Nilotinib Zentiva (Nilotinib)

Nilotinib targets the BCR‑ABL tyrosine kinase pathway that drives chronic myeloid leukemia and related disease phases.

• Chronic phase CML: achieves hematologic and cytogenetic remission.
• Accelerated phase CML: reduces disease progression and improves survival.
• Blast phase CML: provides disease control when combined with other therapies.

• Nilotinib selectively binds to the ATP‑binding site of the BCR‑ABL fusion protein, inhibiting its tyrosine kinase activity. This blockade prevents downstream signaling that promotes leukemic cell proliferation and survival, leading to apoptosis of malignant cells while sparing most normal cells.

Nilotinib may cause a range of adverse reactions that vary in frequency and severity.

Common Side Effects

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

Serious or Rare Side Effects

• QT interval prolongation: may predispose to cardiac arrhythmias.
• Pancreatitis: abdominal pain with elevated enzymes.
• Severe hepatic injury: marked elevation of liver transaminases.
• Neutropenia: significant reduction in white blood cells.
• Thrombocytopenia: low platelet counts increasing bleeding risk.
• Stevens‑Johnson syndrome: severe skin and mucosal reactions.

Before initiating therapy, clinicians should assess patient-specific risk factors and monitor relevant parameters.

• Cardiac monitoring: obtain baseline ECG and periodically assess QT interval.
• Hepatic function: check liver enzymes before and during treatment.
• Pancreatic enzymes: monitor amylase and lipase regularly.
• Drug interactions: avoid concurrent strong CYP3A4 inhibitors.
• Pregnancy and lactation: risk unknown; avoid use in pregnant or breastfeeding women.
• Store at ambient temperature: keep in original container, protect from moisture and light.

Nilotinib interacts with several drug classes; careful review of concomitant medications is essential.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): may increase nilotinib exposure.
• QT‑prolonging agents (e.g., amiodarone, sotalol): additive risk of cardiac arrhythmia.
• Antacids containing aluminum or magnesium: reduce nilotinib absorption.

Moderate Interactions (Monitor Closely)

• CYP3A4 inducers (e.g., rifampin, carbamazepine): may lower nilotinib levels.
• Warfarin: potential alteration of anticoagulant effect.
• Statins metabolized by CYP3A4 (e.g., simvastatin): monitor for myopathy.
• Diuretics causing electrolyte shifts: watch for enhanced QT prolongation.
• Other tyrosine kinase inhibitors: assess cumulative toxicity.