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Cabozantinib

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Molecule Summary

Uses
Kidney and Liver cancer
Therapy
Anti-Neoplastic
Side Effects
Diarrhoea, Hand-Foot Skin Reaction, Tiredness, High Blood Pressure
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NPPA
Regulated

Molecule Description

Cabozantinib is a prescription cancer medicine in the kinase inhibitor class. It works by blocking multiple proteins (including MET, VEGF receptors, and AXL) involved in tumour growth, blood-vessel formation, and cancer spread. This medicine is used in adults with advanced renal cell carcinoma (kidney cancer), either as a first treatment in patients with intermediate or poor risk disease, or after previous treatment with a VEGF-targeted therapy, and in adults with hepatocellular carcinoma (liver cancer) who have previously been treated with sorafenib. In both cancers, it is given alone. Cabozantinib is taken on an empty stomach, and treatment usually continues for as long as it benefits you and side effects remain manageable. Because many adverse reactions occur early in treatment, your doctor will monitor you closely during the first couple of months and may adjust your dose if needed.

Uses

  • Advanced renal cell carcinoma (kidney cancer): as a first treatment in patients with intermediate or poor risk disease, or after previous VEGF-targeted therapy.
  • Hepatocellular carcinoma (liver cancer): in patients previously treated with sorafenib.

Contraindications

When should one not use Cabozantinib

  • If you are allergic (hypersensitive) to cabozantinib or any other ingredient of Cabozantinib.

Side effects

Common side effects of this drug are:

  • Very common side effects:
  • Diarrhoea
  • Fatigue, weakness, and mucosal inflammation
  • Hand-foot syndrome (palmar-plantar erythrodysaesthesia), causing redness, pain, swelling, or blistering on the palms and soles
  • Nausea, vomiting, and mouth sores (stomatitis)
  • Constipation, indigestion, and abdominal pain
  • Decreased appetite and weight loss
  • High blood pressure (hypertension)
  • Bleeding (haemorrhage)
  • Low blood counts (anaemia, low platelets, )
  • Underactive thyroid (hypothyroidism)
  • Changes in taste (dysgeusia), headache, and dizziness
  • Hoarseness or voice changes (dysphonia), breathlessness, and cough
  • Skin rash
  • Raised liver enzymes (ALT/AST)
  • Pain in the arms or legs, and swelling of the hands or feet (peripheral oedema)
  • Other commonly reported side effects:
  • Dehydration
  • Muscle spasms and joint pain
  • Protein in the urine (proteinuria)
  • Dry mouth, oral pain, and difficulty swallowing
  • Itching, dry skin, hair colour change, and hair thinning
  • Blood clots in the veins (including the lungs)
  • Hepatic encephalopathy (confusion due to liver problems, seen in liver cancer patients)
  • Changes in blood sugar, calcium, sodium, or bilirubin on blood tests
  • Serious side effects requiring immediate medical attention:
  • Serious or life-threatening bleeding: contact your doctor immediately if you cough up blood, vomit blood or material that looks like coffee grounds, pass red or black tarry stools, or have unusually heavy bleeding of any kind.
  • A tear in the stomach or intestine (perforation) or an abnormal connection between organs (fistula): seek urgent care for new, severe, or persistent abdominal pain.
  • Blood clots, heart attack, or stroke: get emergency help for chest pain, sudden breathlessness, swelling or pain in a limb, sudden weakness or numbness, trouble speaking, or a sudden severe headache.
  • Hypertensive crisis: dangerously high blood pressure.
  • Osteonecrosis of the jaw: contact your doctor if you have jaw pain, toothache, loose teeth, or gum sores.
  • Reversible Posterior Leukoencephalopathy Syndrome (RPLS): a rare brain condition; seek urgent care for seizures, severe headache, confusion, or vision changes.
  • Hepatic encephalopathy in liver cancer patients: contact your doctor promptly for new confusion, drowsiness, or altered behaviour.

Precautions and Warnings

Pregnancy

Pregnancy

No. Cabozantinibshould not normally be used during pregnancy, as it may harm an unborn baby. Women and men who could have children should use effective contraception during treatment and for at least 4 months after the last dose. If oral contraceptive pills are used, an additional barrier method such as condoms is recommended.

Breast Feeding

Breast Feeding

Do not breastfeed during treatment or for at least 4 months after the last dose, as it is not known whether cabozantinib passes into breast milk and it may harm the baby. Talk to your doctor about safe feeding alternatives.

Driving

Driving

Cabozantinib may cause tiredness or weakness, which can affect your ability to drive or use machines. Avoid driving if you feel tired, weak, dizzy, or unwell.

Alcohol

Alcohol

There is no specific alcohol interaction established for Cabozantinib. However, alcohol may worsen tiredness, dizziness, dehydration, or stomach-related side effects. Ask your doctor whether alcohol is appropriate for you.

Other General Warnings

Other General Warnings

Talk to your doctor if
  • You have unusual or heavy bleeding, as Cabozantinib can cause serious bleeding.
  • You develop persistent or severe abdominal pain, which may be a sign of a hole (perforation) or abnormal connection (fistula) in the stomach or intestine.
  • You experience sudden chest pain, breathlessness, or swelling or pain in a limb, as these may signal a serious blood clot.
  • Your blood pressure is high or difficult to control; it should be well-controlled before starting and monitored throughout treatment.
  • You develop jaw pain, tooth pain, loose teeth, or gum sores, or you need any dental procedure, as Cabozantinib can cause jaw bone damage (osteonecrosis); a dental exam is advised before starting.
  • You are planning any surgery, including dental surgery, treatment should be stopped at least 4 weeks beforehand and restarted only once your doctor confirms the wound has healed adequately.
  • You develop seizures, severe headache, vision changes, or confusion, as these may be signs of a rare brain condition (RPLS).
  • You have liver cancer and notice new confusion, drowsiness, or personality changes, as this may be hepatic encephalopathy.
  • You feel unusually tired, gain weight, or feel cold often, as this medicine can affect thyroid function. Thyroid function will be checked before and during treatment.
  • You have heart problems or an abnormal heart rhythm, as your doctor may need to monitor your heart rhythm and blood electrolyte levels.
  • You have liver problems; your doctor may adjust your dose in moderate liver impairment, and Cabozantinib is not recommended in severe liver impairment. Liver function tests will be done before and during treatment.
  • You have kidney problems; the medicine is used with caution in mild-to-moderate kidney impairment and is not recommended in severe kidney impairment.
  • You are a man or woman planning to have children, as Cabozantinib may impair fertility in both sexes; ask about fertility preservation before starting.
  • Always take Cabozantinib on an empty stomach, at least 1 hour before or 2 hours after food, as food can affect how much of the medicine your body absorbs.
  • Never substitute the tablets with cabozantinib capsules; the two are not interchangeable.
  • Tell your doctor immediately about any unusual bleeding, such as coughing up blood, vomiting blood, or red or black tarry stools, as this medicine can cause serious bleeding.
  • Report painful redness, swelling, or blisters on your palms or soles at the first sign, as early management of hand-foot syndrome can stop it from worsening.
  • Have a dental check-up before starting, maintain good oral hygiene, and tell your dentist you are on this medicine, as it carries a risk of jawbone problems.
  • Monitor your blood pressure regularly, as high blood pressure is very common on this medicine and may need treatment.
  • Avoid grapefruit and St. John's Wort throughout your treatment.
  • Both men and women should use effective contraception (including a barrier method) during treatment and for at least 4 months after the last dose.
  • Stop Cabozantinib at least 4 weeks before any planned surgery or invasive dental procedure, but only under your doctor's instruction.
  • Keep out of reach of children and pets.

Mode of Action

How Does It Work?

Cabozantinib works by blocking multiple proteins called receptor tyrosine kinases, including MET, VEGF receptors, and AXL, which are involved in tumour growth and blood-vessel formation. By blocking several of these signalling pathways at once, Cabozantinib interferes with signals that support tumour growth and spread.

Interactions

Interactions with other medicines

  • Some medicines can affect how Cabozantinib works. Tell your doctor about all medicines, supplements, vitamins, and herbal products you take.
  • Strong CYP3A4 inhibitors (such as ketoconazole, itraconazole, clarithromycin, erythromycin, and ritonavir) can increase Cabozantinib levels and the risk of side effects. Your doctor may adjust the dose.
  • Strong CYP3A4 inducers (such as rifampicin, phenytoin, carbamazepine, phenobarbital, and St. John's Wort) can reduce its effectiveness and should generally be avoided.
  • Cabozantinib may affect some other medicines, such as digoxin, dabigatran, colchicine, and warfarin. Your doctor may need to monitor you more closely.
  • Oral contraceptive pills may be less reliable during treatment. Use an additional barrier method, such as condoms.
  • Antacids, PPIs, and H2-blockers generally do not significantly affect Cabozantinib and can usually be taken without changing the dose.
  • Note: Always tell your doctor about all prescription medicines, over-the-counter medicines, vitamins, supplements, and herbal products you take.

Interactions with food items

Cabozantinib must be taken on an empty stomach, at least 1 hour before or at least 2 hours after eating, as food increases the amount of medicine absorbed. Avoid grapefruit, grapefruit juice, and supplements containing grapefruit throughout treatment, as they can increase the level of the medicine in your blood. Avoid St. John's Wort, as it can reduce the medicine's effectiveness. Drink enough water and fluids through the day, especially if you have diarrhoea or vomiting, to avoid dehydration.

Dosage

Overdose

If you have taken more Cabozantinib than prescribed, contact your doctor or go to the nearest hospital immediately. There is no specific antidote for an overdose. Treatment focuses on monitoring and managing any symptoms.

Missed a Dose

If your next dose is 12 hours or more away, take the missed dose as soon as you remember. If your next dose is less than 12 hours away, skip the missed dose and take your next dose at the usual time. Do not take two doses to make up for a missed dose.

Frequently Asked Questions (FAQs)

Cabozantinib is used for the conditions listed in the Uses section of this page. Your doctor will decide whether it is suitable for your cancer type and stage.

No. Do not stop, delay or change your treatment on your own, even if you feel well. Stopping early can make the treatment less effective. Always speak to your doctor first.

Yes. Your doctor will usually advise regular blood tests and clinical check-ups during treatment to monitor how your body is responding and to pick up side effects early.

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