Nilotinib Zentiva (Nilotinib)

Nilotinib is a targeted therapy that inhibits BCR‑ABL tyrosine kinase activity in certain leukemias.

• Chronic Myeloid Leukemia (CML) – chronic phase: Reduces malignant cell proliferation and achieves disease control.
• Chronic Myeloid Leukemia (CML) – accelerated phase: Provides an additional therapeutic option when resistance to first‑line TKIs occurs.
• Philadelphia chromosome‑positive Acute Lymphoblastic Leukemia (Ph+ ALL): Improves remission rates by blocking BCR‑ABL signaling.

• Nilotinib binds to the ATP‑binding site of the BCR‑ABL fusion protein, preventing its kinase activity. This inhibition blocks downstream signaling pathways that drive uncontrolled proliferation of leukemic cells. The drug also suppresses KIT and PDGFR kinases, contributing to its antineoplastic effects in BCR‑ABL‑positive malignancies.

Common Side Effects

• Nausea: mild to moderate gastrointestinal upset.
• 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 interval prolongation: may predispose to cardiac arrhythmias.
• Pancreatitis: inflammation of the pancreas.
• Severe hepatic injury: elevated liver enzymes or hepatitis.
• Neutropenia: marked reduction in neutrophil count.
• Thrombocytopenia: low platelet levels increasing bleeding risk.
• Cardiovascular events: myocardial infarction or stroke.

Before initiating therapy, clinicians should assess baseline cardiac function and electrolyte status.

• Cardiac monitoring: perform ECG and correct electrolyte imbalances.
• Hematologic monitoring: regular complete blood counts to detect neutropenia or thrombocytopenia.
• Hepatic monitoring: periodic liver function tests.
• Drug interactions: avoid concomitant use of strong CYP3A4 inhibitors or QT‑prolonging agents.
• Pregnancy safety: contraindicated in pregnancy (Category D); use effective contraception.
• Store at room temperature: keep in the original container, protect from moisture and direct sunlight.

Nilotinib may interact with several drug classes, requiring careful management.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): increase nilotinib exposure.
• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine): reduce therapeutic levels.
• QT‑prolonging agents (e.g., amiodarone, sotalol): heighten risk of arrhythmia.

Moderate Interactions (Monitor Closely)

• Moderate CYP3A4 inhibitors (e.g., erythromycin): may modestly raise concentrations.
• Moderate CYP3A4 inducers (e.g., phenobarbital): may modestly lower concentrations.
• Warfarin: monitor INR for potential anticoagulant effect changes.
• Statins (e.g., simvastatin): assess for increased statin exposure and muscle toxicity.