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Crizotinib

(kriz-oh-tuh-nib)

Trade/other name(s): Xalkori

Why would this drug be used?

This drug is used to treat advanced non-small cell lung cancers that have a certain mutation in the ALK gene. It is also being studied for use against other types of cancer.

How does this drug work?

Crizotinib is a type of targeted therapy known as a kinase inhibitor. Kinases are proteins on or near the surface of a cell that transmit important signals to the cell's control center. When the ALK gene is mutated, it makes a kinase that tells the cell to grow and divide in an out of control way. Crizotinib blocks the mutated form of the ALK kinase, as well as some other kinases.

Only a small portion of non-small cell lung cancers have the mutated ALK gene. Your doctor will test your cancer cells to be sure they have this mutation before starting treatment with this drug.

Before taking this medicine

Tell your doctor…

  • If you are allergic to anything, including medicines, dyes, additives, or foods.
  • If you have any type of liver disease (including hepatitis). This drug is cleared from the body mainly by the liver. It may also affect the liver itself. Reduced liver function might result in more drug than expected staying in the body, which could lead to unwanted side effects. If this happens, your doctor may need to adjust your dose.
  • If you have any type of kidney disease. Some of this drug is cleared from the body by the kidneys. Reduced kidney function might result in more drug than expected staying in the body, which could lead to unwanted side effects. Your doctor may need to follow you more closely or even adjust your dose.
  • If you have ever been diagnosed with heart problems, especially long QT syndrome, any abnormal heart rhythm, congestive heart failure, or if you have been told you have low blood levels of potassium, calcium, or magnesium (which can affect the heart). Crizotinib can cause a change in the electrical activity in the heart, which can lead to irregular heartbeats and can be life threatening. People with long QT syndrome should not take this drug. People with other heart rhythm problems, congestive heart failure, or low blood levels of certain minerals need to be monitored closely while on this drug.
  • If you have any other medical conditions such as bleeding problems, diabetes, gout, or infections. These conditions may require that your medicine dose, regimen, or timing be changed.
  • If you are pregnant, trying to get pregnant, or if there is any chance of pregnancy. This drug may cause problems with the fetus if taken at the time of conception or during pregnancy. Women who could become pregnant and men who are taking this drug should use some kind of birth control during and for at least 90 days after finishing treatment. Check with your doctor about what kinds of birth control can be used with this medicine. In pregnant women, treatment with this drug should be used only if the potential benefit to the mother outweighs the risk to the fetus.
  • If you are breast-feeding. While no studies have been done, this drug may pass into breast milk and affect the baby. Breast-feeding is not recommended during treatment with this drug.
  • If you think you might want to have children in the future. This drug may affect fertility. Talk with your doctor about the possible risk with this drug.
  • About any other prescription or over-the-counter medicines you are taking, including vitamins and herbs. In fact, keeping a written list of each of these medicines (including the doses of each and when you take them) with you in case of emergency may help prevent complications if you get sick.

Interactions with other drugs

Crizotinib can interact with a number of drugs and supplements, so it is important to check with your health care team before taking any new medicines.

The following drugs and supplements can lower the levels of crizotinib in the blood and might make it less effective:

  • Anti-seizure drugs, such as carbamazepine (Tegretol), phenobarbital (Solfoton), and phenytoin (Dilantin)
  • Drugs to treat tuberculosis (TB), such as rifampin (Rifadin, Rimactane; also in Rifamate and Rifater), rifabutin (Mycobutin), and rifapentine (Prifin)
  • The steroid drug dexamethasone (Decadron)
  • St. John's wort (herbal dietary supplement)

Some drugs and supplements could cause crizotinib to build up in your blood, which might worsen side effects and other problems:

  • Some antibiotics, such as erythromycin, clarithromycin (Biaxin), telithromycin (Ketek), and similar drugs
  • Anti-fungal medicines such as ketoconazole (Nizoral), itraconazole (Sporanox), and voriconazole (Vfend)
  • Some anti-depressant drugs, such as nefazodone (Serzone)
  • Anti-HIV drugs such as indinavir (Crixivan), ritonavir (Kaletra), nelfinavir (Viracept), atazanavir (Reyataz), saquinavir (Invirase), and others

If you need to take any of these drugs, your doctor may need to adjust your dose of crizotinib. Do not start or stop taking any of these medicines while on crizotinib without talking with the prescribing doctor(s) about all of the medicines you take, including crizotinib.

Be sure to tell your doctor if you are taking any prescription or over-the counter drugs for stomach problems such as heartburn, reflux, or ulcers. This includes antacids such as Tums, Rolaids, or Alka-Seltzer; proton pump inhibitors such as omeprazole (Prilosec) or lansoprazole (Prevacid); and histamine blockers such as cimetidine (Tagamet) or ranitidine (Zantac). These drugs may lower the amount of crizotinib absorbed by your body.

Because crizotinib may affect the rhythm of your heart, be sure your doctor is aware of any drugs you take that affect heart rhythm, such as amiodarone (Cordarone), disopyramide (Norpace), dofetilide (Tikosyn), flecainide (Tambocor), mexiletine (Mexitil), moricizine (Ethmozine), procainamide (Procanbid, Pronestyl), propafenone (Rythmol), quinidine (Quinidex), and tocainide (Tonocard).

Beta blocker drugs also slow the heart rate and can worsen effects on the heart. This class includes drugs like acebutolol (Sectral), atenolol (Tenormin), bisoprolol (Zebeta), esmolol (Brevibloc), metoprolol (Lopressor, Lopressor LA, Toprol XL), nadolol (Corgard), propranolol (Inderal), sotalol (Betapace), and timolol (Blocadren).

Clonidine (Catapres), digoxin (Lanoxin, Cardoxin, Digitek), and the calcium calcium channel blockers diltiazem (Cardizem) and verapamil (Covera, Calan, Verelan) can also slow the heart and might cause problems with crizotinib.

Other medicines or supplements may affect blood levels of crizotinib, or levels of these drugs may be affected by taking crizotinib. Crizotinib can cause drugs like fentanyl, sirolimus, quinidine, ergotamine, dihydroergotamine, pimozide, cyclosporine, and tacrolimus to build up to dangerously high levels in the body. Make sure your doctor is aware of all drugs and supplements you are taking.

Check with your doctor, nurse, or pharmacist about any other medicines, herbs, and supplements you are taking, and whether alcohol can cause problems with this medicine.

Interactions with foods

Grapefruit and grapefruit juice may affect the amount of crizotinib in the body, so they should not be consumed while taking this drug. Check with your doctor, nurse, or pharmacist about whether any other specific foods may be a problem.

Tell all the doctors, dentists, nurses, and pharmacists you visit that you are taking this drug.

How is this drug taken or given?

Crizotinib is taken by mouth as capsules. The usual starting dose is one 250 mg (milligram) capsule, taken twice a day. The capsules should be swallowed whole (not chewed, crushed, or opened). They can be taken with or without food. Your dose may need to be adjusted if you have side effects.

Take this drug exactly as directed by your doctor. If you do not understand the instructions, ask your doctor or nurse to explain them to you. Keep the medicine in a tightly closed container away from heat and moisture and out of the reach of children and pets.

Precautions

This drug may interact with a number of other drugs or supplements in the body. (See "Interactions" above.) Be sure your doctor is aware of all drugs and supplements you are taking. Do not start or stop taking any drug without talking to your doctor about all of them.

Crizotinib may affect the heart's rhythm. Tell your doctor if you have ever been diagnosed with any type of heart disease, especially an abnormal heart rhythm or long QT syndrome. Your doctor may need to test your heart rhythm with an EKG and test your blood levels of certain minerals that could affect heart rhythm during treatment. Report any episodes of fast or irregular heartbeat, very slow heartbeat, chest pain, lightheadedness, dizziness, fainting, or shortness of breath to your doctor right away.

This drug can cause swelling in the lungs (pneumonitis) in a small portion of people when it is given, which in some cases may be life threatening. Tell your doctor or nurse right away if you have new symptoms such as shortness of breath, cough, or fever while taking the drug.

This drug may cause liver damage. Your doctor will order blood tests and will check you for signs of liver problems before and during treatment to make sure your liver is working well. Tell your doctor or nurse right away if you have yellowing of the skin or the whites of your eyes (jaundice), dark (tea-colored) urine, fatigue, nausea or vomiting, loss of appetite, pain on the right side of your belly, itching, or any abnormal bruising or bleeding.

This drug may cause vision problems in some people. Tell your doctor or nurse right away if you notice any changes in vision while taking this drug, such as flashes of light, blurred vision, floaters in your field of vision, or light hurting your eyes.

If you have vision problems or feel tired or dizzy when talking this drug, be very careful when driving a car, using machinery, or doing anything else that requires you to be alert.

You may have nausea and vomiting while taking this drug. These are usually not severe, but tell your doctor or nurse if you have these symptoms. Ask if they can offer ways to help relieve them.

Avoid pregnancy while taking this drug and for at least 90 days afterward. It may harm the fetus. Both men and women should use effective birth control during treatment and for at least 90 days afterward. Talk with your doctor about this.

Possible side effects

You will probably not have most of the following side effects, but if you have any talk to your doctor or nurse. They can help you understand the side effects and cope with them.

Common

  • Vision problems*
  • Nausea*
  • Vomiting*
  • Diarrhea
  • Constipation
  • Swelling, often in the hands or feet, but can also affect the face and eye area
  • Feeling tired
  • Loss of appetite
  • Feeling dizzy*
  • Trouble swallowing or heartburn
  • Nerve damage (neuropathy), which can cause weakness or numbness, tingling, or even pain in the hands or feet
  • Shortness of breath*
  • Cough*
  • Upper respiratory infection (a “cold”)

Less common

  • Belly pain
  • Mouth sores
  • Chest pain
  • Fever*
  • Joint pain
  • Back pain
  • Headache
  • Changes in taste
  • Weight loss
  • Trouble sleeping
  • Skin rash
  • Lowered white blood cell counts, which may increase your risk of infection
  • Abnormal blood tests suggesting drug may be affecting the liver (Your doctor will discuss the importance of this finding, if any.)*
  • Blood clots in the lung (pulmonary embolus)
  • Slowed heart rate

Rare

  • Changes in heart rhythm, which may be life threatening*
  • Swelling in the lungs, which may be life threatening*
  • Kidney cysts
  • Lowered blood platelet counts, which may increase your risk of bleeding
  • Death due to severe liver damage, blood clot in the lung, or lung disease*

*See the "Precautions" section for more detailed information.

Other side effects not listed above can also occur in some patients. Tell your doctor or nurse if you develop these or any other problems.

FDA approval

Yes – first approved in 2011

Disclaimer: This information does not cover all possible uses, actions, precautions, side effects, or interactions. It is not intended as medical advice, and should not be relied upon as a substitute for talking with your doctor, who is familiar with your medical needs.


Last Medical Review: 12/19/2013
Last Revised: 12/19/2013