Nilotinib Stada 50 Mg Tvrdé Tobolky (Nilotinib)

Nilotinib is a targeted therapy that inhibits the BCR‑ABL tyrosine kinase pathway in chronic myeloid leukemia.

• Chronic Myeloid Leukemia (chronic phase): reduces leukemic cell proliferation and achieves disease control.
• Chronic Myeloid Leukemia (accelerated phase): helps achieve hematologic and cytogenetic responses.
• Chronic Myeloid Leukemia (blast crisis): used as part of combination therapy to improve remission rates.
• Imatinib‑resistant or intolerant CML: provides an alternative kinase inhibition strategy to restore therapeutic response.

• Nilotinib selectively binds to the ATP‑binding site of the BCR‑ABL fusion protein, stabilizing its inactive conformation and preventing phosphorylation of downstream substrates. By blocking this constitutively active tyrosine kinase, the drug halts proliferative signaling pathways such as RAS/MAPK and PI3K/AKT, leading to apoptosis of leukemic cells and inhibition of disease progression.

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

Common Side Effects

• Rash: mild skin irritation or erythema.
• Nausea: occasional upset stomach.
• Diarrhea: loose stools.
• Fatigue: general tiredness.
• Elevated liver enzymes: mild transaminase increase.
• Muscle cramps: intermittent leg or calf cramps.

Serious or Rare Side Effects

• Cardiovascular events: myocardial infarction or ischemic heart disease.
• QT interval prolongation: risk of serious arrhythmia.
• Pancreatitis: inflammation of the pancreas.
• Severe hepatic toxicity: marked elevation of liver enzymes or hepatitis.
• Severe neutropenia: dangerously low white blood cell count.
• Tumor lysis syndrome: rapid breakdown of malignant cells.

When prescribing nilotinib, clinicians should consider several safety measures and patient‑specific factors.

• Cardiac assessment: evaluate baseline ECG and cardiovascular risk before initiating therapy.
• Hepatic function: monitor liver enzymes regularly during treatment.
• Electrolyte balance: correct hypokalemia, hypomagnesemia, and hypocalcemia to reduce QT prolongation risk.
• Drug interactions: avoid concomitant use of strong CYP3A4 inhibitors or inducers without dose adjustment.
• Pregnancy and lactation: contraindicated; advise effective contraception and discuss risks with women of childbearing potential.
• 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.
• Strong CYP3A4 inducers (e.g., rifampicin, carbamazepine): can markedly reduce nilotinib exposure, compromising efficacy.
• Antacids containing aluminum or magnesium: decrease absorption if taken concurrently.

Moderate Interactions (Monitor Closely)

• Proton pump inhibitors (e.g., omeprazole): may reduce nilotinib bioavailability; separate dosing recommended.
• Statins metabolized by CYP3A4 (e.g., simvastatin, atorvastatin): increased risk of myopathy; consider dose adjustment.
• Anticoagulants (e.g., warfarin): monitor INR as nilotinib may affect coagulation parameters.