Nilotinib Zentiva K.S. (Nilotinib)

Nilotinib is a targeted tyrosine kinase inhibitor used in the management of chronic myeloid leukemia.

• Chronic myeloid leukemia (chronic phase): Reduces leukemic cell proliferation and improves long‑term survival.
• Chronic myeloid leukemia (accelerated phase): Controls disease progression and helps achieve hematologic response.
• Chronic myeloid leukemia (blast phase): Provides therapeutic benefit when combined with other agents in advanced disease.

• Nilotinib selectively inhibits the BCR‑ABL tyrosine kinase, a fusion protein that drives uncontrolled cell growth in Philadelphia chromosome‑positive leukemias. By binding to the ATP‑binding site of BCR‑ABL, it blocks downstream signaling pathways such as RAS‑RAF‑MEK‑ERK and PI3K‑AKT, thereby halting proliferation and inducing apoptosis of malignant cells.

Nilotinib may cause a range of adverse reactions, varying from mild to severe.

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 prolongation: cardiac repolarization abnormality that can lead to arrhythmia.
• Pancreatitis: inflammation of the pancreas, presenting with abdominal pain.
• Severe hepatic injury: marked elevation of liver enzymes or jaundice.
• Severe neutropenia or thrombocytopenia: dangerously low white blood cells or platelets.
• Anaphylactic reactions: rare but potentially life‑threatening hypersensitivity.

When prescribing Nilotinib, clinicians should observe several safety measures to minimize risk.

• ECG monitoring: Perform baseline and periodic ECGs to detect QT prolongation.
• Liver function tests: Monitor hepatic enzymes regularly for signs of toxicity.
• Hematologic monitoring: Check complete blood counts to identify neutropenia or thrombocytopenia.
• Pregnancy avoidance: Do not use in pregnant women; advise effective contraception.
• Store at below 25°C: Keep in original packaging, protect from moisture and light.

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

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole): Can markedly increase Nilotinib levels, raising risk of QT prolongation.
• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine): May reduce drug exposure, compromising efficacy.
• QT‑prolonging agents (e.g., amiodarone, sotalol): Additive effect on cardiac repolarization.

Moderate Interactions (Monitor Closely)

• Moderate CYP3A4 inhibitors (e.g., erythromycin, fluconazole): May require dose adjustment.
• Statins metabolized by CYP3A4 (e.g., simvastatin, atorvastatin): Increased risk of myopathy; consider alternative statin.
• Antacids containing aluminum or magnesium: Can reduce absorption; separate administration by at least 2 hours.