Pazopanib

DB06589

small molecule approved

Deskripsi

Pazopanib is a small molecule inhibitor of multiple protein tyrosine kinases with potential antineoplastic activity. It is developed by GlaxoSmithKline and was FDA approved on October 19, 2009.

Struktur Molekul 2D

Berat 437.518
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 35 hours. Oral absorption is not the rate limiting step of elimination from the plasma.
Volume Distribusi Vd steady state, IV administration 5 mg, cancer patient = 11.1 L (range of 9.15 - 13.4)
Klirens (Clearance) CL, cancer patient, IV administration 5 mg = 4mL/min Half of the absorbed dose is cleared via oxidative metabolism.

Absorpsi

Absorption of pazopanib in cancer patients is slow and incomplete. In patients with solid tumour, over a dose range of 50-2000 mg, absorption is nonlinear. Significant accumulation of pazopanib can also be observed in patients receiving 800 mg once daily for 22 days. Crushing tablets may increase exposure (increase in Cmax and AUC, while Tmax decreases by 2 hours). Bioavailability, oral tablet 800 mg, cancer patient = 21%; Bioavailability may be low due to incomplete absorption from the gastrointestinal tract. The major circulating component of the drug in the systemic is pazopanib, and not its metabolites. Mean maximum plasma concentration= 58.1 µg/mL; Mean AUC= 1037 µg · h/mL;

Metabolisme

Metabolized by CYP3A4 and to a lesser extent by CYP1A2 and CYP2C8. Metabolites are less active than pazopanib (10 to 20-fold less active). Three of its metabolites can be observed in the systemic and account for <10% of plasma radioactivity.

Rute Eliminasi

Primarily excreted via feces (82.2%) and to a negligible extent via urine (<4%) in cancer patients. Most of the administered dose is excreted unchanged. Approximately 10% of dose are oxidative metabolites and are mostly eliminated via the feces.

Farmakogenomik

2 Varian
UGT1A1 (rs3064744)

The presence of this polymorphism in UGT1A1 is associated with an increase in the incidence of hyperbilirubinemia when treated with pazopanib.

HCP5 (rs2395029)

The presence of this polymorphism in HCP5 may indicate an increased risk of ALT elevation leading to drug-related hepatotoxicty from pazpanib therapy.

Interaksi Makanan

4 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of pazopanib.
  • 2. Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum concentration of pazopanib.
  • 3. Take on an empty stomach. Separate pazopanib from meals by at least 1 hour before and 2 hours after eating as food increases pazopanib bioavailability.
  • 4. Take separate from antacids. Separate the administration of pazopanib and antacids by several hours.

Interaksi Obat

1534 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Pazopanib.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Pazopanib.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Pazopanib.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Pazopanib.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Pazopanib.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Pazopanib.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Pazopanib.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Pazopanib.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Pazopanib.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Pazopanib.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Pazopanib.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Pazopanib.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Pazopanib.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Pazopanib.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Pazopanib.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Pazopanib.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Pazopanib.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Pazopanib.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Pazopanib.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Pazopanib.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Pazopanib.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Pazopanib.
Cladribine Pazopanib may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Pazopanib.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Pazopanib.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Pazopanib.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Pazopanib.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Pazopanib.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Pazopanib.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Pazopanib.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Pazopanib.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Pazopanib.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Pazopanib.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Pazopanib.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Pazopanib.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Pazopanib.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Pazopanib.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Pazopanib.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Pazopanib.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Pazopanib.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Pazopanib.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Pazopanib.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Pazopanib.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Pazopanib.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Pazopanib.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Pazopanib.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Pazopanib.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Pazopanib.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Pazopanib.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Pazopanib.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Pazopanib.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Pazopanib.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Pazopanib.
Thalidomide The metabolism of Pazopanib can be increased when combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Pazopanib.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Pazopanib.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Pazopanib.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Pazopanib.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Pazopanib.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Pazopanib.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Pazopanib.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Pazopanib.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Pazopanib.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Pazopanib.
Ciclesonide The risk or severity of adverse effects can be increased when Ciclesonide is combined with Pazopanib.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Pazopanib.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Pazopanib.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Pazopanib.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Pazopanib.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Pazopanib.
Aldosterone The risk or severity of adverse effects can be increased when Aldosterone is combined with Pazopanib.
Pirfenidone The risk or severity of adverse effects can be increased when Pirfenidone is combined with Pazopanib.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Pazopanib.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Pazopanib.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Pazopanib.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Pazopanib.
Mepolizumab The risk or severity of adverse effects can be increased when Pazopanib is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Pazopanib is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Pazopanib is combined with Belatacept.
Bendamustine The risk or severity of adverse effects can be increased when Pazopanib is combined with Bendamustine.
Pralatrexate The risk or severity of adverse effects can be increased when Pazopanib is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Pazopanib is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Pazopanib is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Pazopanib is combined with Belimumab.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Pazopanib is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Pazopanib is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Pazopanib is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Pazopanib is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Pazopanib is combined with Dinutuximab.
Vilanterol The risk or severity of QTc prolongation and ventricular arrhythmias can be increased when Vilanterol is combined with Pazopanib.
Tixocortol The risk or severity of adverse effects can be increased when Pazopanib is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Pazopanib is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Pazopanib is combined with Antilymphocyte immunoglobulin (horse).
Fluprednisolone The risk or severity of adverse effects can be increased when Pazopanib is combined with Fluprednisolone.
Tepoxalin The risk or severity of adverse effects can be increased when Pazopanib is combined with Tepoxalin.
Melengestrol The risk or severity of adverse effects can be increased when Pazopanib is combined with Melengestrol.
Ixekizumab The risk or severity of adverse effects can be increased when Pazopanib is combined with Ixekizumab.
Ravulizumab The risk or severity of adverse effects can be increased when Pazopanib is combined with Ravulizumab.
Pirarubicin The risk or severity of adverse effects can be increased when Pazopanib is combined with Pirarubicin.
Peficitinib The risk or severity of adverse effects can be increased when Pazopanib is combined with Peficitinib.

Target Protein

Vascular endothelial growth factor receptor 1 FLT1
Vascular endothelial growth factor receptor 2 KDR
Vascular endothelial growth factor receptor 3 FLT4
Platelet-derived growth factor receptor alpha PDGFRA
Platelet-derived growth factor receptor beta PDGFRB
Mast/stem cell growth factor receptor Kit KIT
Fibroblast growth factor receptor 3 FGFR3
Tyrosine-protein kinase ITK/TSK ITK
Fibroblast growth factor 1 FGF1
SH2B adapter protein 3 SH2B3

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18230058
    Sonpavde G, Hutson TE, Sternberg CN: Pazopanib, a potent orally administered small-molecule multitargeted tyrosine kinase inhibitor for renal cell carcinoma. Expert Opin Investig Drugs. 2008 Feb;17(2):253-61. doi: 10.1517/13543784.17.2.253.
  • PMID: 23488774
    Verweij J, Sleijfer S: Pazopanib, a new therapy for metastatic soft tissue sarcoma. Expert Opin Pharmacother. 2013 May;14(7):929-35. doi: 10.1517/14656566.2013.780030. Epub 2013 Mar 14.
  • PMID: 23548165
    Deng Y, Sychterz C, Suttle AB, Dar MM, Bershas D, Negash K, Qian Y, Chen EP, Gorycki PD, Ho MY: Bioavailability, metabolism and disposition of oral pazopanib in patients with advanced cancer. Xenobiotica. 2013 May;43(5):443-53. doi: 10.3109/00498254.2012.734642. Epub 2012 Nov 16.
  • PMID: 23072642
    Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000.

Contoh Produk & Brand

Produk: 19 • International brands: 0
Produk
  • Eugia-pazopanib
    Tablet • 200 mg • Oral • Canada • Approved
  • Pazopanib
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • Approved
  • Pazopanib
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • Approved
  • Pazopanib
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • Approved
  • Pazopanib
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • Approved
  • Pazopanib
    Tablet • 200 mg/1 • Oral • US • Generic • Approved
  • Pazopanib
    Tablet • 200 mg/1 • Oral • US • Generic • Approved
  • Pazopanib
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 19 produk.

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