Indications
Renal Cell Carcinoma Cabozantinib is used to treat patients with advanced renal cell carcinoma (RCC). Hepatocellular Carcinoma Cabozantinib is also used for patients with hepatocellular carcinoma (HCC) who have already been treated with Sorafenib.
⚠️ Always consult a registered physician before taking any medicine.
Pharmacology
Cabozantinib blocks the tyrosine kinase activity of MET, VEGFR-1, -2 and -3, AXL, RET, ROS1, TYRO3, MER, KIT, TRKB, FLT-3 and TIE-2, according to in vitro biochemical and/or cellular assays. These receptor tyrosine kinases take part in normal cell function, and also in disease processes such as oncogenesis, metastasis, tumor angiogenesis, drug resistance and maintenance of the tumor microenvironment.
Absorption: The median time to peak cabozantinib concentrations (Tmax) ranged from 3 to 4 hours after the dose. After a single 140 mg dose, the Cmax of Cabozantinib was 19% higher than with a Cabozantinib capsule formulation. The AUC differed by less than 10% between the two.
Distribution: The oral volume of distribution (Vz/F) of Cabozantinib is approximately 319 L. Cabozantinib is highly protein-bound in human plasma (≥99.7%).
Elimination: The predicted terminal half-life is approximately 99 hours, and clearance (CL/F) at steady state is estimated to be 2.2 L/hr.
Metabolism: In vitro, Cabozantinib is a substrate of CYP3A4.
Excretion: Healthy subjects were given a single dose of radiolabeled 14 C-Cabozantinib, and approximately 81% of the total administered radioactivity was recovered within a 48-day collection period. About 54% was found in feces and 27% in urine. Unchanged Cabozantinib made up 43% of the total radioactivity in feces, and it could not be detected in urine over a 72-hour collection.
Pregnancy & Breastfeeding
Pregnancy: Cabozantinib can harm an unborn baby if a pregnant woman takes it. There are no data in pregnant women that could show what the exact risk is.
Breastfeeding: Nobody knows whether Cabozantinib or its metabolites pass into human milk, or what they might do to a breastfed child or to milk production. Because serious side effects in a breastfed child are possible, women should be advised not to breastfeed while on Cabozantinib and for 4 months after the final dose.
Contraception: As Cabozantinib can cause fetal harm when given to a pregnant woman, females of reproductive potential should be advised to use effective contraception during treatment and for 4 months after the final dose.
Infertility: Animal findings suggest that Cabozantinib may impair fertility in both females and males of reproductive potential.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Dosage Reference
⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.
Side Effects & Interactions
Side Effects
No side-effect data recorded yet.