Nilotinib

Nilotinib is used to treat chronic myeloid leukemia by targeting the BCR‑ABL tyrosine kinase pathway.

• Chronic myeloid leukemia – chronic phase: Achieves hematologic and cytogenetic remission by suppressing leukemic cell proliferation.
• Chronic myeloid leukemia – accelerated phase: Controls disease progression and improves survival when used after intolerance or resistance to prior therapy.
• Chronic myeloid leukemia – blast crisis: Provides disease control in the aggressive blast phase, often as part of combination regimens.

• Nilotinib selectively inhibits the BCR‑ABL tyrosine kinase as well as related kinases such as KIT and PDGFR. By binding to the ATP‑binding site of these enzymes, it blocks downstream signaling cascades that drive proliferation and survival of leukemic cells, leading to apoptosis and reduced disease burden with sustained pathway suppression.

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

Common Side Effects

• Rash: mild to moderate skin eruptions that may be itchy or erythematous.
• Nausea: occasional gastrointestinal upset, often transient and manageable with anti‑emetics.
• Diarrhea: loose stools that can vary from mild to moderate severity.
• Elevated liver enzymes: mild increases in ALT and AST, usually reversible upon monitoring.

Serious or Rare Side Effects

• Cardiovascular events: includes arterial occlusive disease, hypertension, and rare cases of myocardial infarction.
• Pancreatitis: inflammation of the pancreas presenting with abdominal pain, nausea and elevated amylase.
• Severe hypersensitivity: rare reactions such as Stevens‑Johnson syndrome or toxic epidermal necrolysis requiring immediate medical attention.

When prescribing Nilotinib, clinicians should consider several precautionary measures to ensure safe use.

• Dose adjustment: required in patients with hepatic impairment or severe renal dysfunction.
• Cardiac monitoring: baseline and periodic ECGs are advised due to risk of QT prolongation.
• Electrolyte balance: correct potassium and magnesium levels before initiating therapy to reduce cardiac risk.
• Drug interactions: avoid concomitant use with strong CYP3A4 inhibitors or inducers without dose modification.
• Pregnancy and lactation: contraindicated in pregnancy; women of childbearing potential should use effective contraception.
• 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 markedly raise Nilotinib levels, increasing risk of serious adverse events such as QT prolongation.
• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine): can substantially lower drug exposure, reducing efficacy.
• Antacids containing aluminum or magnesium: reduce absorption if taken simultaneously.

Moderate Interactions (Monitor Closely)

• Proton pump inhibitors: may decrease bioavailability; spacing doses can mitigate effect.
• Statins metabolized by CYP3A4 (e.g., simvastatin): increased risk of statin‑related muscle toxicity.
• Anticoagulants (e.g., warfarin): may require closer INR monitoring due to potential interaction.