nilotinib (Tasigna): Leukemia Drug Side Effects & Dosage

What is nilotinib? What is nilotinib used for?

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.

What brand names are available for nilotinib?

Tasigna

Is nilotinib available as a generic drug?

Do I need a prescription for nilotinib?

Yes

What are the side effects of nilotinib?

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.

Other important side effects caused by Nilotinib include:

low phosphate (hypophosphatemia),
low potassium (hypokalemia),
high potassium (hyperkalemia),
low calcium (hypocalcemia),
and low sodium (hyponatremia) concentrations in the 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.

What is the dosage for nilotinib?

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.

Which drugs or supplements interact with nilotinib?

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.

Is nilotinib safe to take if I’m pregnant or breastfeeding?

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

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.

What else should I know about nilotinib?

What preparations of nilotinib are available?

Capsules: 150 and 200 mg

How should I keep nilotinib stored?

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