Nilotinib is an inhibitor that targets the Bcr-Abl kinase, primarily indicated for the treatment of adult patients with Philadelphia chromosome-positive chronic myeloid leukemia (CML) who are resistant or intolerant to imatinib.
How to Use Nilotinib
Routine Dosing Regimen
Standard dose: 400mg orally, twice daily, with an interval of approximately 12 hours.
Administration requirements: The drug must be taken on an empty stomach. Fasting is required for at least 2 hours before administration and 1 hour after administration.
Capsule administration: Swallow the capsules whole; do not chew, crush, or open them.
Dietary restriction: Avoid grapefruit or products containing grapefruit, as they may increase the blood concentration of the drug.
Management of Missed Doses
If a dose is missed, do not make up for it; take the next dose as scheduled.
Dose Adjustment of Nilotinib
QT Interval Prolongation
QTc > 480 msec: Suspend medication. After correcting hypokalemia/hypomagnesemia:
If QTc returns to < 450 msec, resume the original dose.
If QTc remains between 450-480 msec, reduce the dose to 400mg once daily.
If QTc persists > 480 msec, discontinue the medication permanently.
Monitoring requirements: An electrocardiogram (ECG) should be rechecked at baseline, 7 days after starting medication, and after dose adjustments.
Hematologic Toxicity
Neutrophils < 1.0×10⁹/L or platelets < 50×10⁹/L: Suspend medication; resume the original dose once counts recover.
If recovery takes more than 2 weeks: Reduce the dose to 400mg once daily.
Non-Hematologic Toxicity
Pancreatitis (grade ≥ 3 amylase/lipase elevation) or hepatic enzyme abnormalities (grade ≥ 3 ALT/AST or bilirubin elevation): Suspend medication; after recovery, reduce the dose to 400mg once daily.
Drug Interactions
Strong CYP3A4 inhibitors (e.g., ketoconazole): Concomitant use should be avoided. If use is necessary, it is recommended to reduce the Nilotinib dose to 400mg once daily and closely monitor the QT interval.
Strong CYP3A4 inducers (e.g., rifampicin): An increase in the Nilotinib dose may be required.
Use of Nilotinib in Special Populations
Patients with Hepatic Impairment
Mild to moderate hepatic impairment: No dose adjustment is needed, but close monitoring of the QT interval and liver function is required.
Severe hepatic impairment: Data are limited; use with caution.
Pregnancy and Lactation
Pregnant women: Classified as Pregnancy Category D, as it may cause fetal malformations. Effective contraception is required during medication use.
Lactating women: The drug may be excreted in breast milk; it is recommended to discontinue the medication or stop breastfeeding.
Children and Elderly Patients
Children: Efficacy has not been established.
Elderly patients (≥ 65 years old): No dose adjustment is needed, but efficacy may be reduced in patients with accelerated-phase CML.
Other Precautions
Patients with heart disease: Avoid use in patients with uncontrolled cardiovascular disease or long QT syndrome.
Patients with lactose intolerance: Capsules contain lactose; use with caution in patients with severe lactose intolerance.
