Peringatan Keamanan

Some of the more serious toxic effects seen in patients taking axitinib include, but are not limited to, hypertension, thrombotic events, hemorrhage, and GI perforation.

Axitinib

DB06626

small molecule approved investigational

Deskripsi

Axitinib is a second generation tyrosine kinase inhibitor that works by selectively inhibiting vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3).L6676 Through this mechanism of action, axitinib blocks angiogenesis, tumour growth and metastases. It is reported to exhibit potency that is 50-450 times higher than that of the first generation VEGFR inhibitors.L6676 Axitinib is an indazole derivative.A179398 It is most commonly marketed under the name Inlyta® and is available in oral formulations.

Struktur Molekul 2D

Berat 386.47
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Axitinib has a half life of 2.5 to 6.1 hours.
Volume Distribusi The volume of distribution is 160 L.
Klirens (Clearance) The average clearance of axitinib is 38 L/h.

Absorpsi

After one 5 mg dose of axitinib, it takes about 2.5 to 4.1 hours to reach maximum plasma concentration.

Metabolisme

Axitinib undergoes mainly hepatic metabolism. CYP3A4 and CYP3A5 are the main hepatic enzymes while CYP1A2, CYP2C19, and UGT1A1 enzymes are secondary.

Rute Eliminasi

Axitinib is mainly eliminated unchanged in the feces (41%) with 12% of the original dose as unchanged axitinib. There is also 23% eliminated in the urine, most of which are metabolites.

Interaksi Makanan

4 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of axitinib.
  • 2. Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum concentration of axitinib.
  • 3. Take with a full glass of water.
  • 4. Take with or without food.

Interaksi Obat

993 Data
Deferasirox The serum concentration of Axitinib can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Axitinib can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Axitinib can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Axitinib can be decreased when it is combined with Teriflunomide.
Dabrafenib The serum concentration of Axitinib can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Axitinib can be increased when it is combined with Luliconazole.
Metreleptin The metabolism of Axitinib can be increased when combined with Metreleptin.
Propacetamol The serum concentration of Propacetamol can be increased when it is combined with Axitinib.
Crizotinib The metabolism of Axitinib can be decreased when combined with Crizotinib.
Abiraterone The serum concentration of Axitinib can be increased when it is combined with Abiraterone.
Sulpiride The risk or severity of adverse effects can be increased when Axitinib is combined with Sulpiride.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Axitinib.
Cyproterone acetate The metabolism of Axitinib can be increased when combined with Cyproterone acetate.
Lumacaftor The serum concentration of Axitinib can be decreased when it is combined with Lumacaftor.
Albendazole The metabolism of Axitinib can be increased when combined with Albendazole.
Ticlopidine The metabolism of Axitinib can be decreased when combined with Ticlopidine.
Imipramine The metabolism of Axitinib can be decreased when combined with Imipramine.
Clomipramine The metabolism of Axitinib can be decreased when combined with Clomipramine.
Lansoprazole The metabolism of Axitinib can be decreased when combined with Lansoprazole.
Osimertinib The serum concentration of Axitinib can be decreased when it is combined with Osimertinib.
Vemurafenib The serum concentration of Axitinib can be increased when it is combined with Vemurafenib.
Apalutamide The serum concentration of Axitinib can be increased when it is combined with Apalutamide.
Cholic Acid The excretion of Axitinib can be increased when combined with Cholic Acid.
Pitolisant The serum concentration of Axitinib can be decreased when it is combined with Pitolisant.
Valsartan The excretion of Axitinib can be decreased when combined with Valsartan.
Levocarnitine The excretion of Axitinib can be decreased when combined with Levocarnitine.
Sulfasalazine The excretion of Axitinib can be decreased when combined with Sulfasalazine.
Novobiocin The excretion of Axitinib can be decreased when combined with Novobiocin.
Ouabain The excretion of Axitinib can be decreased when combined with Ouabain.
Bezafibrate The excretion of Axitinib can be decreased when combined with Bezafibrate.
Hyperforin The excretion of Axitinib can be decreased when combined with Hyperforin.
Posizolid The excretion of Axitinib can be decreased when combined with Posizolid.
Acetylcysteine The excretion of Axitinib can be decreased when combined with Acetylcysteine.
Torasemide The excretion of Torasemide can be decreased when combined with Axitinib.
Penicillamine The excretion of Penicillamine can be decreased when combined with Axitinib.
Repaglinide The excretion of Repaglinide can be decreased when combined with Axitinib.
Dinoprostone The excretion of Dinoprostone can be decreased when combined with Axitinib.
Benzylpenicillin The excretion of Benzylpenicillin can be decreased when combined with Axitinib.
Atrasentan The excretion of Atrasentan can be decreased when combined with Axitinib.
Gimatecan The excretion of Gimatecan can be decreased when combined with Axitinib.
Temocapril The excretion of Temocapril can be decreased when combined with Axitinib.
Cholecystokinin The excretion of Cholecystokinin can be decreased when combined with Axitinib.
Gadoxetic acid The excretion of Gadoxetic acid can be decreased when combined with Axitinib.
Technetium Tc-99m mebrofenin The excretion of Technetium Tc-99m mebrofenin can be decreased when combined with Axitinib.
Fimasartan The excretion of Fimasartan can be decreased when combined with Axitinib.
Sacubitril The excretion of Axitinib can be decreased when combined with Sacubitril.
Nystatin The excretion of Axitinib can be decreased when combined with Nystatin.
Levosalbutamol The excretion of Levosalbutamol can be decreased when combined with Axitinib.
Caspofungin The excretion of Axitinib can be decreased when combined with Caspofungin.
Dipyridamole The excretion of Axitinib can be decreased when combined with Dipyridamole.
Quercetin The metabolism of Axitinib can be decreased when combined with Quercetin.
Taurocholic acid The excretion of Axitinib can be increased when combined with Taurocholic acid.
Enalapril The excretion of Enalapril can be decreased when combined with Axitinib.
Candesartan The excretion of Axitinib can be decreased when combined with Candesartan.
Methotrexate The excretion of Methotrexate can be decreased when combined with Axitinib.
Sumatriptan The excretion of Sumatriptan can be decreased when combined with Axitinib.
Ezetimibe The excretion of Ezetimibe can be decreased when combined with Axitinib.
Bempedoic acid The excretion of Axitinib can be decreased when combined with Bempedoic acid.
Ivermectin The excretion of Axitinib can be decreased when combined with Ivermectin.
Rosiglitazone The excretion of Axitinib can be decreased when combined with Rosiglitazone.
Trazodone The serum concentration of Axitinib can be decreased when it is combined with Trazodone.
Dexamethasone acetate The serum concentration of Axitinib can be decreased when it is combined with Dexamethasone acetate.
Dacomitinib The serum concentration of Axitinib can be increased when it is combined with Dacomitinib.
Pibrentasvir The serum concentration of Axitinib can be increased when it is combined with Pibrentasvir.
Istradefylline The serum concentration of Axitinib can be increased when it is combined with Istradefylline.
Reserpine The serum concentration of Axitinib can be increased when it is combined with Reserpine.
Everolimus The serum concentration of Axitinib can be increased when it is combined with Everolimus.
Voxilaprevir The serum concentration of Axitinib can be increased when it is combined with Voxilaprevir.
Daclatasvir The serum concentration of Axitinib can be increased when it is combined with Daclatasvir.
Velpatasvir The serum concentration of Axitinib can be increased when it is combined with Velpatasvir.
Valspodar The serum concentration of Axitinib can be increased when it is combined with Valspodar.
Fedratinib The serum concentration of Axitinib can be increased when it is combined with Fedratinib.
Sildenafil The serum concentration of Axitinib can be increased when it is combined with Sildenafil.
Simvastatin The serum concentration of Axitinib can be increased when it is combined with Simvastatin.
Elagolix The serum concentration of Axitinib can be increased when it is combined with Elagolix.
Propafenone The serum concentration of Axitinib can be increased when it is combined with Propafenone.
Carvedilol The serum concentration of Axitinib can be increased when it is combined with Carvedilol.
Vardenafil The serum concentration of Axitinib can be increased when it is combined with Vardenafil.
Zonisamide The serum concentration of Axitinib can be increased when it is combined with Zonisamide.
Paliperidone The serum concentration of Axitinib can be increased when it is combined with Paliperidone.
Ponatinib The serum concentration of Axitinib can be increased when it is combined with Ponatinib.
Vorapaxar The serum concentration of Axitinib can be increased when it is combined with Vorapaxar.
Suvorexant The serum concentration of Axitinib can be increased when it is combined with Suvorexant.
Loxapine The serum concentration of Axitinib can be increased when it is combined with Loxapine.
Toremifene The serum concentration of Axitinib can be increased when it is combined with Toremifene.
Biricodar The serum concentration of Axitinib can be increased when it is combined with Biricodar.
Elacridar The serum concentration of Axitinib can be increased when it is combined with Elacridar.
Flibanserin The serum concentration of Axitinib can be increased when it is combined with Flibanserin.
Vandetanib The serum concentration of Axitinib can be increased when it is combined with Vandetanib.
Zosuquidar The serum concentration of Axitinib can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Axitinib can be increased when it is combined with Tariquidar.
Carfilzomib The serum concentration of Axitinib can be increased when it is combined with Carfilzomib.
Mirabegron The serum concentration of Axitinib can be increased when it is combined with Mirabegron.
Canagliflozin The serum concentration of Axitinib can be increased when it is combined with Canagliflozin.
Afatinib The serum concentration of Axitinib can be increased when it is combined with Afatinib.
Ledipasvir The serum concentration of Axitinib can be increased when it is combined with Ledipasvir.
Niguldipine The serum concentration of Axitinib can be increased when it is combined with Niguldipine.
Rolapitant The serum concentration of Axitinib can be increased when it is combined with Rolapitant.
Lasmiditan The serum concentration of Axitinib can be increased when it is combined with Lasmiditan.
Neratinib The serum concentration of Axitinib can be increased when it is combined with Neratinib.

Target Protein

Tyrosine-protein kinase ABL1 ABL1
Vascular endothelial growth factor receptor 1 FLT1
Vascular endothelial growth factor receptor 2 KDR
Vascular endothelial growth factor receptor 3 FLT4

Referensi & Sumber

Synthesis reference: Hu-Lowe D, Hallin M, Feeley R, Zou H, Rewolinski D, Wickman G, Chen E, Kim Y, Riney S, Reed J, Heller D, Simmons B, Kania R, McTigue M, Niesman M, Gregory S, Shalinsky D, Bender S. Characterization of potency and activity of the VEGF/PDGF receptor tyrosine kinase inhibitor AG013736. Proc Am Assoc Cancer Res. 2002;43:A5357.
Artikel (PubMed)
  • PMID: 18541897
    Cohen EE, Rosen LS, Vokes EE, Kies MS, Forastiere AA, Worden FP, Kane MA, Sherman E, Kim S, Bycott P, Tortorici M, Shalinsky DR, Liau KF, Cohen RB: Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study. J Clin Oncol. 2008 Oct 10;26(29):4708-13. doi: 10.1200/JCO.2007.15.9566. Epub 2008 Jun 9.
  • PMID: 15215160
    Inai T, Mancuso M, Hashizume H, Baffert F, Haskell A, Baluk P, Hu-Lowe DD, Shalinsky DR, Thurston G, Yancopoulos GD, McDonald DM: Inhibition of vascular endothelial growth factor (VEGF) signaling in cancer causes loss of endothelial fenestrations, regression of tumor vessels, and appearance of basement membrane ghosts. Am J Pathol. 2004 Jul;165(1):35-52.
  • PMID: 16027439
    Rugo HS, Herbst RS, Liu G, Park JW, Kies MS, Steinfeldt HM, Pithavala YK, Reich SD, Freddo JL, Wilding G: Phase I trial of the oral antiangiogenesis agent AG-013736 in patients with advanced solid tumors: pharmacokinetic and clinical results. J Clin Oncol. 2005 Aug 20;23(24):5474-83. Epub 2005 Jul 18.
  • PMID: 16425985
    Rini BI: SU11248 and AG013736: current data and future trials in renal cell carcinoma. Clin Genitourin Cancer. 2005 Dec;4(3):175-80.
  • PMID: 23211371
    Gilbert JA, Adhikari LJ, Lloyd RV, Halfdanarson TR, Muders MH, Ames MM: Molecular markers for novel therapeutic strategies in pancreatic endocrine tumors. Pancreas. 2013 Apr;42(3):411-21. doi: 10.1097/MPA.0b013e31826cb243.
  • PMID: 24250243
    Gross-Goupil M, Francois L, Quivy A, Ravaud A: Axitinib: a review of its safety and efficacy in the treatment of adults with advanced renal cell carcinoma. Clin Med Insights Oncol. 2013 Oct 29;7:269-77. doi: 10.4137/CMO.S10594.

Contoh Produk & Brand

Produk: 20 • International brands: 0
Produk
  • Inlyta
    Tablet, film coated • 1 mg • Oral • EU • Approved
  • Inlyta
    Tablet, film coated • 1 mg • Oral • EU • Approved
  • Inlyta
    Tablet, film coated • 1 mg • Oral • EU • Approved
  • Inlyta
    Tablet, film coated • 5 mg • Oral • EU • Approved
  • Inlyta
    Tablet, film coated • 5 mg • Oral • EU • Approved
  • Inlyta
    Tablet, film coated • 5 mg • Oral • EU • Approved
  • Inlyta
    Tablet, film coated • 3 mg • Oral • EU • Approved
  • Inlyta
    Tablet, film coated • 3 mg • Oral • EU • Approved
Menampilkan 8 dari 20 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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