Cometriq, Cabometyx
Generic Name
Cabozantinib
Manufacturer
Exelixis, Ipsen
Country
USA (originator)
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Description
Overview of the medicine
Cabozantinib is an orally bioavailable small molecule that inhibits the activity of multiple receptor tyrosine kinases (RTKs), including MET, VEGFR2, AXL, and RET. It is used in the treatment of various cancers, including medullary thyroid cancer, renal cell carcinoma, and hepatocellular carcinoma.
Uses & Indications
Dosage
Adults
For MTC and HCC: 60 mg orally once daily. For RCC and DTC: 40 mg orally once daily. Doses should be adjusted based on tolerability.
Elderly
No specific dose adjustment is required based on age, but caution is advised due to potential for increased adverse reactions.
Renal_impairment
No dose adjustment needed for mild to moderate renal impairment. Data limited for severe impairment.
How to Take
Take orally on an empty stomach (at least 1 hour before or 2 hours after a meal). Do not crush or chew tablets.
Mechanism of Action
Cabozantinib inhibits the tyrosine kinase activity of MET, VEGFR2, AXL, and RET. These kinases are involved in tumor growth, angiogenesis, and metastasis. By inhibiting these targets, Cabozantinib reduces tumor cell proliferation and survival, and decreases angiogenesis.
Pharmacokinetics
Onset
Clinical effects usually observed within weeks of treatment initiation.
Excretion
Primarily excreted in feces (approximately 81%), with a minor portion excreted in urine (approximately 8%).
Half life
Approximately 55-90 hours (range).
Absorption
Peak plasma concentrations are achieved 2-4 hours after oral administration. Absorption is decreased when taken with food.
Metabolism
Primarily metabolized by CYP3A4. Minor metabolism by CYP2C8.
Side Effects
Contraindications
- Severe hypersensitivity to Cabozantinib or any excipients.
Drug Interactions
P-gp inhibitors (e.g., cyclosporine)
May increase Cabozantinib exposure.
Strong CYP3A4 inducers (e.g., rifampicin, phenytoin)
Decrease Cabozantinib exposure; dose increase may be needed.
Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin)
Increase Cabozantinib exposure; dose reduction may be needed.
Storage
Store at room temperature (20°C to 25°C), away from moisture and heat. Keep out of reach of children.
Overdose
There is no specific antidote for Cabozantinib overdose. In case of overdose, supportive treatment should be initiated, and the patient should be closely monitored.
Pregnancy & Lactation
Cabozantinib can cause fetal harm. Pregnant women should not take it. 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 is excreted in human milk; 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 manufacturing date, check product label for specific expiry.
Availability
Globally available in specialized pharmacies
Approval Status
FDA/EMA Approved
Patent Status
Patented, with market exclusivity
Clinical Trials
Cabozantinib has been extensively studied in several pivotal clinical trials, including the EXAM study (MTC), METEOR and CABOSUN studies (RCC), and CELESTIAL study (HCC), demonstrating significant improvements in progression-free and overall survival.
Lab Monitoring
- Blood pressure monitoring
- Complete Blood Count (CBC) with differential
- Thyroid function tests
- Liver function tests (ALT, AST, bilirubin)
- Serum electrolytes (calcium, potassium, magnesium)
- Urine protein (urinalysis)
Doctor Notes
- Monitor blood pressure and proteinuria regularly.
- Manage side effects proactively with dose modifications or supportive care.
- Counsel patients on potential severe bleeding and GI perforation risks.
Patient Guidelines
- Take the medicine exactly as prescribed by your doctor.
- Do not eat for at least 1 hour before and 2 hours after taking Cabozantinib.
- Report any severe side effects immediately to your doctor, especially unusual bleeding, severe abdominal pain, or swelling/pain in hands/feet.
Missed Dose Advice
If a dose is missed, take it as soon as you remember. If it is less than 12 hours until the next dose, skip the missed dose and continue with the regular schedule. Do not take two doses to make up for a missed one.
Driving Precautions
Cabozantinib may cause fatigue, dizziness, or vision disturbances, which could impair your ability to drive or operate machinery. Exercise caution until you know how the medicine affects you.
Lifestyle Advice
- Maintain good hydration, especially if experiencing diarrhea.
- Manage fatigue by pacing activities and ensuring adequate rest.
- Regularly moisturize hands and feet to prevent or reduce palmar-plantar erythrodysesthesia.
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