Pronunciation:

nye-LOE-ti-nib

Brand Names:

• Tasigna

Dosage Forms:

• Capsule

Warnings:

• QT Prolongation and Sudden Deaths
  • Nilotinib prolongs the QT interval. Sudden deaths have been reported in patients receiving nilotinib. Nilotinib should not be used in patients with hypokalemia, hypomagnesemia, or long QT syndrome. Hypokalemia or hypomagnesemia must be corrected prior to nilotinib administration and should be periodically monitored. Drugs known to prolong the QT interval and strong CYP3A4 inhibitors should be avoided. Patients should avoid food 2 hours before and 1 hour after taking dose. Use with caution in patients with hepatic impairment. ECGs should be obtained to monitor the QTc at baseline, seven days after initiation, and periodically thereafter, as well as following any dose adjustments .

Prolongation of the QT interval and sudden death have been reported. Do not use nilotinib in the presence of hypokalemia, hypomagnesemia, or long QT syndrome. Hypokalemia or hypomagnesemia must be corrected prior to nilotinib administration and monitored during treatment. Avoid drugs that prolong the QT interval and strong CYP3A4 inhibitors. Avoid food 2 hours before and one hour after taking nilotinib. Use with caution in hepatic impairment. Monitor the QTc at baseline, 7 days after initiation, and periodically thereafter, and with any dose adjustments .

Classifications:

Therapeutic—

Antineoplastic Agent

Pharmacologic—

Tyrosine Kinase Inhibitor

Uses of This Medicine:

Nilotinib belongs to the group of medicines called antineoplastics. It is used to treat a type of cancer called Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) after other treatments (including imatinib [e.g., Gleevec®]) have failed. CML is a disease in which your body makes too many abnormal white blood cells, which can cause you to become sick more often and to feel weak or tired. Nilotinib helps your body stop making these abnormal white blood cells .

Nilotinib interferes with the growth of cancer cells, which are eventually destroyed. Since the growth of normal cells may also be affected by the medicine, other effects will also occur. Some of these may be serious and must be reported to your doctor. Other effects may not be serious but may cause concern .

Before you begin treatment with nilotinib, you and your doctor should talk about the good this medicine will do as well as the possible risks of using it .

This medicine is available only with your doctor's prescription .

Before Using This Medicine:

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies—

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Children—

Appropriate studies have not been performed on the relationship of age to the effects of nilotinib in the pediatric population. Safety and efficacy have not been established .

Older adults—

Appropriate studies performed to date have not demonstrated geriatrics-specific problems that would limit the usefulness of nilotinib in the elderly .

Pregnancy—

	Pregnancy Category	Explanation
All Trimesters	D	Studies in pregnant women have demonstrated a risk to the fetus. However, the benefits of therapy in a life threatening situation or a serious disease, may outweigh the potential risk.

Breast-feeding—

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Other medicines—

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Arsenic Trioxide
• Atazanavir
• Carbamazepine
• Cisapride
• Clarithromycin
• Dexamethasone
• Dofetilide
• Droperidol
• Gatifloxacin
• Ibutilide
• Indinavir
• Itraconazole
• Ketoconazole
• Lapatinib
• Levofloxacin
• Mesoridazine
• Methadone
• Midazolam
• Moxifloxacin
• Nefazodone
• Nelfinavir
• Paliperidone
• Phenobarbital
• Phenytoin
• Pimozide
• Quinidine
• Ranolazine
• Rifabutin
• Rifampin
• Rifapentine
• Ritonavir
• Saquinavir
• Sodium Phosphate
• Sotalol
• St John's Wort
• Sunitinib
• Telithromycin
• Vardenafil
• Voriconazole
• Warfarin
• Ziprasidone

Other interactions—

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Grapefruit Juice

Other medical problems—

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Heart rhythm problems (e.g., long QT syndrome) or
• Hyperkalemia (high potassium in the blood) or
• Hypocalcemia (low calcium in the blood) or
• Hypokalemia (low potassium in the blood) or
• Hypomagnesemia (low magnesium in the blood) or
• Hyponatremia (low sodium in the blood) or
• Hypophosphatemia (low phosphate in the blood)—These conditions should be treated first before using this medicine .

• Heart problems or
• Pancreatitis (inflammation of the pancreas), history of—Use with caution. This medicine may worsen these conditions .

• Lactose intolerance—Use with caution. This medicine contains lactose .

• Liver problems—Drug effects may be increased because of slower removal of nilotinib from the body .

Proper Use of This Medicine:

This medicine should come with a Medication Guide. Read and follow these instructions carefully. Ask your doctor or pharmacist if you have any questions. Ask your pharmacist for the Medication Guide if you do not have one. Your doctor might ask you to sign some forms to show that you understand this information .

It is best to take this medicine on an empty stomach (at least 1 hour before or 2 hours after a meal) .

Swallow the capsule whole with water. Do not open the capsules .

Dosing—

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (capsules):
  • For the treatment of CML:
    • Adults—400 milligrams (mg) two times a day, with about 12 hours between the two doses. Your doctor may adjust your dose if needed.
    • Children—Use and dose must be determined by your doctor .

Missed dose—

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage—

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using This Medicine:

It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly. Blood tests may be needed to check for unwanted effects .

This medicine can cause changes in heart rhythms, such as a condition called QT prolongation. It may change the way your heart beats and cause fainting or serious side effects in some patients. Check with your doctor right away if you have any symptoms of heart rhythm problems, such as fast, pounding, or irregular heartbeats .

Using this medicine while you are pregnant can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant. If you think you have become pregnant while using the medicine, tell your doctor right away .

Nilotinib can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection. It can also lower the number of platelets, which are necessary for proper blood clotting. If this occurs, there are certain precautions you can take, especially when your blood count is low, to reduce the risk of infection or bleeding:

• If you can, avoid people with infections. Check with your doctor immediately if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination.
• Check with your doctor immediately if you notice any unusual bleeding or bruising; black, tarry stools; blood in urine or stools; or pinpoint red spots on your skin.
• Be careful when using a regular toothbrush, dental floss, or toothpick. Your medical doctor, dentist, or nurse may recommend other ways to clean your teeth and gums. Check with your medical doctor before having any dental work done.
• Do not touch your eyes or the inside of your nose unless you have just washed your hands and have not touched anything else in the meantime.
• Be careful not to cut yourself when you are using sharp objects such as a safety razor or fingernail or toenail cutters.
• Avoid contact sports or other situations where bruising or injury could occur .

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements .

Do not eat grapefruit or drink grapefruit juice while you are using this medicine. Grapefruit and grapefruit juice may change the amount of this medicine that is absorbed in the body .

Side Effects of This Medicine:

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

Abdominal pain or tenderness

black, tarry stools

bleeding gums

blood in urine or stools

blurred vision

bone pain

clay colored stools

confusion

convulsions

cough or hoarseness

dark urine

decreased appetite

difficult or labored breathing

dry mouth

fainting

fever or chills

flushed, dry skin

fruit-like breath odor

headache

increased hunger

increased thirst

increased urination

irregular heartbeat, recurrent

itching

loss of appetite

lower back or side pain

muscle aches, cramps, or pain

nausea and vomiting

no blood pressure

no breathing

no pulse

numbness, tingling, pain, or weakness in hands or feet

painful or difficult urination

pale skin

pinpoint red spots on skin

seizures

shortness of breath

skin rash

sore throat

stuffy or runny nose

sweating

swelling of hands, ankles, feet, or lower legs

tightness in chest

trembling

troubled breathing with exertion

ulcers, sores, or white spots in mouth

unexplained weight loss

unusual bleeding or bruising

unusual tiredness or weakness

weakness and heaviness of legs

wheezing

yellow eyes or skin

Less common

Coma

decreased urine output

dizziness

fast heartbeat

mood or mental changes

muscle cramps in hands, arms, feet, legs, or face

nervousness

numbness and tingling around the mouth, fingertips, or lips

tremor

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

Back pain

diarrhea

difficulty having a bowel movement (stool)

difficulty in moving

lack or loss of strength

muscle spasms

muscle stiffness

pain in arms or legs

pain in joints

swollen joints

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.