Nilotinib Stada 50 Mg Cápsulas (Nilotinib)

Nilotinib is employed in the management of BCR‑ABL positive leukemias, primarily chronic myeloid leukemia.

• Chronic phase CML: first‑line treatment for newly diagnosed adult patients, improving molecular response rates.
• Accelerated phase CML: therapy for patients who have progressed or are resistant to prior tyrosine‑kinase inhibitors.
• Blast phase CML: used as part of combination regimens in advanced disease to achieve cytogenetic remission.

• Nilotinib selectively inhibits the BCR‑ABL tyrosine kinase by binding to its ATP‑binding site, preventing phosphorylation of downstream substrates. This blockade halts the proliferative signaling cascade that drives leukemic cell growth and survival. The drug also exhibits activity against related kinases such as KIT and PDGFR, contributing to its antineoplastic effect in BCR‑ABL positive malignancies. By maintaining inhibition over prolonged periods, nilotinib sustains suppression of malignant clones.

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

Common Side Effects

• Nausea: mild to moderate gastrointestinal upset.
• Diarrhea: loose stools that may require hydration.
• Rash: skin irritation or erythema.
• Fatigue: general tiredness affecting daily activities.

Serious or Rare Side Effects

• QT interval prolongation: may lead to potentially life‑threatening cardiac arrhythmia.
• Pancreatitis: inflammation of the pancreas presenting with abdominal pain.
• Severe hepatic injury: marked elevation of liver enzymes and possible liver failure.
• Severe neutropenia: significant reduction in white blood cells increasing infection risk.

When prescribing nilotinib, clinicians should observe several precautionary measures to minimize risks.

• Cardiac monitoring: obtain baseline ECG and repeat periodically because of QT prolongation risk.
• Liver function: assess hepatic enzymes before initiation and during therapy to detect toxicity.
• Electrolyte balance: correct potassium and magnesium levels to reduce the likelihood of cardiac events.
• Drug interactions: avoid concomitant use of strong CYP3A4 inhibitors or other QT‑prolonging agents.
• Pregnancy and lactation: drug may cause fetal harm; avoid use in pregnant or breastfeeding women.
• Store at ambient temperature: keep below 25 °C, protect from moisture and light in the original packaging.

Nilotinib is metabolized primarily by CYP3A4, making it susceptible to several clinically important drug interactions.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): increase nilotinib plasma concentrations and toxicity risk.
• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine): decrease nilotinib exposure, potentially reducing efficacy.
• QT‑prolonging drugs (e.g., amiodarone, sotalol): additive effect on cardiac repolarization leading to arrhythmias.

Moderate Interactions (Monitor Closely)

• Antacids or proton pump inhibitors: may reduce nilotinib absorption; separate dosing by at least two hours.
• Warfarin: potential alteration of anticoagulant effect; monitor INR closely.