(nye-LOE-ti-nib)

Generic Name: nilotinib
Trade Name(s): Tasigna

Nilotinib is the generic for the trade chemotherapy drug Tasigna. In some cases, health care professionals may use the trade name Tasigna when referring to the generic drug name nilotinib.

Drug Type:

Nilotinib is targeted therapy. Nilotinib is classified as a signal transduction inhibitor - protein-tyrosine kinase inhibitor.  For more detail, see How Nilotinib Works below.

What Nilotinib Is Used For:

Nilotinib is used for treatment of Philadelphia chromosome-positve CML that is refactory or intolerant to prior therapy, including imatinib.

Note: If a drug has been approved for one use, physicians may elect to use this same drug for other problems if they believe it may be helpful.

How Nilotinib Is Given:

• Nilotinib is a pill, taken by mouth, once or twice daily.
• Nilotinib must be taken on an empty stomach:
• Avoid food at least 2 hours before the dose is taken
• Avoid food for 1 hour after the dose is taken
• Avoid grapefruit or grapefruit juice while taking this medication.
• The amount of nilotinib that you will receive depends on many factors, including your general health or other health problems, and the type of cancer or condition you have. Your doctor will determine your exact nilotinib dosage and schedule.

Side Effects:

Important things to remember about the side effects of nilotinib:

• Most people will not experience all of the side effects listed.
• Side effects are often predictable in terms of their onset, and duration.
• Side effects are almost always reversible and will go away after therapy is complete.
• Side effects may be quite manageable. There are many options to minimize or prevent the side effects of nilotinib.

The following side effects are common (occurring in greater than 30%) for patients taking nilotinib:

• Low blood counts.  Your white and red blood cells and platelets may temporarily decrease.  This can put you at increased risk for infection, anemia and/or bleeding.
• Rash
• Headache

These are less common side effects for patients receiving nilotinib:

• Itching
• Diarrhea
• Nausea or Vomiting
• Constipation
• Fatigue
• Joint pain
• Elevated liver enzymes
• Fever
• Muscle pain
• Cough
• Weakness
• Cold symptoms
• Abdominal pain
• Muscle spasm
• Edema (swelling of the face, feet, hands)
• Bone pain
• Back pain
• Shortness of breath
• High blood glucose levels

A rare, but potentially serious side effect of nilotinib is liver toxicity.  There may be elevations in transaminase, bilirubin, and lactate dehydrogenase. Liver function will be monitored while taking this medication.

Not all side effects are listed above. Some that are rare (occurring in less than 10% of patients) are not listed here.  However, you should always inform your health care provider if you experience any unusual symptoms.

When to contact your doctor or health care provider:

Contact your doctor or health care provider immediately, day or night, if you should experience any of the following symptoms:

• Fever of 100.4° F (38° C) or higher, chills (possible signs of infection)
• Shortness of breath, difficulty breathing

The following symptoms require medical attention, but are not an emergency. Contact your doctor or health care provider within 24 hours of noticing any of the following:

• Nausea (interferes with ability to eat and unrelieved with prescribed medication)
• Vomiting (vomiting more than 4-5 times in a 24 hour period)
• Diarrhea (4-6 episodes in a 24-hour period)
• Unusual bleeding or bruising
• Black or tarry stools or blood in your stools
• Blood in your urine
• Extreme fatigue (unable to carry on self-care activities)
• Swelling of the feet or ankles.  Sudden weight gain.
• Unusual cough.

• Yellowing of the skin or eyes
• Swelling of the feet or ankles.  Sudden weight gain.

Always inform your doctor or health care provider if you experience any unusual symptoms.

Precautions:

• Before starting nilotinib treatment, make sure you tell your doctor about any other medications you are taking (including prescription, over-the-counter, vitamins, herbal remedies, etc.). While taking nilotinib do not take aspirin or products containing aspirin unless your doctor specifically permits this. St. John's Wort may decrease the effectiveness of this medication.
• Avoid grapefruit or grapefruit juice while taking this medication.  

• Do not receive any kind of immunization or vaccination without your doctor's approval while taking nilotinib.
• Inform your health care professional if you are pregnant or may be pregnant prior to starting this treatment.  Pregnancy category D (nilotinib may be hazardous to the fetus.  Women who are pregnant or become pregnant must be advised of the potential hazard to the fetus).

• For both men and women: Use contraceptives and do not conceive a child (get pregnant) while taking Nilotinib. Barrier methods of contraception such as condoms are recommended.
• Do not breast feed while taking Nilotinib.

Self-Care Tips:

• Take as directed on an empty stomach, 1 hour before or 2 hours after a meal.
• While taking nilotinib, drink at least two to three quarts of fluid every 24 hours, unless you are instructed otherwise.

• If you miss a dose of this medication, do not take the missed dose at all and do not double the next one.  Instead, go back to your regular dosing schedule and check with your health care provider.
• You may be at risk of infection so try to avoid crowds or people with colds and those not feeling well, and report fever or any other signs of infection immediately to your health care provider.
• Wash your hands often. 
• Use an electric razor and a soft toothbrush to minimize bleeding.
• Avoid contact sports or activities that could cause injury.
• To reduce nausea, take anti-nausea medications as prescribed by your doctor, and eat small, frequent meals while taking nilotinib.
• In general, drinking alcoholic beverages should be kept to a minimum or avoided completely.  You should discuss this with your doctor.
• Avoid sun exposure. Wear SPF 15 (or higher) sunblock and protective clothing.
• Get plenty of rest. 
• Maintain good nutrition.
• If you experience symptoms or side effects, be sure to discuss them with your health care team.  They can prescribe medications and/or offer other suggestions that are effective in managing such problems.

Monitoring and Testing:

You will be checked regularly by your doctor while you are taking nilotinib to monitor side effects and check your response to therapy. Periodic blood work will be obtained to monitor your complete blood count (CBC) as well as the function of other organs (such as your kidneys and liver) will also be ordered by your doctor.

How Nilotinib Works:

Targeted therapy is the result of about 100 years of research dedicated to understanding the differences between cancer cells and normal cells. To date, cancer treatment has focused primarily on killing rapidly dividing cells because one feature of cancer cells is that divide rapidly. Unfortunately, some of our normal cells divide rapidly too, causing multiple side effects.

Targeted therapy is about identifying other features of cancer cells. Scientists look for specific differences in the cancer cells and the normal cells. This information is used to create a targeted therapy to attack the cancer cells without damaging the normal cells, thus leading to fewer side effects. Each type of targeted therapy works a little bit differently but all interfere with the ability of the cancer cell to grow, divide, repair and/or communicate with other cells.

There are different types of targeted therapies, defined in three broad categories. Some targeted therapies focus on the internal components and function of the cancer cell. The targeted therapies use small molecules that can get into the cell and disrupt the function of the cells, causing them to die. There are several types of targeted therapy that focus on the inner parts of the cells. Other targeted therapies target receptors that are on the outside of the cell. Therapies that target receptors are also known as monoclonal antibodies. Antiangiogenesis inhibitors target the blood vessels that supply oxygen to the cells, ultimately causing the cells to starve.

Nilotinib belongs to the signal transduction inhibitor category of targeted therapies.  It is particularly a protein-tyrosine kinase inhibitor and targets BCR-ABl kinase, c-KIT and platelet derived growth factor receptor (PDGFR).

Research continues to identify which cancers may be best treated with targeted therapies and to identify additional targets for more types of cancer. 

Note: We strongly encourage you to talk with your health care professional about your specific medical condition and treatments. The information contained in this website is meant to be helpful and educational, but is not a substitute for medical advice.

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