Nilotinib Viatris (Nilotinib)

Nilotinib acts on the BCR‑ABL tyrosine kinase pathway, providing targeted therapy for specific hematologic malignancies.

• Chronic Myeloid Leukemia (chronic phase): reduces leukemic cell proliferation and improves long‑term survival.
• Chronic Myeloid Leukemia (accelerated phase): achieves disease control when used after resistance or intolerance to prior therapy.
• Philadelphia chromosome‑positive Acute Lymphoblastic Leukemia: offers a targeted option to induce remission in Ph+ ALL patients.

• Nilotinib selectively inhibits the BCR‑ABL tyrosine kinase, a fusion protein that drives uncontrolled cell growth in certain leukemias. By binding to the ATP‑binding site of the kinase, it blocks downstream signaling pathways such as RAS‑RAF‑MEK‑ERK and PI3K‑AKT, leading to reduced proliferation and increased apoptosis of malignant cells.

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

Common Side Effects

• Nausea: mild to moderate gastrointestinal upset.
• Diarrhea: loose stools that may require supportive care.
• Rash: skin eruptions ranging from maculopapular to pruritic.
• Headache: transient cranial discomfort.
• Fatigue: generalized tiredness affecting daily activities.
• Myalgia: muscle aches without inflammation.

Serious or Rare Side Effects

• QT interval prolongation: may predispose to ventricular arrhythmias.
• Pancreatitis: inflammation of the pancreas requiring monitoring of serum lipase.
• Severe liver injury: elevated transaminases and bilirubin.
• Grade 3/4 neutropenia: marked reduction in neutrophil count.
• Thrombocytopenia: low platelet levels increasing bleeding risk.
• Stevens‑Johnson syndrome/toxic epidermal necrolysis: severe skin reactions requiring immediate discontinuation.

When prescribing Nilotinib, clinicians should observe several safety considerations to minimize risk.

• Cardiac monitoring: obtain baseline ECG and monitor QT interval during therapy.
• Hepatic function: assess liver enzymes before initiation and periodically thereafter.
• Hematologic surveillance: perform regular complete blood counts to detect cytopenias.
• Drug interactions: avoid concomitant strong CYP3A4 inhibitors and QT‑prolonging agents.
• Pregnancy and lactation: assess risk–benefit; use only if clearly needed.
• Store at ambient temperature: keep below 25 °C in the original container, protect from moisture.

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

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): may increase Nilotinib exposure and toxicity.
• QT‑prolonging drugs (e.g., amiodarone, sotalol): additive risk of cardiac arrhythmias.
• Antacids containing aluminum or magnesium: reduce absorption of Nilotinib.

Moderate Interactions (Monitor Closely)

• Moderate CYP3A4 inhibitors (e.g., fluconazole): may require dose adjustment.
• CYP3A4 inducers (e.g., rifampicin, St. John’s wort): may lower Nilotinib levels.
• Warfarin: monitor INR as Nilotinib can affect anticoagulation control.