Cabozantinib

Cabozantinib Introduction

Cabozantinib is an oral tyrosine kinase inhibitor. It is approved by the US Food and Drug Administration (FDA) for the treatment of advanced renal cell carcinoma (kidney cancer). The drug is manufactured by Exelixis and is marketed as Cabometyx.

Uses For

Cabozantinib is used to treat advanced renal cell carcinoma (kidney cancer). It is also being studied in the treatment of other types of cancer.

Mechanism Of Action

Cabozantinib works by inhibiting certain tyrosine kinases that are the drivers of cancer. By blocking these proteins, cabozantinib is able to interfere with cancer cell growth, which leads to tumor shrinkage and slowed disease progression.

How Long Does It Take To Work?

The effects of cabozantinib can be seen within the first few weeks of treatment. In clinical trials, the first response was seen within 6-12 weeks. The full effects of the treatment might take up to 12 weeks to be seen.

Absorption

Cabozantinib is rapidly and extensively absorbed after oral administration. The peak plasma concentrations of the drug are achieved within 1-2 hours after administration.

Route Of Elimination

Cabozantinib is eliminated primarily through metabolism by the cytochrome P450 (CYP3A4) system. Approximately 80% of the drug is eliminated via metabolism, and the rest is eliminated through the renal system.

Dosage

Recommended Dosage for Renal Cell Carcinoma: The recommended dosage of Cabozantinib is 60 mg once daily without food until the patient no longer experiences clinical benefit or experiences unacceptable toxicity.

Recommended Dosage for Hepatocellular Carcinoma: The recommended dosage of Cabozantinib is 60 mg once daily without food until disease progression or unacceptable toxicity. Or, as directed by the registered physicians.

• Stop treatment with Cabozantinib at least 28 days prior to scheduled surgery, including dental surgery.
• Do not substitute Cabozantinib tablets with Cabozantinib capsules.
• Do not administer Cabozantinib with food. Administer at least 1 hour before or at least 2 hours after eating.
• Swallow Cabozantinib tablets whole. Do not crush Cabozantinib tablets.
• Do not take a missed dose within 12 hours of the next dose.
• Modify the dose for certain patients with hepatic impairment and for patients taking drugs known to strongly induce or inhibit CYP450.

Pediatric Use: The safety and effectiveness of Cabozantinib in pediatric patients have not been established.

The recommended dosage of Cabozantinib is 60 mg orally once a day until disease progression or unacceptable toxicity.

Administration

Cabozantinib should be taken orally with food. Patients should take the drug at the same time each day to reduce the risk of missed doses.

Side Effect

The most common side effects of Cabozantinib are fatigue, diarrhea, mouth sores, nausea, loss of appetite, constipation, vomiting, abdominal pain and rash. Other side effects include hair loss, weight loss, joint pain, headache, dizziness, difficulty breathing, and anemia.

Toxicity

Cabozantinib has been associated with Grade 3/4 adverse reactions such as hypertension, neutropenia, diarrhea, fatigue, and thrombocytopenia. Close monitoring of blood and vital signs is recommended for the management of these reactions.

Precaution

Patients should not take cabozantinib if they are pregnant or breastfeeding. Patients should also avoid taking cabozantinib if they have hepatic or renal impairment, or if they are taking strong CYP3A4 inhibitors. Cabozantinib should be used with caution in patients with cardiovascular disease and hypertension.

Interaction

Cabozantinib can interact with medications such as strong CYP3A4 inhibitors, CYP3A4 inducers, and oral anticoagulants. Patients should inform their healthcare provider of any medications they are taking before starting cabozantinib therapy.

Disease Interaction

There are no known disease interactions with cabozantinib. However, it is always important to discuss any existing medical conditions with a doctor before taking any new medication.

Drug Interaction

Cabozantinib can interact with medications such as strong CYP3A4 inhibitors, CYP3A4 inducers, and oral anticoagulants. Patients should inform their healthcare provider of any medications they are taking before starting cabozantinib therapy.

Food Interactions

Cabozantinib should be taken with food when administered orally. High fat meals may increase the amount of the drug in your system and increase the risk of side effects.

Pregnancy Use

Cabozantinib should not be used during pregnancy. Women should use effective birth control methods while taking cabozantinib and should not breastfeed while taking the medication.

Lactation Use

Cabozantinib should not be used during lactation. Women should not breastfeed while taking cabozantinib.

Acute Overdose

The clinical symptoms of an overdose of cabozantinib are not known. In case of an overdose, supportive care should be provided as needed. Cabozantinib is not dialyzable.

Contraindication

Cabozantinib is contraindicated in patients with a known hypersensitivity or serious adverse reaction to cabozantinib, or any of its components.

Use Direction

Cabozantinib should be taken orally with food. It should be taken at the same time each day to reduce the risk of missing doses. The drug should not be chewed or crushed, and should be swallowed whole.

Storage Condition

Cabozantinib should be stored at room temperature (20-25°C). It should be kept away from light and heat, and should not be exposed to moisture.

Volume Of Distribution

The volume of distribution for cabozantinib is estimated to be 39L.

Half Life

The half life of cabozantinib is about 5 hours.

Clearance

The clearance of cabozantinib is estimated to be 31L/h/kg.

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Some Frequently Asked Questions About Cabozantinib