Nilotinib Zentiva (Nilotinib)

Nilotinib is a targeted therapy that inhibits BCR‑ABL tyrosine kinase activity in chronic myeloid leukemia.

• Chronic phase chronic myeloid leukemia (CML): helps achieve deeper molecular response and prolongs progression‑free survival in adult patients.
• Accelerated phase CML: provides disease control when prior tyrosine kinase inhibitor therapy has failed.

• Nilotinib selectively binds to the ATP‑binding site of the BCR‑ABL fusion protein and other kinases such as KIT and PDGFR, preventing phosphorylation of downstream substrates. This blockade halts proliferative signaling pathways that drive the growth of Philadelphia chromosome‑positive leukemic cells, leading to cell cycle arrest and apoptosis of malignant clones.

Common Side Effects

• Nausea: mild to moderate upset stomach often occurring early in therapy.
• Diarrhea: loose stools that may be transient or persistent.
• Rash: skin erythema or pruritus, usually mild.
• Fatigue: generalized tiredness without specific cause.

Serious or Rare Side Effects

• QT interval prolongation: may predispose to ventricular arrhythmias.
• Pancreatitis: acute inflammation of the pancreas with abdominal pain.
• Severe hepatic toxicity: marked elevation of liver enzymes or hepatitis.
• Neutropenia: significant reduction in white blood cells increasing infection risk.
• Arterial occlusive events: rare cases of ischemic heart disease or peripheral vascular disease.
• Stevens‑Johnson syndrome: severe skin reaction requiring immediate medical attention.

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

• Cardiac monitoring: obtain baseline ECG and repeat periodically to detect QT prolongation.
• Hepatic function: assess liver enzymes before initiation and during therapy.
• Hematologic surveillance: perform regular complete blood counts to identify neutropenia or thrombocytopenia.
• Drug interactions: avoid concomitant strong CYP3A4 inhibitors and other QT‑prolonging agents.
• Cardiovascular risk: use caution in patients with a history of arrhythmia, ischemic heart disease, or uncontrolled hypertension.
• Store at ambient temperature: keep below 25 °C in the original container, protect from moisture and direct sunlight.

Nilotinib may interact with several medicines, requiring dose adjustments or avoidance.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole): may increase nilotinib plasma concentrations and toxicity.
• QT‑prolonging drugs (e.g., amiodarone, sotalol): additive risk of cardiac arrhythmias.
• Antacids containing aluminum or magnesium: can reduce nilotinib absorption if taken simultaneously.

Moderate Interactions (Monitor Closely)

• CYP3A4 inducers (e.g., rifampin, carbamazepine): may lower nilotinib exposure, reducing efficacy.
• Warfarin: may require more frequent INR monitoring.
• Statins metabolized by CYP3A4 (e.g., simvastatin): monitor for myopathy and consider dose reduction.
• Proton pump inhibitors: may modestly affect nilotinib absorption; assess clinical response.