Home Drug Guide Cabozantinib S-malate

Drug Guide

Generic Name

Cabozantinib S-malate

Brand Names Cometriq, Cabometyx

Classification

Therapeutic: Antineoplastic agent

Pharmacological: Tyrosine kinase inhibitor

FDA Approved Indications

Medullary thyroid carcinoma, unresectable or metastatic
Renal cell carcinoma, advanced
Hepatocellular carcinoma, hepatocellular carcinoma (HCC)

Mechanism of Action

Cabozantinib inhibits multiple tyrosine kinases including VEGFR, MET, and AXL, which are involved in tumor growth, angiogenesis, and metastasis.

Dosage and Administration

Adult: The dose varies depending on the indication, but generally 60 mg orally once daily. Adjustments may be needed based on tolerance and side effects.

Pediatric: Safety and efficacy not established.

Geriatric: Use with caution due to potential increased sensitivity; consider dose adjustments.

Renal Impairment: Adjust dose based on severity of renal impairment.

Hepatic Impairment: Use is contraindicated in severe hepatic impairment; in mild to moderate impairment, consider dose adjustments.

Pharmacokinetics

Absorption: Bioavailability approximately 37%.

Distribution: Widely distributed in tissues; high plasma protein binding (~99%).

Metabolism: Metabolized primarily via CYP3A4; also undergoes glucuronidation.

Excretion: Excreted mainly in feces (~74%) and urine (~16%).

Half Life: Approximately 56 hours.

Contraindications

Hypersensitivity to cabozantinib or any component of the formulation

Precautions

Risk of bleeding, hypertension, gastrointestinal perforation or fistula, hepatic impairment, wound healing complications. Use in pregnancy and lactation not recommended.

Adverse Reactions - Common

Diarrhea (Common)
Fatigue (Common)
Elevated blood pressure (Common)
Nausea (Common)
Mucositis/stomatitis (Common)

Adverse Reactions - Serious

Hemorrhage (Serious)
Wound healing complications (Serious)
Hepatotoxicity (Serious)
Gastrointestinal perforation (Serious)
Hypertension, severe (Serious)

Drug-Drug Interactions

CYP3A4 inhibitors or inducers may alter levels of cabozantinib.
Anticoagulants—risk of bleeding.

Drug-Food Interactions

High-fat meals may increase absorption; consistent intake recommended.

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Monitor blood pressure, liver function tests, signs of bleeding, wound healing status, and gastrointestinal symptoms.

Diagnoses:

Risk for bleeding
Impaired tissue integrity
Risk for hypertension

Implementation: Administer with or without food; monitor for adverse effects; educate patient on signs of complications.

Evaluation: Regularly assess for side effects, therapeutic response, and adverse reactions.

Patient/Family Teaching

Report signs of bleeding, severe hypertension, wound issues, or gastrointestinal symptoms.
Avoid pregnancy; use contraception during treatment and for at least 4 weeks after discontinuation.
Monitor blood pressure regularly and maintain follow-up appointments.

Special Considerations

Black Box Warnings:

Wound healing complications, hemorrhage, gastrointestinal perforation, hepatotoxicity, QT interval prolongation.

Genetic Factors: Pharmacogenetic testing not routinely required.

Lab Test Interference: May alter laboratory results related to bleeding and liver function.

Overdose Management

Signs/Symptoms: Severe bleeding, hypertension, diarrhea, fatigue, mucositis.

Treatment: Supportive care; no specific antidote. Discontinue drug and provide symptomatic treatment as needed.

Storage and Handling

Storage: Store at room temperature, 20-25°C (68-77°F).

Stability: Stable under recommended conditions until expiration date.