Nilotinib Zentiva (Nilotinib)

Nilotinib is a targeted therapy used in the management of chronic myeloid leukemia, a disease driven by the BCR‑ABL tyrosine‑kinase pathway.

• Chronic myeloid leukemia (chronic phase): reduces leukemic cell proliferation in Philadelphia chromosome‑positive patients.
• Chronic myeloid leukemia (accelerated phase): helps achieve hematologic and cytogenetic responses.
• Chronic myeloid leukemia (blast phase): provides disease control when combined with other agents.

• Nilotinib selectively inhibits the BCR‑ABL tyrosine kinase, a fusion protein that drives uncontrolled cell growth in Philadelphia chromosome‑positive leukemia. By binding to the ATP‑binding site of BCR‑ABL, it blocks downstream signaling pathways responsible for proliferation, survival, and migration of malignant leukemic cells, thereby restoring normal hematopoiesis.

Adverse reactions may vary in frequency and severity.

Common Side Effects

• Nausea: mild to moderate gastrointestinal upset.
• Diarrhea: loose stools, often transient.
• Rash: skin erythema or pruritus.
• Headache: mild to moderate intensity.
• Fatigue: generalized tiredness.
• Myalgia: muscle aches.

Serious or Rare Side Effects

• Pancreatitis: abdominal pain with elevated enzymes.
• Severe liver injury: jaundice, elevated transaminases.
• QT interval prolongation: risk of cardiac arrhythmia.
• Severe neutropenia: marked reduction in white blood cells.
• Severe thrombocytopenia: low platelet counts leading to bleeding.
• Cardiac failure: signs of reduced cardiac output.

Patients should be monitored closely for safety concerns before and during therapy.

• ECG monitoring: assess QT interval prior to initiation and periodically.
• Liver function tests: check baseline and follow‑up enzymes.
• Hematology monitoring: regular complete blood counts.
• Avoid in known QT‑prolonging conditions: patients with congenital long QT or electrolyte disturbances.
• Use caution in hepatic impairment: dose adjustment may be required.
• Store at below 25°C: keep in the original pack, protect from moisture.

Nilotinib may interact with several concomitant medicines, altering its efficacy or safety.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole): may increase nilotinib exposure.
• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine): may reduce therapeutic levels.
• QT‑prolonging agents (e.g., amiodarone, sotalol): additive risk of cardiac arrhythmia.
• Antacids containing aluminum or magnesium: reduce absorption if taken simultaneously.

Moderate Interactions (Monitor Closely)

• Moderate CYP3A4 inhibitors (e.g., erythromycin): may modestly raise concentrations.
• H2‑blockers (e.g., ranitidine): can affect gastric pH and absorption.
• Statins metabolized by CYP3A4 (e.g., simvastatin): monitor for increased statin levels.
• Warfarin: potential alteration of anticoagulant effect, monitor INR.