Nilotinib Zentiva (Nilotinib)

Nilotinib is a tyrosine kinase inhibitor used in the management of Philadelphia chromosome‑positive chronic myeloid leukemia.

• Chronic myeloid leukemia (chronic phase): reduces proliferation of BCR‑ABL‑positive leukemic cells, leading to hematologic and cytogenetic responses.
• Chronic myeloid leukemia (accelerated phase): achieves disease control and delays progression to blast crisis.
• Chronic myeloid leukemia (blast crisis): provides therapeutic benefit when combined with other agents, improving remission rates.

• Nilotinib selectively binds to the ATP‑binding site of the BCR‑ABL tyrosine kinase, inhibiting its activity. By blocking downstream signaling pathways that drive uncontrolled proliferation of Philadelphia chromosome‑positive leukemic cells, the drug restores normal cell growth regulation and induces apoptosis of malignant clones.

Common Side Effects

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

Serious or Rare Side Effects

• QT interval prolongation: risk of cardiac arrhythmia.
• Pancreatitis: severe abdominal pain and elevated enzymes.
• Hepatic dysfunction: elevated transaminases, jaundice.
• Severe neutropenia: increased infection risk.
• Cardiac failure: signs of reduced cardiac output.
• Severe skin reactions: Stevens‑Johnson syndrome or toxic epidermal necrolysis.

Nilotinib requires careful monitoring and patient education before and during therapy.

• ECG monitoring: assess QT interval before initiation and periodically.
• Liver function tests: check ALT, AST, bilirubin regularly.
• Blood glucose: monitor for hyperglycemia, especially in diabetic patients.
• CYP3A4 inhibitors: avoid strong inhibitors that may increase drug exposure.
• Pregnancy and lactation: contraindicated unless benefits outweigh risks; discuss with physician.
• Store at room temperature: keep in the original container, protect from moisture and direct sunlight.

Nilotinib may interact with several concomitant medications, necessitating dose adjustments or avoidance.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): may markedly increase plasma levels.
• QT‑prolonging agents (e.g., amiodarone, sotalol): additive risk of arrhythmia.
• Antacids containing aluminum or magnesium: reduce absorption if taken simultaneously.
• St. John's wort: potent CYP3A4 inducer, reduces efficacy.
• Proton pump inhibitors: may affect gastric pH and drug dissolution.

Moderate Interactions (Monitor Closely)

• Moderate CYP3A4 inhibitors (e.g., fluconazole): may require dose reduction.
• Diuretics (e.g., furosemide): monitor electrolytes and QT interval.
• Anticoagulants (e.g., warfarin): observe for altered coagulation parameters.
• Statins metabolized by CYP3A4 (e.g., simvastatin): assess for myopathy risk.
• Glucose‑lowering agents: watch for enhanced hypoglycemic effect.