Nilotinib
Nilotinib
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Nilotinib

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Nilotinib

Nilotinib, sold under the brand name Tasigna among others, is an anti-cancer medication used to treat chronic myelogenous leukemia (CML) which has the Philadelphia chromosome. It may be used both in initial cases of chronic phase CML as well as in accelerated and chronic phase CML that has not responded to imatinib. It is taken by mouth.

Common side effects may include low platelets, low white blood cells, anemia, rashes, vomiting, diarrhea, and joint pains. Other serious side effects may include QT prolongation, sudden death, pancreatitis, and liver problems. It is not safe for use during pregnancy. Nilotinib is a Bcr-Abl tyrosine kinase inhibitor and works by interfering with signalling within the cancer cell.

Nilotinib was approved for medical use in the United States in 2007. It is on the World Health Organization's List of Essential Medicines. It is approved as a generic medication.

Nilotinib is used to treat Philadelphia chromosome (Ph+)-positive chronic myelogenous leukaemia. It is indicated for the treatment of newly diagnosed Philadelphia chromosome positive chronic myeloid leukemia in chronic phase; adults with chronic phase and accelerated phase Philadelphia chromosome positive chronic myeloid leukemia resistant to or intolerant to prior therapy that included imatinib; and children with chronic phase and accelerated phase Philadelphia chromosome positive chronic myeloid leukemia resistant or intolerant to prior tyrosine-kinase inhibitor therapy.

Nilotinib has a number of adverse effects including headache, fatigue, gastrointestinal problems such as nausea, vomiting, diarrhea and constipation, muscle and joint pain, rash and other skin conditions, flu-like symptoms, and reduced blood cell count. Less typical side effects are those of the cardiovascular system, such as high blood pressure, various types of arrhythmia, and prolonged QT interval. Nilotinib can also affect the body's electrolyte and glucose balance. Though lung-related adverse effects are rare when compared with imatinib and dasatinib, there is a case report of acute respiratory failure from diffuse alveolar hemorrhage in a people taking nilotinib.

Nilotinib carries a black box warning in the United States for possible heart complications. Contraindications include long QT syndrome, hypokalaemia, hypomagnesaemia, pregnancy, planned pregnancy, lactation and galactose/lactose intolerance.

Cautions include:

Dose reduction has been recommended in people with liver problems which involves recommendation of lower starting dose and monitoring of any hepatic function abnormalities.

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