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Nilotinib

(nil-lot-uh-nib)

Trade/other name(s): Tasigna, AMN107

Why would this drug be used?

This drug is used to treat chronic myelogenous leukemia (CML). It is also being studied for use against other kinds of leukemia and some other cancers.

How does this drug work?

Nilotinib is a targeted therapy called a kinase inhibitor. These kinases are proteins on or near the surface of a cell that send important signals to the cell’s control center. Nilotinib blocks the signals from these proteins and helps stop cancer cells from growing.

Before taking this medicine

Tell your doctor…

  • If you are allergic to anything, including medicines, dyes, additives, or foods.
  • If you have or have had any type of liver disease (including hepatitis). This drug is cleared from the body mainly by the liver. Poor liver function may result in more drug than expected staying in the body, which could lead to serious side effects. Your doctor may need to adjust your dose.
  • If you have any type of heart problem, especially if you have been told you (or a family member) have a “long QT syndrome” or that you have low blood levels of potassium or magnesium. This drug may affect the rhythm of the heart.
  • If you have congestive heart failure, angina, or have had a recent heart attack. This drug may contribute to heart failure or make existing conditions worse.
  • If you have had surgery to remove your stomach. Your dose may need to be changed.
  • If you are lactose or galactose intolerant. This drug contains lactose.
  • If you have ever had pancreatitis (inflammation of the pancreas). This drug may affect the pancreas.
  • If you have any other medical conditions such as kidney disease, high blood pressure, 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 can cause problems with the fetus if taken at the time of conception or during pregnancy. 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. Although 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. It is not known if this drug affects fertility. Talk with your doctor about the possible risk with this drug and the options that may preserve your ability to have children.
  • 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

Nilotinib can interact with a number of drugs and supplements. Certain medicines can raise nilotinib levels in the blood, which could lead to serious side effects:

  • Nefazodone (Serzone), an antidepressant
  • Antibiotics such as erythromycin (EES), clarithromycin (Biaxin) and telithromycin (Ketek)
  • Anti-fungals such as ketoconazole (Nizoral), itraconazole (Sporanox), voriconazole (Vfend)
  • HIV drugs such as indinavir, ritonavir, saquinavir, nelfinavir, atazanavir, and others

Do not start or stop taking these medicines while on nilotinib without talking with the prescribing doctor(s) about all of the medicines you take, including nilotinib.

These drugs and supplements can lower the levels of nilotinib in the blood, which might make it less effective:

  • Anti-seizure drugs carbamazepine (Tegretol), phenobarbital (Luminal), and phenytoin (Dilantin)
  • TB drugs rifampin (Rifadin, Rimactane; also in Rifamate and Rifater), rifapentin (Priftin), and rifabutin (Mycobutin)
  • The steroid drug dexamethasone (Decadron)
  • St. John’s wort (herbal dietary supplement)

If you need to take these drugs, your doctor may need to adjust your dose of nilotinib.

This drug may change your heart rhythm. Medicines that can affect heart rhythm or the heart’s electrical system may increase the risk of serious effects on the heart:

  • Antibiotics such as ciprofloxacin (Cipro), levofloxacin Levaquin), sparfloxacin (Zagam), moxifloxacin (Avelox), erythromycin (E.E.S., E-Mycin, Erythrocin), clarithromycin (Biaxin), or pentamidine (Pentam, NebuPent)
  • Anti-fungal drugs (amphotericin B)
  • Heart rhythm drugs such as amiodorone (Cordarone, Pacerone), disopyramide (Norpace), dofetilide (Tikosyn), flecainide (Tambocor), mexiletine (Mexitil), moricizine (Ethmozine), procainamide (Procanbid, Pronestyl), propafenone (Rythmol), quinidine (Quinidex), sotalol (Betapace, Betapace AF), and tocainide (Tonocard)
  • Mental health drugs such as haloperidol (Haldol), thioridazine (Mellaril), pimozide (Orap), mesoridazine (Serentil), chlorpromazine (Thorazine)
  • Methadone (Dolophine, Methadose)
  • The anti-nausea drug droperidol (Inapsine)
  • Anti-malaria drugs halofantrine (Halfan) and chloroquine (Aralen)
  • Bepridil (Vascor), a drug for angina or heart pain

Many drugs used to treat heartburn, reflux, or ulcers can reduce the acid levels in the stomach, which can affect the amount of nilotinib your body can absorb:

    • H2 blockers such as cimetidine (Tagamet), ranitidine (Zantac), famotidine (Pepcid), or nizatidine (Axid)

    • Proton pump inhibitors such as omeprazole (Prilosec), esomeprazole (Nexium), pantoprazole (Protonix), rabeprazole (AcipHex), lansoprazole (Prevacid), or dexlansoprazole (Dexilant).

    • Antacids such as Maalox, Mylanta, Tums, etc.

Talk with your doctor about whether you need to stop taking these drugs during treatment.

Any drugs or supplements that interfere with blood clotting can raise the risk of bleeding during treatment with nilotinib. These include:

  • Vitamin E
  • Non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen (Advil, Motrin), naproxen (Aleve, Naprosyn), and many others
  • Warfarin (Coumadin)
  • Ticlopidine (Ticlid)
  • Clopidogrel (Plavix)
  • Dabigatran (Pradaxa)
  • Rivaroxaban (Xarelto)
  • Apixaban (Eliquis)
  • Any type of heparin injections

Note that many cold, flu, fever, and headache remedies contain aspirin or ibuprofen. Ask your pharmacist if you aren’t sure what’s in the medicines you take.

Nilotinib may alter blood levels of other drugs you are taking, including warfarin (Coumadin), midazolam (Versed), and other drugs.

Other medicines or supplements may affect blood levels of nilotinib, or levels of these drugs may be affected by taking nilotinib. Make sure your doctor is aware of all drugs and supplements you are taking, and any changes in the medicines you take.

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

Interactions with foods

This drug should be taken on an empty stomach. Food may raise the level of nilotinib in your blood (see next section).

Grapefruit, grapefruit juice, or grapefruit extract may change the level of nilotinib in your blood. You should avoid grapefruit products during treatment with nilotinib. Check with your doctor, nurse, or pharmacist about whether some other 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?

Nilotinib is a capsule taken by mouth on an empty stomach. Take nilotinib at least 2 hours after eating, and wait at least 1 hour after taking nilotinib before eating again. The usual starting dose is 400 mg taken twice a day, about 12 hours apart. Swallow the capsules whole with water – do not open capsules.

The dose or schedule may need to be changed if you have side effects, if you have liver or pancreas problems, if your heart rhythm is affected, if you develop low blood counts, or if you are taking certain other drugs that may interact with nilotinib. This drug is a long-term treatment, so keep taking nilotinib for as long as your doctor prescribes it.

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. Store the medicine in a tightly closed container away from heat and moisture and away from children and pets.

Precautions

This drug may affect the heart rhythm. Tell your doctor if you have ever had heart problems before starting treatment. Your doctor should order a test of the heart rhythm (an ECG or EKG) before treatment begins and repeat the test during treatment to check for any problems. Blood tests may also be done to check level of potassium and magnesium. Tell your doctor right away if you notice changes in heartbeat (including changes in rhythm, pounding, or racing), chest pain, gasping for breath, fainting (passing out), or if you have a seizure. This problem can be an emergency, since on rare occasions it can cause sudden death.

Nilotinib may cause fluid to build up around your heart or lungs or in your abdomen, and may cause swelling around your eyes or in your hands or feet (edema). Tell your doctor or nurse right away if you gain weight, have swelling around your eyes or in your hands or feet, notice bloating or swelling in your abdomen, or have trouble breathing (shortness of breath).

Your doctor will probably test your blood throughout your treatment to look for effects of the drug on blood counts or on blood chemistry levels. Based on the test results, you may be given medicines to help treat any effects. Your doctor may also need to lower or delay your next dose of this drug, or even stop it altogether. Keep all your appointments for lab tests, heart checks, and doctor visits.

Nilotinib may lower your blood platelet count in the weeks after it is given, which can raise your risk of bleeding. Talk with your doctor before taking any drugs or supplements that could affect your body’s ability to stop bleeding, such as aspirin or aspirin-containing medicines, warfarin (Coumadin) or other “blood thinners”, or vitamin E (see “Interactions with other drugs” section). Tell your doctor right away if you notice unusual bruising, or bleeding such as nosebleeds, bleeding gums when you brush your teeth, blood in the urine, or black, tarry stools. Bleeding in the brain can cause headache, trouble speaking or moving, being confused, fainting or losing consciousness.

This drug can lower your white blood cell count, especially in the weeks after the drug is given. This can increase your chance of getting an infection. Tell your doctor or nurse right away if you have any signs of infection, such as fever (100.5° or higher), chills, pain when urinating, new onset of cough, or bringing up sputum.

This drug may lower your red blood cell count. If this happens, it is usually a few weeks after starting treatment. A low red blood cell count (known as anemia) can cause shortness of breath, or make you feel weak or tired all the time. Your doctor may give you medicines to help prevent or treat this condition, or you may need to have blood transfusions.

Do not get any immunizations (vaccines), either during or after treatment with nilotinib, without your doctor’s OK. Nilotinib may affect your immune system. This could keep vaccinations from working, or even lead to serious infections if you get a live virus vaccine during or soon after treatment. Try to avoid contact with people who have recently received a vaccine that uses live virus, such as the oral polio vaccine or smallpox vaccine. Check with your doctor about this.

Your liver may be affected by this drug, which could increase liver enzyme levels in your blood. Your doctor will check your liver function with blood tests. Tell your doctor right away if you notice your eyes or skin look yellow (jaundice) or if your urine becomes dark in color.

This drug may affect your pancreas. Your doctor will check your pancreas function with regular blood tests. Tell your doctor right away if you have nausea, vomiting, or pain in the stomach or mid back. Nilotinib may need to be stopped or the dose changed if the effects are severe.

Avoid pregnancy while taking this drug and for some time afterward. The drug may harm the fetus. 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

  • Skin rash
  • Itching
  • Nausea
  • Vomiting*
  • Constipation
  • Diarrhea
  • Feeling tired
  • Headache
  • Fever
  • Low white blood cell count (with increased risk of infection)*
  • Low blood platelet count (with increased risk for bleeding)*

Less common

  • Change in heart rhythm*
  • Pain in the stomach area, indigestion*
  • Swelling around the eyes or in the hands or feet (edema)*
  • Feeling weak
  • Muscle, joint, or bone pain
  • Back pain*
  • Shortness of breath*
  • Cough
  • Stuffy nose
  • High blood pressure
  • Feeling dizzy
  • Loss of appetite
  • Trouble sleeping
  • Low red blood cell counts (anemia)*
  • Low blood phosphate levels (Your doctor will discuss the importance of this finding, if any.)
  • Abnormal blood tests suggesting drug may be affecting the liver or pancreas. (Your doctor will discuss the importance of this finding, if any.)*

Rare

  • Infections*
  • Hair loss
  • Weight loss or weight gain
  • Abnormal blood levels of sodium, potassium, magnesium, or calcium (Your doctor will discuss the importance of this finding, if any.)
  • Congestive heart failure (can cause shortness of breath or swelling in hands or feet)*
  • Bleeding from the stomach or intestines*
  • Sudden death due to changes in heart rhythm*

*See “Precautions” section for more detailed information.

There are other side effects not listed above that 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 2007.

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: 12/29/2011
Last Revised: 01/29/2013