Nilotinib Stada 200 Mg Tvrdé Tobolky (Nilotinib)

Nilotinib is indicated for diseases driven by the BCR‑ABL tyrosine kinase, most notably chronic myeloid leukemia.

• Chronic phase CML: reduces leukemic cell proliferation and achieves hematologic and cytogenetic responses.
• Accelerated phase CML: provides disease control when prior therapy is insufficient.
• Blast phase CML: offers targeted inhibition of BCR‑ABL in advanced disease stages.
• CML resistant to prior tyrosine kinase inhibitors: offers an alternative therapeutic option for patients with inadequate response.

• Nilotinib selectively binds to the ATP‑binding site of the BCR‑ABL fusion protein, inhibiting its tyrosine kinase activity. By blocking phosphorylation of downstream substrates, it prevents uncontrolled cell proliferation and induces apoptosis in leukemic cells. The drug also inhibits the related kinases KIT and PDGFR, contributing to its antineoplastic effect in chronic myeloid leukemia. This targeted inhibition restores normal hematopoiesis and reduces disease burden over time.

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, often transient.
• Rash: skin eruptions that may be pruritic.
• Fatigue: generalized tiredness.
• Headache: mild to moderate intensity.
• Elevated lipase: asymptomatic increase in pancreatic enzymes.
• Myalgia: muscle aches.
• Peripheral edema: swelling of limbs.

Serious or Rare Side Effects

• QT interval prolongation: can lead to cardiac arrhythmias.
• Pancreatitis: severe abdominal pain with elevated enzymes.
• Hepatotoxicity: significant increase in liver transaminases.
• Arterial occlusive events: risk of ischemic heart disease or peripheral arterial disease.
• Severe hypersensitivity: including Stevens‑Johnson syndrome.
• Severe neutropenia: low white blood cell count.
• Thromboembolic events: deep vein thrombosis or pulmonary embolism.

When prescribing nilotinib, clinicians should observe several safety precautions to minimize risk.

• Cardiac monitoring: obtain baseline ECG and monitor QT interval regularly.
• Blood glucose assessment: monitor fasting glucose and HbA1c due to hyperglycemia risk.
• Liver function tests: check ALT, AST, and bilirubin before and during therapy.
• Avoid strong CYP3A4 inhibitors: concomitant use can increase nilotinib exposure.
• Caution in cardiovascular disease: assess history of ischemic events before initiation.
• Store at room temperature: keep tablets in original container, protect from moisture and light.

Nilotinib interacts with several medicines; understanding the interaction level guides clinical management.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): markedly increase nilotinib plasma concentrations.
• QT‑prolonging agents (e.g., amiodarone, sotalol): elevate risk of serious cardiac arrhythmias.
• Antacids raising gastric pH (e.g., aluminum‑magnesium hydroxide): significantly reduce nilotinib absorption.

Moderate Interactions (Monitor Closely)

• Moderate CYP3A4 inducers (e.g., rifampin, carbamazepine): may lower nilotinib effectiveness.
• Statins metabolized by CYP3A4 (e.g., simvastatin, lovastatin): increased risk of statin toxicity.
• Warfarin: potential alteration of INR, requiring closer coagulation monitoring.
• Digoxin: possible increase in serum levels, necessitating dose adjustment.