Cabozantinib - A Descriptive Overview

Overview

The drug Cabozantinib inhibits receptors involved in cancer development. The drug is available as a tablet that should be administered orally once a day. Patients have been informed of the various precautions to take when administering this drug. Cabozantinib was approved by the FDA (Food and Drug Administration) in 2012.

On March 26, 2025, the drug was approved for adults and children 12 years of age and older with previously treated, unresectable, locally advanced, or metastatic well-differentiated pancreatic neuroendocrine tumors (pNET) and well-differentiated extra-pancreatic neuroendocrine tumors (epNET).

How Does Cabozantinib Work?

Cabozantinib works by inhibiting certain tyrosine kinase receptors (enzymes) that, in turn, inhibit the growth and development of cancer-producing cells, thereby decreasing the intensity of cancer cell growth.

What Are the Available Doses and Dosage Forms?

Cabozantinib is available in tablets of 20 milligrams (mg), 40 mg, and 60 mg.

• A 60-milligram tablet is administered orally, once daily, without food.

• A 40-milligram tablet is administered orally once daily without food, in combination with Nivolumab (240 milligrams every 2 weeks, with 30-minute intravenous infusions).

The tablets are available in the following shapes and colors.

• 30 oval-shaped yellow film tablets containing 60 mg of Cabozantinib are in one bottle.

• 40-milligram tablets of Cabozantinib are triangle-shaped and yellow film-coated.

• 20-milligram yellow-filmed Cabozantinib tablets, round in shape, are available in bottles of 30 tablets.

Warnings and Precautions:

• Hemorrhage - Internal bleeding due to a ruptured vessel is called hemorrhage. Under such circumstances, Cabozantinib should not be administered.

• Fistulas and Perforations - Any abnormal connection between two organs, or the organ and the external surface of the body, should be checked before Cabozantinib.

• Hypertension - Increased blood pressure is a common condition that can be caused by lifestyle factors. Blood pressure is monitored in every patient, and Cabozantinib is discontinued if blood pressure is elevated.

• Diarrhea - Increased bowel movements cause diarrhea. Stop Cabozantinib immediately if severe diarrhea occurs.

• Proteinuria - If protein in urine is detected, then Cabozantinib is discontinued.

• Impaired Wound Healing - Cabozantinib is withheld for at least three weeks before any surgery.

For Patients:

Important Things to Tell the Doctor Before Taking Cabozantinib

Inform your doctor if you have:

• High blood pressure.

• Bleeding problems.

• Recent surgery or dental treatment.

• Ulcerative colitis or Crohn’s disease.

• History of heart attack, stroke, or blood clots.

• Kidney, liver, or thyroid problems.

Common Side Effects of Cabozantinib

• Tiredness.

• Nausea or vomiting.

• Diarrhea.

• Weight loss.

• Constipation.

• Mouth sores.

• Skin rashes.

• High blood pressure.

Serious Side Effects (Need Medical Attention)

• Severe bleeding.

• Severe abdominal pain.

• Chest pain or stroke symptoms.

• Severe headache or confusion.

• Yellowing of eyes or skin (liver problem).

• Swelling of legs or feet (kidney problem).

• Jaw pain or mouth sores.

• Delayed wound healing.

How to Take Cabozantinib

• Take the medicine exactly as prescribed.

• Usually taken once daily.

• Do not eat food 2 hours before and 1 hour after taking the tablet.

• Swallow the tablet whole with water.

• Do not crush the tablet.

Missed Dose

• If more than 12 hours are left, take the missed dose.

• If less than 12 hours are left, skip the missed dose.

• Never take two doses together.

Can Cabozantinib Be Stopped?

Do not stop the medicine without your doctor’s advice.

Overdose Warning

Taking too much Cabozantinib can cause confusion, memory problems, and weakness. Seek medical help immediately.

Storage Instructions

• Store at room temperature.

• Keep away from children.

• Protect from sunlight.

Important Advice

Do not take Cabozantinib without a doctor’s prescription. Self-medication can be dangerous.

For Doctors:

What Is Clinical Pharmacology?

Mechanism of Action:

The tyrosine kinase activity of certain receptors, such as MET, AXLL, RET, MER, KIT, TRKB, and TIE-2, is inhibited by Cabozantinib. These tyrosine kinase receptors are responsible for both normal cellular functioning and pathological processes, including tumor angiogenesis, metastasis, oncogenesis, maintenance of the tumor microenvironment, and drug resistance.

Pharmacodynamics:

The response to the concentration of the drug-exposed or the safety relationship has not been established. In patients with medullary thyroid cancer, cabozantinib increased the QTc interval by 10 to 15 ms four weeks after administration. A definitive relationship between QTc and drug concentration cannot be established. Changes in the waveform morphology of the heart or new rhythms are not observed. All the studies were done through cardiac electrophysiology.

Pharmacokinetics:

A daily administration of a normal dosage of Cabozantinib formulation, twenty times, resulted in the accumulation of the drug five times more than the administration of a single dose.

Absorption:

The maximum concentration of Cabozantinib was found at its peak time, three to four hours after the dose. A nearly 20% increase in concentration was observed with the Cabozantinib single-dose 140-milligram capsule formulation.

Nonclinical Toxicology:

• Carcinogenesis, mutagenesis, and impairment of fertility can occur due to toxicity.

• Cabozantinib's carcinogenic potential is under evaluation, and it is effective in reproductive tract tissues.

• Male and female fertility is impaired with the treatment of Cabozantinib.

• Impairment is indicated by reduced sperm counts and increased weight of the reproductive organ.

• Loss of pre- and post-implantation embryos is seen most commonly in females.

What Are the Drug Interactions of Cabozantinib?

• Using a strong CYP3A4 inhibitor with Cabozantinib increased drug exposure. The increase in exposure causes increased risk of exposure-related toxicity.

  • Management can be achieved by avoiding CYP3A4 inhibitors or, when that is not possible, reducing the drug dosage.

• Cabozantinib exposure is decreased when it is used with CYP3A4 inducers compared with when it is administered alone. A decrease in drug exposure can lead to reduced efficacy.

  • Prevention or management can be done by increasing the drug dosage when CYP3A4 inducers cannot be avoided.

Use in Specific Populations:

• Pregnancy: Cabozantinib can cause harm to the fetus when administered to pregnant women. There is no associated risk with the drug. This medicine can be harmful to an unborn baby. Doctors must explain this risk clearly to the patient. Studies show that there is about a 5% risk of birth defects or miscarriage in pregnant women who use this drug. Research on this risk is still ongoing.

• Breastfeeding (Lactation): This medicine is not found in human breast milk. There are no known harmful effects on a breastfed baby. However, this drug can cause serious side effects. Because of this, women should not breastfeed while taking Cabozantinib. Breastfeeding should also be avoided for at least four months after the last dose.

• Contraception: This drug can harm a fetus if taken during pregnancy. Women who can become pregnant should use effective birth control while taking Cabozantinib to prevent pregnancy.

• Infertility: This medicine may affect the ability to have children. It can change fertility in both men and women who are of childbearing age.

• Use in Children (Pediatric Use): The safety and effectiveness of this drug in children are still being studied. It may cause problems with bone growth, teeth development, and bone strength. Some bone problems may improve after stopping the drug. However, damage to the kidneys and reproductive organs may last even after treatment ends.

• Geriatric Use: Around 50 percent of the population aged 65 years or older received this medication. Adverse reactions were common, and no differences were observed between younger and older patients.

• Hepatic Impairment: Cabozantinib exposure has been associated with serious adverse reactions in cases of mild to moderate hepatic impairment.