Vandetanib

DB05294

small molecule approved

Deskripsi

Vandetanib is an oral once-daily kinase inhibitor of tumour angiogenesis and tumour cell proliferation with the potential for use in a broad range of tumour types.

On April 6 2011, vandetanib was approved by the FDA to treat nonresectable, locally advanced, or metastatic medullary thyroid cancer in adult patients.

Struktur Molekul 2D

Berat 475.354
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Median half life of 19 days.
Volume Distribusi Vd of about 7450 L.
Klirens (Clearance) -

Absorpsi

Slow- peak plasma concentrations reached at a median 6 hours. On multiple dosing, Vandetanib accumulates about 8 fold with steady state reached after around 3 months.

Metabolisme

Unchanged vandentanib and metabolites vandetanib N-oxide and N-desmethyl vandetanib were detected in plasma, urine and feces. N-desmethyl-vandetanib is primarily produced by CYP3A4, and vandetanib-N-oxide is primarily produced by flavin–containing monooxygenase enzymes FMO1 and FMO3.

Rute Eliminasi

About 69% was recovered following 21 days after a single dose of vandentanib. 44% was found in feces and 25% in urine.

Interaksi Makanan

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

Interaksi Obat

922 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Vandetanib.
Modafinil The metabolism of Vandetanib can be increased when combined with Modafinil.
Armodafinil The metabolism of Vandetanib can be increased when combined with Armodafinil.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Vandetanib.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Vandetanib.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Vandetanib.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Vandetanib.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Vandetanib.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Vandetanib.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Vandetanib.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Vandetanib.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Vandetanib.
Silodosin The excretion of Silodosin can be decreased when combined with Vandetanib.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Vandetanib.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Vandetanib.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Vandetanib.
Metreleptin The metabolism of Vandetanib can be increased when combined with Metreleptin.
Propacetamol The serum concentration of Propacetamol can be increased when it is combined with Vandetanib.
Crizotinib The metabolism of Vandetanib can be decreased when combined with Crizotinib.
Vincristine The excretion of Vincristine can be decreased when combined with Vandetanib.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Vandetanib.
Leuprolide The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Vandetanib.
Goserelin The risk or severity of QTc prolongation can be increased when Goserelin is combined with Vandetanib.
Azithromycin The risk or severity of QTc prolongation can be increased when Azithromycin is combined with Vandetanib.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Vandetanib.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Sulfisoxazole is combined with Vandetanib.
Sulpiride The risk or severity of QTc prolongation can be increased when Sulpiride is combined with Vandetanib.
Nimodipine The risk or severity of QTc prolongation can be increased when Nimodipine is combined with Vandetanib.
Promazine The risk or severity of QTc prolongation can be increased when Promazine is combined with Vandetanib.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Prochlorperazine is combined with Vandetanib.
Droperidol The risk or severity of QTc prolongation can be increased when Droperidol is combined with Vandetanib.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Vandetanib.
Fluorouracil The risk or severity of QTc prolongation can be increased when Fluorouracil is combined with Vandetanib.
Perflutren The risk or severity of QTc prolongation can be increased when Perflutren is combined with Vandetanib.
Cinnarizine The risk or severity of QTc prolongation can be increased when Cinnarizine is combined with Vandetanib.
Atropine The risk or severity of QTc prolongation can be increased when Atropine is combined with Vandetanib.
Chloroquine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Vandetanib.
Adenosine The risk or severity of QTc prolongation can be increased when Adenosine is combined with Vandetanib.
Pentamidine The risk or severity of QTc prolongation can be increased when Pentamidine is combined with Vandetanib.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Vandetanib.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Carbinoxamine is combined with Vandetanib.
Dolasetron The risk or severity of QTc prolongation can be increased when Dolasetron is combined with Vandetanib.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Nalidixic acid is combined with Vandetanib.
Cinoxacin The risk or severity of QTc prolongation can be increased when Cinoxacin is combined with Vandetanib.
Granisetron The risk or severity of QTc prolongation can be increased when Granisetron is combined with Vandetanib.
Ondansetron The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Vandetanib.
Levosimendan The risk or severity of QTc prolongation can be increased when Levosimendan is combined with Vandetanib.
Mesoridazine The risk or severity of QTc prolongation can be increased when Mesoridazine is combined with Vandetanib.
Desloratadine The risk or severity of QTc prolongation can be increased when Desloratadine is combined with Vandetanib.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Lomefloxacin is combined with Vandetanib.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Vandetanib.
Papaverine The risk or severity of QTc prolongation can be increased when Papaverine is combined with Vandetanib.
Chlorpheniramine The risk or severity of QTc prolongation can be increased when Chlorpheniramine is combined with Vandetanib.
Levofloxacin The risk or severity of QTc prolongation can be increased when Levofloxacin is combined with Vandetanib.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Gemifloxacin is combined with Vandetanib.
Ofloxacin The risk or severity of QTc prolongation can be increased when Ofloxacin is combined with Vandetanib.
Propafenone The risk or severity of QTc prolongation can be increased when Propafenone is combined with Vandetanib.
Flecainide The risk or severity of QTc prolongation can be increased when Flecainide is combined with Vandetanib.
Probucol The risk or severity of QTc prolongation can be increased when Probucol is combined with Vandetanib.
Aceprometazine The risk or severity of QTc prolongation can be increased when Aceprometazine is combined with Vandetanib.
Terlipressin The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Vandetanib.
Prenylamine The risk or severity of QTc prolongation can be increased when Prenylamine is combined with Vandetanib.
Fluspirilene The risk or severity of QTc prolongation can be increased when Fluspirilene is combined with Vandetanib.
Lofexidine The risk or severity of QTc prolongation can be increased when Lofexidine is combined with Vandetanib.
Azimilide The risk or severity of QTc prolongation can be increased when Azimilide is combined with Vandetanib.
Pracinostat The risk or severity of QTc prolongation can be increased when Pracinostat is combined with Vandetanib.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Technetium Tc-99m ciprofloxacin is combined with Vandetanib.
Garenoxacin The risk or severity of QTc prolongation can be increased when Garenoxacin is combined with Vandetanib.
Tedisamil The risk or severity of QTc prolongation can be increased when Tedisamil is combined with Vandetanib.
Tucidinostat The risk or severity of QTc prolongation can be increased when Tucidinostat is combined with Vandetanib.
Telavancin The risk or severity of QTc prolongation can be increased when Telavancin is combined with Vandetanib.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Nemonoxacin is combined with Vandetanib.
Antazoline The risk or severity of QTc prolongation can be increased when Antazoline is combined with Vandetanib.
Bedaquiline The risk or severity of QTc prolongation can be increased when Vandetanib is combined with Bedaquiline.
Fendiline The risk or severity of QTc prolongation can be increased when Fendiline is combined with Vandetanib.
Eperisone The risk or severity of QTc prolongation can be increased when Eperisone is combined with Vandetanib.
Butriptyline The risk or severity of QTc prolongation can be increased when Butriptyline is combined with Vandetanib.
Melperone The risk or severity of QTc prolongation can be increased when Melperone is combined with Vandetanib.
Dexchlorpheniramine maleate The risk or severity of QTc prolongation can be increased when Dexchlorpheniramine maleate is combined with Vandetanib.
Amifampridine The risk or severity of QTc prolongation can be increased when Amifampridine is combined with Vandetanib.
Mocetinostat The risk or severity of QTc prolongation can be increased when Mocetinostat is combined with Vandetanib.
Entinostat The risk or severity of QTc prolongation can be increased when Entinostat is combined with Vandetanib.
Gilteritinib The risk or severity of QTc prolongation can be increased when Gilteritinib is combined with Vandetanib.
CUDC-101 The risk or severity of QTc prolongation can be increased when CUDC-101 is combined with Vandetanib.
Simendan The risk or severity of QTc prolongation can be increased when Simendan is combined with Vandetanib.
Ricolinostat The risk or severity of QTc prolongation can be increased when Ricolinostat is combined with Vandetanib.
Mizolastine The risk or severity of QTc prolongation can be increased when Mizolastine is combined with Vandetanib.
Abexinostat The risk or severity of QTc prolongation can be increased when Abexinostat is combined with Vandetanib.
Oxatomide The risk or severity of QTc prolongation can be increased when Oxatomide is combined with Vandetanib.
Sitafloxacin The risk or severity of QTc prolongation can be increased when Sitafloxacin is combined with Vandetanib.
Sultopride The risk or severity of QTc prolongation can be increased when Sultopride is combined with Vandetanib.
Otilonium The risk or severity of QTc prolongation can be increased when Otilonium is combined with Vandetanib.
Nizofenone The risk or severity of QTc prolongation can be increased when Nizofenone is combined with Vandetanib.
Bunaftine The risk or severity of QTc prolongation can be increased when Bunaftine is combined with Vandetanib.
Lorcainide The risk or severity of QTc prolongation can be increased when Lorcainide is combined with Vandetanib.
Dexchlorpheniramine The risk or severity of QTc prolongation can be increased when Dexchlorpheniramine is combined with Vandetanib.
Penfluridol The risk or severity of QTc prolongation can be increased when Penfluridol is combined with Vandetanib.
Dexverapamil The risk or severity of QTc prolongation can be increased when Dexverapamil is combined with Vandetanib.
Quetiapine The risk or severity of QTc prolongation can be increased when Quetiapine is combined with Vandetanib.
Levacetylmethadol The risk or severity of QTc prolongation can be increased when Levacetylmethadol is combined with Vandetanib.

Target Protein

Vascular endothelial growth factor receptor 2 KDR
Proto-oncogene tyrosine-protein kinase receptor Ret RET
Epidermal growth factor receptor EGFR
Vascular endothelial growth factor A, long form VEGFA
Protein-tyrosine kinase 6 PTK6
Angiopoietin-1 receptor TEK

Referensi & Sumber

Artikel (PubMed)
  • PMID: 14763134
    Bates D: ZD-6474. AstraZeneca. Curr Opin Investig Drugs. 2003 Dec;4(12):1468-72.
  • PMID: 23640345
    Ton GN, Banaszynski ME, Kolesar JM: Vandetanib: a novel targeted therapy for the treatment of metastatic or locally advanced medullary thyroid cancer. Am J Health Syst Pharm. 2013 May 15;70(10):849-55. doi: 10.2146/ajhp120253.
  • PMID: 23562906
    Andriamanana I, Gana I, Duretz B, Hulin A: Simultaneous analysis of anticancer agents bortezomib, imatinib, nilotinib, dasatinib, erlotinib, lapatinib, sorafenib, sunitinib and vandetanib in human plasma using LC/MS/MS. J Chromatogr B Analyt Technol Biomed Life Sci. 2013 May 1;926:83-91. doi: 10.1016/j.jchromb.2013.01.037. Epub 2013 Mar 16.

Contoh Produk & Brand

Produk: 11 • International brands: 2
Produk
  • Caprelsa
    Tablet, film coated • 300 mg • Oral • EU • Approved
  • Caprelsa
    Tablet • 100 mg/1 • Oral • US • Approved
  • Caprelsa
    Tablet • 300 mg/1 • Oral • US • Approved
  • Caprelsa
    Tablet • 100 mg • Oral • Canada • Approved
  • Caprelsa
    Tablet • 300 mg • Oral • Canada • Approved
  • Caprelsa
    Tablet, film coated • 100 mg/1 • Oral • US • Approved
  • Caprelsa
    Tablet, film coated • 300 mg/1 • Oral • US • Approved
  • Caprelsa
    Tablet, film coated • 300 mg/1 • Oral • US
Menampilkan 8 dari 11 produk.
International Brands
  • Zactima — AstraZeneca
  • Zictifa — AstraZeneca

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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