Peringatan Keamanan

Cabozantinib carries a warning of serious gastrointestinal fistulas and perforations, and potentially fatal hemoptysis and gastrointestinal hemorrhage.

Cabozantinib

DB08875

small molecule approved investigational

Deskripsi

Cabozantinib was first approved in 2012 and is a non-specific tyrosine kinase inhibitor. It was initially approved in the US under the brand name Cometriq, which is indicated for the treatment of metastatic medullary thyroid cancer.L15123 In 2016, a capsule formulation (Cabometyx) was approved for the treatment of advanced renal cell carcinoma, and this same formulation gained additional approval in both the US and Canada in 2019 for the treatment of hepatocellular carcinoma in previously treated patients.L15128,L15133

Struktur Molekul 2D

Berat 501.514
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Cabozantinib has a long half-life of 55 hours.
Volume Distribusi The volume of distribution is 349L.
Klirens (Clearance) At steady state, the clearance is 4.4 L/hr.

Absorpsi

After oral administration, peak plasma concentration was achieved in 2-5 hours.

Metabolisme

Cabozantinib is metabolized mostly by CYP3A4 and, to a minor extent, by CYP2C9. Both enzyme produce an N-oxide metabolite.

Rute Eliminasi

Cabozantinib is eliminated mostly by the feces (54%) and also by the urine (27%).

Interaksi Makanan

4 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase levels of cabozantinib.
  • 2. Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce serum levels of cabozantinib.
  • 3. Take on an empty stomach. Separate the administration of cabozantinib from food by at least 1 hour before or 2 hours after eating.
  • 4. Take with a full glass of water.

Interaksi Obat

513 Data
Acetaminophen The serum concentration of Acetaminophen can be increased when it is combined with Cabozantinib.
Pitolisant The serum concentration of Cabozantinib can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Cabozantinib can be increased when combined with Metreleptin.
Tazarotene The metabolism of Tazarotene can be decreased when combined with Cabozantinib.
Beraprost The metabolism of Beraprost can be decreased when combined with Cabozantinib.
Eltrombopag The metabolism of Eltrombopag can be decreased when combined with Cabozantinib.
Muraglitazar The metabolism of Muraglitazar can be decreased when combined with Cabozantinib.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Cabozantinib is combined with Benzyl alcohol.
Ombitasvir The metabolism of Ombitasvir can be decreased when combined with Cabozantinib.
Elagolix The metabolism of Elagolix can be decreased when combined with Cabozantinib.
Anastrozole The metabolism of Anastrozole can be decreased when combined with Cabozantinib.
Theophylline The metabolism of Theophylline can be decreased when combined with Cabozantinib.
Morphine The metabolism of Morphine can be decreased when combined with Cabozantinib.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Cabozantinib.
Chloroquine The metabolism of Chloroquine can be decreased when combined with Cabozantinib.
Mycophenolate mofetil The metabolism of Mycophenolate mofetil can be decreased when combined with Cabozantinib.
Repaglinide The metabolism of Repaglinide can be decreased when combined with Cabozantinib.
Almotriptan The metabolism of Almotriptan can be decreased when combined with Cabozantinib.
Domperidone The metabolism of Domperidone can be decreased when combined with Cabozantinib.
Halofantrine The metabolism of Halofantrine can be decreased when combined with Cabozantinib.
Lapatinib The metabolism of Lapatinib can be decreased when combined with Cabozantinib.
Sitagliptin The metabolism of Sitagliptin can be decreased when combined with Cabozantinib.
Odanacatib The metabolism of Odanacatib can be decreased when combined with Cabozantinib.
Capravirine The metabolism of Capravirine can be decreased when combined with Cabozantinib.
Perospirone The metabolism of Perospirone can be decreased when combined with Cabozantinib.
Riociguat The metabolism of Riociguat can be decreased when combined with Cabozantinib.
Dasabuvir The metabolism of Dasabuvir can be decreased when combined with Cabozantinib.
Netoglitazone The metabolism of Netoglitazone can be decreased when combined with Cabozantinib.
Rivoglitazone The metabolism of Rivoglitazone can be decreased when combined with Cabozantinib.
Ciglitazone The metabolism of Ciglitazone can be decreased when combined with Cabozantinib.
Selexipag The metabolism of Selexipag can be decreased when combined with Cabozantinib.
Velpatasvir The metabolism of Velpatasvir can be decreased when combined with Cabozantinib.
Glasdegib The metabolism of Glasdegib can be decreased when combined with Cabozantinib.
Voxilaprevir The metabolism of Voxilaprevir can be decreased when combined with Cabozantinib.
Balaglitazone The metabolism of Balaglitazone can be decreased when combined with Cabozantinib.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Cabozantinib.
Pioglitazone The metabolism of Pioglitazone can be decreased when combined with Cabozantinib.
Ozanimod The metabolism of Ozanimod can be decreased when combined with Cabozantinib.
Apomorphine The metabolism of Apomorphine can be decreased when combined with Cabozantinib.
Hydroxychloroquine The metabolism of Hydroxychloroquine can be decreased when combined with Cabozantinib.
Cisapride The metabolism of Cisapride can be decreased when combined with Cabozantinib.
Finerenone The metabolism of Finerenone can be decreased when combined with Cabozantinib.
Phenprocoumon The metabolism of Phenprocoumon can be decreased when combined with Cabozantinib.
Paclitaxel The metabolism of Paclitaxel can be decreased when combined with Cabozantinib.
Dabrafenib The serum concentration of Cabozantinib can be decreased when it is combined with Dabrafenib.
Sorafenib The metabolism of Sorafenib can be decreased when combined with Cabozantinib.
Tegafur The metabolism of Tegafur can be decreased when combined with Cabozantinib.
Enasidenib The metabolism of Enasidenib can be decreased when combined with Cabozantinib.
Erlotinib The metabolism of Erlotinib can be decreased when combined with Cabozantinib.
Pazopanib The metabolism of Pazopanib can be decreased when combined with Cabozantinib.
Cabazitaxel The metabolism of Cabazitaxel can be decreased when combined with Cabozantinib.
Ponatinib The metabolism of Ponatinib can be decreased when combined with Cabozantinib.
Brigatinib The metabolism of Brigatinib can be decreased when combined with Cabozantinib.
Propacetamol The serum concentration of Propacetamol can be increased when it is combined with Cabozantinib.
Troglitazone The metabolism of Cabozantinib can be decreased when combined with Troglitazone.
Fluoxetine The metabolism of Cabozantinib can be decreased when combined with Fluoxetine.
Imatinib The metabolism of Cabozantinib can be decreased when combined with Imatinib.
Medical Cannabis The metabolism of Cabozantinib can be decreased when combined with Medical Cannabis.
Capecitabine The serum concentration of Cabozantinib can be increased when it is combined with Capecitabine.
Mephenytoin The metabolism of Mephenytoin can be decreased when combined with Cabozantinib.
Piroxicam The metabolism of Piroxicam can be decreased when combined with Cabozantinib.
Naproxen The metabolism of Naproxen can be decreased when combined with Cabozantinib.
Propofol The metabolism of Propofol can be decreased when combined with Cabozantinib.
Tolbutamide The metabolism of Tolbutamide can be decreased when combined with Cabozantinib.
Licofelone The metabolism of Licofelone can be decreased when combined with Cabozantinib.
Olodaterol The metabolism of Olodaterol can be decreased when combined with Cabozantinib.
Bosentan The metabolism of Cabozantinib can be increased when combined with Bosentan.
Valsartan The metabolism of Cabozantinib can be decreased when combined with Valsartan.
Torasemide The metabolism of Cabozantinib can be decreased when combined with Torasemide.
Progesterone The metabolism of Cabozantinib can be decreased when combined with Progesterone.
Zafirlukast The metabolism of Cabozantinib can be decreased when combined with Zafirlukast.
Tamoxifen The metabolism of Cabozantinib can be decreased when combined with Tamoxifen.
Clopidogrel The metabolism of Cabozantinib can be decreased when combined with Clopidogrel.
Phenylbutazone The metabolism of Cabozantinib can be decreased when combined with Phenylbutazone.
Sulfamethoxazole The metabolism of Cabozantinib can be decreased when combined with Sulfamethoxazole.
Glyburide The metabolism of Cabozantinib can be decreased when combined with Glyburide.
Fluvastatin The metabolism of Cabozantinib can be decreased when combined with Fluvastatin.
Leflunomide The metabolism of Cabozantinib can be decreased when combined with Leflunomide.
Sertraline The metabolism of Cabozantinib can be decreased when combined with Sertraline.
Etoricoxib The metabolism of Cabozantinib can be decreased when combined with Etoricoxib.
Doconexent The metabolism of Cabozantinib can be decreased when combined with Doconexent.
Estrone sulfate The metabolism of Cabozantinib can be decreased when combined with Estrone sulfate.
Sitaxentan The metabolism of Cabozantinib can be decreased when combined with Sitaxentan.
Triclabendazole The metabolism of Cabozantinib can be decreased when combined with Triclabendazole.
Candesartan The metabolism of Cabozantinib can be decreased when combined with Candesartan.
Glimepiride The metabolism of Cabozantinib can be decreased when combined with Glimepiride.
Indomethacin The metabolism of Cabozantinib can be decreased when combined with Indomethacin.
Treprostinil The metabolism of Treprostinil can be decreased when combined with Cabozantinib.
Acetohexamide The metabolism of Cabozantinib can be decreased when combined with Acetohexamide.
Nabumetone The metabolism of Cabozantinib can be decreased when combined with Nabumetone.
Tenoxicam The metabolism of Cabozantinib can be decreased when combined with Tenoxicam.
Chlorpropamide The metabolism of Cabozantinib can be decreased when combined with Chlorpropamide.
Flurbiprofen The metabolism of Cabozantinib can be decreased when combined with Flurbiprofen.
Etodolac The metabolism of Cabozantinib can be decreased when combined with Etodolac.
Candesartan cilexetil The metabolism of Cabozantinib can be decreased when combined with Candesartan cilexetil.
Tolazamide The metabolism of Cabozantinib can be decreased when combined with Tolazamide.
Salicylic acid The metabolism of Cabozantinib can be decreased when combined with Salicylic acid.
Acetylsalicylic acid The metabolism of Cabozantinib can be decreased when combined with Acetylsalicylic acid.
Formoterol The metabolism of Cabozantinib can be decreased when combined with Formoterol.
Thalidomide The metabolism of Cabozantinib can be decreased when combined with Thalidomide.

Target Protein

Hepatocyte growth factor receptor MET
Vascular endothelial growth factor receptor 2 KDR
Proto-oncogene tyrosine-protein kinase receptor Ret RET

Referensi & Sumber

Artikel (PubMed)
  • PMID: 21314233
    Durante C, Russo D, Verrienti A, Filetti S: XL184 (cabozantinib) for medullary thyroid carcinoma. Expert Opin Investig Drugs. 2011 Mar;20(3):407-413. doi: 10.1517/13543784.2011.559163.
  • PMID: 26406150
    Choueiri TK, Escudier B, Powles T, Mainwaring PN, Rini BI, Donskov F, Hammers H, Hutson TE, Lee JL, Peltola K, Roth BJ, Bjarnason GA, Geczi L, Keam B, Maroto P, Heng DY, Schmidinger M, Kantoff PW, Borgman-Hagey A, Hessel C, Scheffold C, Schwab GM, Tannir NM, Motzer RJ: Cabozantinib versus Everolimus in Advanced Renal-Cell Carcinoma. N Engl J Med. 2015 Nov 5;373(19):1814-23. doi: 10.1056/NEJMoa1510016. Epub 2015 Sep 25.
  • PMID: 26536165
    Krajewska J, Olczyk T, Jarzab B: Cabozantinib for the treatment of progressive metastatic medullary thyroid cancer. Expert Rev Clin Pharmacol. 2016;9(1):69-79. doi: 10.1586/17512433.2016.1102052. Epub 2015 Nov 4.
  • PMID: 24756794
    Grullich C: Cabozantinib: a MET, RET, and VEGFR2 tyrosine kinase inhibitor. Recent Results Cancer Res. 2014;201:207-14. doi: 10.1007/978-3-642-54490-3_12.
  • PMID: 27835047
    Escudier B, Lougheed JC, Albiges L: Cabozantinib for the treatment of renal cell carcinoma. Expert Opin Pharmacother. 2016 Dec;17(18):2499-2504. doi: 10.1080/14656566.2016.1258059. Epub 2016 Nov 22.

Contoh Produk & Brand

Produk: 22 • International brands: 0
Produk
  • Cabometyx
    Tablet • 60 mg/1 • Oral • US • Approved
  • Cabometyx
    Tablet • 40 mg/1 • Oral • US • Approved
  • Cabometyx
    Tablet • 20 mg/1 • Oral • US • Approved
  • Cabometyx
    Tablet • 20 mg • Oral • Canada • Approved
  • Cabometyx
    Tablet • 40 mg • Oral • Canada • Approved
  • Cabometyx
    Tablet • 60 mg • Oral • Canada • Approved
  • Cabometyx
    Tablet, film coated • 20 mg • Oral • EU • Approved
  • Cabometyx
    Tablet, film coated • 40 mg • Oral • EU • Approved
Menampilkan 8 dari 22 produk.

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