Nilotinib Zentiva (Nilotinib)

Nilotinib targets the BCR‑ABL tyrosine‑kinase pathway and is used in the management of chronic myeloid leukemia.

• Chronic myeloid leukemia (chronic phase): reduces leukemic cell proliferation and improves survival.
• Philadelphia‑positive CML after imatinib resistance: provides an alternative targeted therapy.
• Maintenance therapy for patients who have achieved a molecular response: helps sustain remission.

• Nilotinib selectively inhibits the BCR‑ABL tyrosine kinase, blocking its ATP‑binding site and preventing downstream signaling that drives uncontrolled proliferation of leukemic cells. By halting this pathway, the drug induces apoptosis and reduces the growth of malignant clones in chronic myeloid leukemia.

Nilotinib may cause a range of adverse reactions, which are categorized by frequency and severity.

Common Side Effects

• Nausea: mild to moderate stomach upset.
• Diarrhea: loose stools that may require fluid replacement.
• Rash: skin irritation or erythema.
• Elevated liver enzymes: mild transaminase increase.
• Fatigue: generalized tiredness.
• Headache: occasional throbbing pain.

Serious or Rare Side Effects

• Cardiovascular events: myocardial infarction or arterial occlusion.
• Pancreatitis: severe abdominal pain with elevated enzymes.
• Severe hepatic dysfunction: marked elevation of liver enzymes or jaundice.
• QT interval prolongation: risk of arrhythmia requiring ECG monitoring.

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

• Cardiac assessment: baseline ECG and periodic monitoring for QT prolongation.
• Liver function: check transaminases before start and during treatment.
• Pancreatic enzymes: monitor amylase and lipase if abdominal symptoms arise.
• Drug interactions: review concomitant medications that affect CYP3A4.
• Pregnancy and lactation: avoid use unless benefits outweigh risks; discuss with specialist.

Store at ambient temperature: keep in original container, protect from moisture and direct sunlight.

Nilotinib interacts with several agents that can alter its plasma concentration or increase toxicity.

Major Interactions (Avoid)

• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine): markedly reduce nilotinib exposure.
• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): significantly increase nilotinib levels and risk of QT prolongation.
• Antacids containing aluminum or magnesium: may decrease absorption if taken simultaneously.

Moderate Interactions (Monitor Closely)

• Proton pump inhibitors: may modestly reduce absorption; separate dosing by at least 2 hours.
• Statins metabolized by CYP3A4 (e.g., simvastatin): may increase statin exposure; consider dose adjustment.
• Anticoagulants (warfarin): monitor INR more frequently due to potential interaction.