunitinib.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Sunitinib.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Sunitinib.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Sunitinib.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Sunitinib.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Sunitinib.
Cladribine The excretion of Cladribine can be decreased when combined with Sunitinib.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Sunitinib.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Sunitinib.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Sunitinib.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Sunitinib.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Sunitinib.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Sunitinib.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Sunitinib.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Sunitinib.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Sunitinib.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Sunitinib.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Sunitinib.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Sunitinib.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Sunitinib.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Sunitinib.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Sunitinib.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Sunitinib.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Sunitinib.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Sunitinib.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Sunitinib.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Sunitinib.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Sunitinib.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Sunitinib.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Sunitinib.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Sunitinib.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Sunitinib.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Sunitinib.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Sunitinib.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Sunitinib.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Sunitinib.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Sunitinib.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Sunitinib.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Sunitinib.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Sunitinib.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Sunitinib.
Thalidomide The metabolism of Sunitinib can be increased when combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Sunitinib.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Sunitinib.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Sunitinib.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Sunitinib.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Sunitinib.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Sunitinib.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Sunitinib.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Sunitinib.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Sunitinib.
Nelarabine The risk or severity of adverse effects can be increased when Sunitinib is combined with Nelarabine.
Stepronin The risk or severity of adverse effects can be increased when Sunitinib is combined with Stepronin.
Castanospermine The risk or severity of adverse effects can be increased when Sunitinib is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Sunitinib is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Sunitinib is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Sunitinib is combined with Brequinar.
Pirfenidone The risk or severity of adverse effects can be increased when Sunitinib is combined with Pirfenidone.
Interferon alfa The risk or severity of adverse effects can be increased when Sunitinib is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Sunitinib is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Sunitinib is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Sunitinib is combined with Human interferon omega-1.
Mepolizumab The risk or severity of adverse effects can be increased when Sunitinib is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Sunitinib is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Sunitinib is combined with Belatacept.
Bendamustine The risk or severity of adverse effects can be increased when Sunitinib is combined with Bendamustine.
Pralatrexate The risk or severity of adverse effects can be increased when Sunitinib is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Sunitinib is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Sunitinib is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Sunitinib is combined with Belimumab.
Teriflunomide The risk or severity of liver damage can be increased when Sunitinib is combined with Teriflunomide.
Carfilzomib The risk or severity of adverse effects can be increased when Sunitinib is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Sunitinib is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Sunitinib is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Sunitinib is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Sunitinib is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Sunitinib is combined with Dinutuximab.
Vilanterol The risk or severity of QTc prolongation and ventricular arrhythmias can be increased when Vilanterol is combined with Sunitinib.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Sunitinib is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Sunitinib is combined with Antilymphocyte immunoglobulin (horse).
Tepoxalin The risk or severity of adverse effects can be increased when Sunitinib is combined with Tepoxalin.
Ixekizumab The risk or severity of adverse effects can be increased when Sunitinib is combined with Ixekizumab.
Ravulizumab The risk or severity of adverse effects can be increased when Sunitinib is combined with Ravulizumab.

Target Protein

Platelet-derived growth factor receptor beta PDGFRB
Vascular endothelial growth factor receptor 1 FLT1
Mast/stem cell growth factor receptor Kit KIT
Vascular endothelial growth factor receptor 2 KDR
Vascular endothelial growth factor receptor 3 FLT4
Receptor-type tyrosine-protein kinase FLT3 FLT3
Macrophage colony-stimulating factor 1 receptor CSF1R
Platelet-derived growth factor receptor alpha PDGFRA
Hepatocyte growth factor receptor MET

Referensi & Sumber

Synthesis reference: Ettore BIGATTI, Augusto CANAVESI, Peter Lindsay MACDONALD, Francesca Scarpitta, "PROCESSES FOR PREPARING SUNITINIB AND SALTS THEREOF." U.S. Patent US20090247767, issued October 01, 2009.
Artikel (PubMed)
  • PMID: 17215529
    Motzer RJ, Hutson TE, Tomczak P, Michaelson MD, Bukowski RM, Rixe O, Oudard S, Negrier S, Szczylik C, Kim ST, Chen I, Bycott PW, Baum CM, Figlin RA: Sunitinib versus interferon alfa in metastatic renal-cell carcinoma. N Engl J Med. 2007 Jan 11;356(2):115-24.
  • PMID: 17046465
    Demetri GD, van Oosterom AT, Garrett CR, Blackstein ME, Shah MH, Verweij J, McArthur G, Judson IR, Heinrich MC, Morgan JA, Desai J, Fletcher CD, George S, Bello CL, Huang X, Baum CM, Casali PG: Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial. Lancet. 2006 Oct 14;368(9544):1329-38.

Contoh Produk & Brand

Produk: 84 • International brands: 0
Produk
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    Capsule • 12.5 mg • Oral • Canada • Generic • Approved
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    Capsule • 25 mg • Oral • Canada • Generic • Approved
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    Capsule • 37.5 mg • Oral • Canada • Generic • Approved
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  • Eugia-sunitinib
    Capsule • 12.5 mg • Oral • Canada • Approved
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    Capsule • 25 mg • Oral • Canada • Approved
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    Capsule • 37.5 mg • Oral • Canada • Approved
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Menampilkan 8 dari 84 produk.

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