Nilotinib Teva (Nilotinib Hydrochloride Dihydrate)

Nilotinib is a tyrosine kinase inhibitor used in the management of Philadelphia chromosome‑positive chronic myeloid leukemia.

• Chronic myeloid leukemia (chronic phase): improves hematologic and cytogenetic response in adult patients.
• Chronic myeloid leukemia (accelerated phase): achieves disease control and prolongs survival.
• Chronic myeloid leukemia (blast phase): provides therapeutic benefit when combined with other agents.

• Nilotinib selectively inhibits the BCR‑ABL tyrosine kinase by binding to its ATP‑binding site, preventing phosphorylation of downstream substrates. This blockade suppresses the signaling pathways that drive proliferation and survival of leukemic cells, leading to apoptosis and reduced disease progression. The drug also exhibits activity against several other kinases, including KIT and PDGFR, contributing to its antineoplastic profile and enhances the effectiveness of concurrent chemotherapy.

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

Common Side Effects

• Nausea: mild to moderate upset stomach.
• Diarrhea: loose stools, often transient.
• Rash: skin erythema or pruritus.
• Fatigue: general tiredness.
• Headache: mild cranial discomfort.
• Myalgia: muscle aches.

Serious or Rare Side Effects

• QT interval prolongation: may lead to cardiac arrhythmias.
• Pancreatitis: inflammation of the pancreas with abdominal pain.
• Severe hepatic injury: marked elevation of liver enzymes or hepatitis.
• Severe neutropenia: critically low neutrophil count increasing infection risk.
• Cardiovascular events: ischemic heart disease or peripheral arterial disease.

Before initiating Nilotinib therapy, clinicians should consider several safety measures to minimise risk.

• Cardiac monitoring: assess baseline ECG and correct electrolyte abnormalities.
• Blood count surveillance: perform regular CBC to detect neutropenia or thrombocytopenia.
• Liver function testing: monitor ALT, AST, and bilirubin levels periodically.
• Drug interaction review: avoid concomitant strong CYP3A4 inhibitors and QT‑prolonging agents.
• QT prolongation risk: use caution in patients with known prolonged QT interval or cardiac disease.
• Store at room temperature: keep in original packaging, protect from moisture and direct sunlight.

Nilotinib interacts with several medicines, requiring careful management to avoid reduced efficacy or increased toxicity.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): may raise nilotinib plasma levels.
• QT‑prolonging drugs (e.g., amiodarone, sotalol): increase risk of cardiac arrhythmias.
• Antacids containing aluminum or magnesium: reduce nilotinib absorption.

Moderate Interactions (Monitor Closely)

• CYP3A4 inducers (e.g., rifampin, St. John’s wort): may lower drug exposure.
• Anticoagulants (e.g., warfarin): may require dose adjustment.
• Statins metabolised by CYP3A4 (e.g., simvastatin): monitor for muscle toxicity.