Cabozantinib
Generic Details
Generic Name
Cabozantinib
Other Names
- Cometriq
Drug Class
- Tyrosine kinase inhibitor
Chemical Formula
C28H24FN3O5
Molecular Weight
501.51 g/mol
Mechanism of Action
- Inhibits multiple receptor tyrosine kinases including MET, VEGFR2, AXL
Indications
- Treatment of medullary thyroid cancer
- Treatment of renal cell carcinoma
- Treatment of hepatocellular carcinoma
Common Dosage Forms
- Tablet
Typical Dosage
- 60 mg once daily on an empty stomach
- Dose may be adjusted based on individual tolerability
Pediatric Dosage
- Safety and efficacy not established in children
Geriatric Dosage
- Dosing adjustments may be required in elderly patients
Side Effects
- Fatigue
- Diarrhea
- Nausea
- Decreased appetite
- Hypertension
- Hand-foot skin reaction
- Proteinuria
Contraindications
- Hypersensitivity to cabozantinib
- Severe hepatic impairment
Pregnancy Category
- D - Positive evidence of risk
Lactation Safety
- Not recommended during breastfeeding
Drug Interactions
- Strong CYP3A4 inhibitors may increase cabozantinib levels
- Strong CYP3A4 inducers may decrease cabozantinib levels
Overdose Symptoms
- Hemorrhage
- Hypertension
- Mucositis
Antidote for Overdose
- No specific antidote, manage symptoms and provide supportive care
Storage Conditions
- Store at room temperature (20-25°C)
Pharmacokinetics
- Absorption: Well absorbed with peak plasma concentrations reached in 2-3 hours
- Distribution: Highly protein-bound and extensively distributed
- Metabolism: Mainly hepatic via CYP3A4
- Excretion: Primarily fecal elimination
Precautions
- Monitor blood pressure regularly
- Monitor for signs of hemorrhage
- Monitor liver function tests
Warnings
- Risk of perforations and fistulas
- Hypertension may occur
- Cardiac complications have been reported
Others
- Cabozantinib may cause reversible posterior leukoencephalopathy syndrome (RPLS)
- Patients should be advised on the risk of bleeding