Nilotinib is a tyrosine kinase inhibitor used for the treatment of Philadelphia chromosome-positive chronic myeloid leukemia (CML), primarily indicated for adult patients in the chronic phase and accelerated phase who are resistant or intolerant to imatinib.
What Are the Side Effects of Nilotinib?
Gastrointestinal Reactions
Nausea (31%).
Diarrhea (22%).
Constipation (21%).
Vomiting (21%).
Abdominal pain (11%).
Systemic Reactions
Fatigue (28%).
Headache (31%).
Fever (14%).
Laboratory Abnormalities
Thrombocytopenia (28%).
Neutropenia (28%).
Anemia (8%).
Serious Side Effects of Nilotinib to Be Alert For
QT Interval Prolongation and Cardiotoxicity
Nilotinib can prolong the QT interval in a concentration-dependent manner, which may lead to torsades de pointes (a type of ventricular tachycardia) or even sudden death.
Hypokalemia and hypomagnesemia must be corrected before medication use, and concurrent use of other drugs that prolong the QT interval should be avoided.
An electrocardiogram (ECG) should be monitored 7 days after starting medication and after dose adjustments.
Myelosuppression
It can cause grade 3/4 thrombocytopenia (28%), neutropenia (28%), and anemia (8%).
A complete blood count (CBC) should be monitored every 2 weeks in the first 2 months of treatment, and then once a month thereafter.
Medication should be suspended or the dose reduced if severe myelosuppression occurs.
Pancreatitis and Elevated Serum Lipase
15-17% of patients experience elevated lipase levels, and the risk is increased in patients with a history of pancreatitis.
Serum lipase should be monitored regularly; if symptoms of pancreatitis (severe abdominal pain accompanied by nausea and vomiting) occur, the medication should be discontinued immediately.
Hepatotoxicity
It may cause elevations in bilirubin, transaminases, and alkaline phosphatase.
Liver function should be monitored regularly during medication use; patients with liver impairment should use the drug with caution and undergo enhanced QT monitoring.
Precautions for Nilotinib Administration
Contraindicated Populations
Patients with hypokalemia, hypomagnesemia, or long QT syndrome.
Patients with severe hepatic impairment.
Pregnant women and lactating women.
Avoid Concurrent Use
Potent CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin).
Potent CYP3A4 inducers (e.g., rifampicin, phenytoin).
Other drugs that prolong the QT interval.
Use with Caution When Combined
P-glycoprotein substrates (e.g., digoxin).
CYP2C8/2C9/2D6 substrates (e.g., warfarin).
Key Patient Education Points
Strictly follow the requirement of taking the medication on an empty stomach.
Avoid grapefruit products.
Recognize symptoms of QT interval prolongation (palpitations, syncope).
Undergo regular ECG monitoring and laboratory tests.
Seek medical attention immediately if severe adverse reactions occur.
