Nilotinib (Tasigna®)

OncoLink
Last Modified: January 14, 2012

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Pronounced: nye-LOE-ti-nib
Classification: Tyrosine Kinase Inhibitor

About Nilotinib

Nilotinib is a type of medication called a tyrosine kinase inhibitor. Tyrosine kinases are enzymes (a type of protein) that help control the function of various cells in the body. Nilotinib works by inhibiting multiple different kinases, which in turn leads to inhibition of overproduction of leukemia cells. This inhibition occurs in the bone marrow of patients with chronic myeloid leukemia (CML) and other hyperproliferative diseases, while allowing normal red cell, white cell, and platelet production to resume. This helps to stop or slow the spread of cancer cells.

How to Take Nilotinib

Nilotinib comes as a capsule to take by mouth twice a day. The dose should be taken 2 hours after a meal, with a full glass of water and the patient should not eat for 1 hour after the dose. The doses should be taken 12 hours apart, and never less than 8 hours apart. Do not crush or break nilotinib tablets, swallow them whole. Grapefruit and star fruit (and their juices) can interfere with the medication and should be avoided.

Possible Side Effects of Nilotinib

There are a number of things you can do to manage the side effects of Nilotinib. Talk to your doctor or nurse about these recommendations. They can help you decide what will work best for you. These are some of the most common side effects:

Low White Blood Cell Count (Leukopenia or Neutropenia)

White blood cells (WBC) are important for fighting infection. While receiving treatment, your WBC count can drop, putting you at a higher risk of getting an infection. You should let your doctor or nurse know right away if you have a fever (temperature greater than 100.4°), sore throat or cold, shortness of breath, cough, burning with urination, or a sore that doesn't heal.

Tips to preventing infection:

  • Washing hands, both yours and your visitors, is the best way to prevent the spread of infection.
  • Avoid large crowds and people who are sick (i.e.: those who have a cold, fever or cough or live with someone with these symptoms).
  • When working in your yard, wear protective clothing including long pants and gloves.
  • Do not handle pet waste.
  • Keep all cuts or scratches clean.
  • Shower or bath daily and perform frequent mouth care.
  • Do not cut cuticles or ingrown nails. You may wear nail polish, but not fake nails.
  • Ask your doctor or nurse before scheduling dental appointments or procedures.
  • Ask your doctor or nurse before you, or someone you live with, has any vaccinations.

For more suggestions, read the Neutropenia Tip Sheet.

Low Red Blood Cell Count (Anemia)

Your red blood cells are responsible for carrying oxygen to the tissues in your body. When the red cell count is low, you may feel tired or weak. You should let your doctor or nurse know if you experience any shortness of breath, difficulty breathing or pain in your chest. If the count gets too low, you may receive a blood transfusion. Read the anemia tip sheet for more information.

Low Platelet Count (Thrombocytopenia)

Platelets help your blood clot, so when the count is low you are at a higher risk of bleeding. Let your doctor or nurse know if you have any excess bruising or bleeding, including nose bleeds, bleeding gums or blood in your urine or stool. If the count becomes too low, you may receive a transfusion of platelets.

  • Do not use a razor (an electric razor is fine).
  • Avoid contact sports and activities that can result in injury or bleeding.
  • Do not take aspirin (salicylic acid), non-steroidal, anti-inflammatory medications (NSAIDs) such as Motrin®, Aleve®, Advil®, etc. as these can all increase the risk of bleeding. You may take acetaminophen (Tylenol).
  • Do not floss or use toothpicks and use a soft-bristle toothbrush to brush your teeth.

Read the thrombocytopenia tip sheet for more information.

Nausea and/or Vomiting

Take anti-nausea medications as prescribed. If you continue to have nausea or vomiting, notify your doctor or nurse so they can help you manage this side effect. In addition, dietary changes may help. Avoid things that may worsen the symptoms, such as heavy or greasy/fatty, spicy or acidic foods (lemons, tomatoes, oranges). Try antacids, (e.g. milk of magnesia, calcium tablets such as Tums), saltines, or ginger ale to lessen symptoms. Read the Nausea & Vomiting Tip Sheet for more suggestions.

Call your doctor or nurse if you are unable to keep fluids down for more than 12 hours or if you feel lightheaded or dizzy at any time.

Fatigue

While on cancer treatment you may need to adjust your schedule to manage fatigue. Plan times to rest during the day and conserve energy for more important activities. Exercise can help combat fatigue; a simple daily walk with a friend can help. Talk to your healthcare team and see OncoLink's section on fatigue for helpful tips on dealing with this side effect.

Diarrhea

Your oncology team can recommend medications to relieve diarrhea. Also, try eating low-fiber, bland foods, such as white rice and boiled or baked chicken. Avoid raw fruits, vegetables, whole grain breads, cereals and seeds. Soluble fiber is found in some foods that absorbs fluid and can help relieve diarrhea. Foods high in soluble fiber include: applesauce, bananas (ripe), canned fruit, orange and grapefruit sections, boiled potatoes, white rice and products made with white flour, oatmeal, cream of rice, cream of wheat, and farina. Drink 8-10 glasses on non-alcoholic, un-caffeinated fluid a day to prevent dehydration. Read Low Fiber Diet for Diarrhea for more tips.

Muscle or Joint Pain/Aches and Headache

Your doctor or nurse can recommend medication and other strategies to relive pain. Also view OncoLink's page on pain management.

Heart Rhythm Changes

Nilotinib can cause changes in the QT interval, a measure of part of the heart rhythm, which is done with an ECG (electrocardiogram). Elongation of the QT interval can result in an abnormal heart rhythm and, in some cases, can lead to death. Your healthcare team will perform an ECG to check for this abnormality prior to starting nilotinib, 7 days after starting, with any dose changes and periodically while on the drug. Abnormal blood levels of potassium and magnesium can make you more susceptible to this problem, so those blood levels will be monitored as well. If you develop an irregular heart beat, feel your heart beating more than normal or experience fainting, notify your doctor immediately.

Fluid Retention

Nilotinib has been reported to cause fluid retention. This may result in generalized swelling, bloating of the abdomen (ascites), fluid development in the lungs (pleural effusion), or heart failure. Notify your healthcare team if you develop swelling, shortness of breath or difficulty breathing, or if you develop a dry cough.

Reproductive Concerns

Exposure of an unborn child to this medication could cause birth defects, so you should not become pregnant or father a child while on this medication. Effective birth control is necessary during treatment, even if your menstrual cycle stops or you believe your sperm is affected.

Other Side Effects

Some less common side effects that have been reported include: constipation, dry skin and rash.

Drug Reactions

Nilotinib is broken down in the body by an enzyme called CYP3A4. This enzyme is affected by many other medications and grapefruit juice. Taking nilotinib with other medications can lead to either higher or lower levels in the blood of one or both of the medications. Talk to your healthcare team if you are taking any of the following medications that can interfere with nilotinib:

St. John's Wort, ketoconazole, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole, dexamethasone, phenytoin, carbamazepine, rifampicin, or phenobarbital.


News
ASCO: Crizotinib Beats Chemo for ALK-Positive Lung Cancer

Jun 4, 2013 - For patients with chromosomal rearrangements of the anaplastic lymphoma kinase gene (ALK), treatment with an oral tyrosine kinase inhibitor targeting ALK, crizotinib, is superior to standard chemotherapy, according to a study published online June 1 in the New England Journal of Medicine to coincide with presentation at the annual meeting of the American Society of Clinical Oncology, held from May 31 to June 4 in Chicago.



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