Cabometyx, Cometriq
Generic Name
Cabozantinib
Manufacturer
Exelixis, Inc.
Country
USA
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Description
Overview of the medicine
Cabozantinib is an orally bioavailable small molecule inhibitor of receptor tyrosine kinases, including MET, VEGFR2, and RET. It is used in the treatment of various advanced cancers.
Uses & Indications
Dosage
Adults
For Renal Cell Carcinoma, Hepatocellular Carcinoma, and Differentiated Thyroid Cancer: 60 mg orally once daily. For Medullary Thyroid Carcinoma: 140 mg (as Cometriq) orally once daily. Dosage adjustments may be necessary based on tolerability and specific brand/indication.
Elderly
No specific dose adjustment is required, but close monitoring for adverse reactions is recommended.
Renal_impairment
No dose adjustment is required for mild to moderate renal impairment. Data for severe renal impairment is limited; use with caution.
How to Take
Cabozantinib tablets should be taken orally once daily, on an empty stomach. Do not eat for at least 2 hours before and for at least 1 hour after taking cabozantinib. Swallow tablets whole; do not crush, chew, or split.
Mechanism of Action
Cabozantinib inhibits the activity of multiple receptor tyrosine kinases (RTKs) that are involved in tumor growth, angiogenesis, and metastasis. Key targets include MET, VEGFR2, RET, AXL, KIT, FLT3, and TIE-2.
Pharmacokinetics
Onset
Clinical effects typically observed within weeks to months, depending on the indication.
Excretion
Primarily eliminated via feces (approx. 80%), with a smaller portion via urine (approx. 10%).
Half life
Approximately 99 hours (around 4 days).
Absorption
Slowly absorbed, peak plasma concentrations occur 2-4 hours post-dose. Bioavailability is approximately 80%.
Metabolism
Primarily hepatic, mainly by CYP3A4, with minor contributions from CYP2C8 and CYP2C9.
Side Effects
Contraindications
- •Hypersensitivity to cabozantinib or any component of the formulation.
- •Severe bleeding or gastrointestinal perforation within the last 6 months.
Drug Interactions
Strong CYP3A4 inducers (e.g., rifampin, phenytoin)
May decrease cabozantinib exposure; increase cabozantinib dose.
Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin)
May increase cabozantinib exposure; reduce cabozantinib dose.
Proton Pump Inhibitors (PPIs), H2-receptor antagonists, antacids
May reduce cabozantinib absorption due to altered gastric pH; co-administration should be avoided or managed with caution.
Storage
Store at room temperature (20-25°C or 68-77°F); excursions permitted to 15-30°C (59-86°F). Keep in the original container to protect from moisture. Keep out of reach of children.
Overdose
There is no specific antidote for cabozantinib overdose. In case of an overdose, discontinue cabozantinib and initiate general supportive measures. Closely monitor for signs and symptoms of toxicity.
Pregnancy & Lactation
Pregnancy Category D. Cabozantinib can cause fetal harm. Advise females of reproductive potential to use effective contraception during treatment and for at least 4 months after the last dose. It is unknown if cabozantinib or its metabolites are present in human milk; due to the potential for serious adverse reactions in breastfed infants, advise women not to breastfeed during treatment and for at least 4 months after the last dose.
Frequently Asked Questions
Common questions about this medicine
Pack Sizes
Shelf Life
Typically 24-36 months from the date of manufacture, check product specific labeling.
Availability
Available in specialized pharmacies and hospital oncology units
Approval Status
FDA approved
Patent Status
Patented
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Global Brand Names
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