nilotinib, Tasigna

Pharmacy Author:

Omudhome Ogbru, PharmD

Omudhome Ogbru, PharmD

Dr. Ogbru received his Doctorate in Pharmacy from the University of the Pacific School of Pharmacy in 1995. He completed a Pharmacy Practice Residency at the University of Arizona/University Medical Center in 1996. He was a Professor of Pharmacy Practice and a Regional Clerkship Coordinator for the University of the Pacific School of Pharmacy from 1996-99.

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Medical and Pharmacy Editor:

Jay W. Marks, MD

Jay W. Marks, MD

Jay W. Marks, MD, is a board-certified internist and gastroenterologist. He graduated from Yale University School of Medicine and trained in internal medicine and gastroenterology at UCLA/Cedars-Sinai Medical Center in Los Angeles.

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GENERIC NAME: nilotinib

BRAND NAME: Tasigna

DRUG CLASS AND MECHANISM: Nilotinib is an oral medication used for treating chronic myeloid leukemia and acute lymphoblastic leukemia. Nilotinib is classified as a kinase inhibitor. Kinase inhibitors include dasatinib (Sprycel), erlotinib (Tarceva), gefitinib (Iressa), imatinib (Gleevec), pazopanib (Votrient), sunitinib (Sutent), and vandetanib (Caprelsa). Kinase inhibitors prevent the growth of tumors by reducing the action of proteins that control cell division, growth and survival. These proteins are usually present in larger quantities or are more active in cancer cells. By reducing the activity of these proteins, growth and survival of cancer cells are reduced. The FDA approved nilotinib in October 2007.

PRESCRIPTION: Yes

GENERIC AVAILABLE: No

PREPARATIONS: Capsules: 150 and 200 mg

STORAGE: Nilotinib should be stored nilotinib at room temperature between 15-30 C (59-86 F).

PRESCRIBED FOR: Nilotinib is used for the treatment of adults with newly diagnosed Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) or treatment of Ph+ CML after intolerance or failure of therapy that included imatinib.

DOSING: The recommended dose range is 300 mg or 400 mg orally twice daily taken 12 hours apart. Each capsule should be swallowed whole with water or sprinkle contents of capsule on one teaspoon of applesauce. Food increases the blood concentration of nilotinib. Therefore, nilotinib should be taken on an empty stomach, at least 2 hours after eating any food and individuals should wait one hour after taking nilotinib before eating any food.

DRUG INTERACTIONS: The blood concentration of nilotinib may be increased by several drugs that reduce its break down by the liver. Examples include amiodarone (Cordarone), disopyramide, procainamide, quinidine, and sotalol. Increased blood concentrations of nilotinib may increase the occurrence of adverse effects.

Certain drugs decrease the concentration of nilotinib resulting in decreased blood levels and possibly reduced effect. Examples include dexamethasone, carbamazepine, phenobarbital, rifampin, rifabutin, rifapentin, phenytoin, and St John's Wort.

Food increases the blood concentration of nilotinib. Therefore, nilotinib should be taken on an empty stomach, at least 2 hours after eating any food. Individuals should wait one hour after taking nilotinib before eating any food.

PREGNANCY: Nilotinib is harmful to the fetus and should not be used during pregnancy.

NURSING MOTHERS: It is not known whether nilotinib is excreted in human milk. Some related drugs are excreted in breast milk. To avoid any risk to the infant, nursing mothers should consider discontinuing nursing or nilotinib.

SIDE EFFECTS: Common side effects include headache, stomach pain, constipation, diarrhea, weight changes, weakness, nausea and vomiting, swelling of arms and legs, rash, itching, fever, dizziness, hair loss, coughing, runny or stuffy nose, and muscle pain. Increased blood glucose and high blood pressure may also occur. Serious side effects include fainting, seizures, fever associated with reduced white blood cells, reduced platelets and red blood cell counts, infection, bleeding in the brain, reduced liver function, pancreatitis, and increased or reduced thyroid function. Nilotinib can cause low phosphate (hypophosphatemia), low potassium (hypokalemia), high potassium (hyperkalemia), low calcium (hypocalcemia), and low sodium (hyponatremia) concentrations in blood.

Nilotinib may cause a type of abnormal heart rhythm called prolongation of QT interval. Prolongation of the QT interval may lead to sudden death. ECGs should be obtained prior to starting nilotinib, 7 days after start of treatment, after dose adjustments, and as needed thereafter. Low potassium or low magnesium may increase the risk of QT prolongation. Therefore, low potassium and low magnesium should be corrected prior to starting treatment. Food and/or drugs that reduce break down of nilotinib in the liver and/or medicinal products that prolong QT interval may increase the risk of QT prolongation and should not be combined with nilotinib.

Report Problems to the Food and Drug Administration You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088. Need help identifying pills and medications? Use the pill identifier tool on RxList.