Nilotinib Zentiva (Nilotinib)

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

• Chronic myeloid leukemia (chronic phase): reduces leukemic cell proliferation and improves long‑term survival.
• Chronic myeloid leukemia (accelerated phase): achieves hematologic and cytogenetic responses in patients with disease progression.
• Chronic myeloid leukemia (blast phase): provides disease control when combined with appropriate chemotherapy.

• Nilotinib binds competitively to the ATP‑binding site of the BCR‑ABL fusion protein, inhibiting its tyrosine kinase activity. By preventing phosphorylation of downstream substrates, the drug blocks signaling pathways that promote proliferation and survival of leukemic cells. The inhibition also extends to related kinases such as KIT and PDGFR, contributing to its antineoplastic effect in chronic myeloid leukemia.

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

Common Side Effects

• Nausea
• Diarrhea
• Rash or pruritus
• Headache
• Fatigue

Serious or Rare Side Effects

• QT interval prolongation and other cardiac arrhythmias
• Arterial occlusive events (e.g., peripheral arterial disease)
• Severe pancreatitis
• Hepatic toxicity (elevated transaminases, hepatitis)

When prescribing Nilotinib, clinicians should observe several safety precautions to minimize risks.

• Cardiovascular monitoring: obtain baseline ECG and monitor QT interval regularly due to risk of prolongation.
• Hepatic function: assess liver enzymes before initiation and periodically during therapy.
• Electrolyte balance: correct hypokalemia, hypomagnesemia, and hypocalcemia to reduce cardiac risk.
• Drug interactions: avoid concomitant use with strong CYP3A4 inhibitors and adjust doses of interacting agents.
• Pregnancy and lactation: contraindicated unless benefits outweigh risks; discuss with patient.
• Store at ambient temperature: keep tablets below 25 °C in the original container, protected from moisture and light.

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

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): may raise nilotinib levels and heighten adverse effects.
• Proton pump inhibitors and antacids taken within 2 hours of nilotinib: reduce absorption and diminish efficacy.
• Concomitant use with other BCR‑ABL inhibitors: increases risk of overlapping toxicities.

Moderate Interactions (Monitor Closely)

• CYP3A4 inducers (e.g., rifampin, carbamazepine): may lower nilotinib exposure, reducing effectiveness.
• Anticoagulants such as warfarin: nilotinib can affect INR, requiring closer monitoring.
• Statins metabolized by CYP3A4 (e.g., simvastatin): may increase statin concentrations, monitor for myopathy.