Nilosure, containing the active ingredient Nilotinib, is a tyrosine kinase inhibitor used primarily in the treatment of chronic myeloid leukemia (CML). Nilotinib targets and inhibits the BCR-ABL protein, which drives the growth of cancerous cells in CML.

Uses

• Treatment of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in adults in both chronic and accelerated phases.

• Used when resistance or intolerance to prior therapy, including imatinib, occurs.

Mechanism of Action

Nilotinib works by selectively inhibiting the BCR-ABL tyrosine kinase, preventing the proliferation of leukemic cells. It also targets other kinases like KIT and PDGFR.

Onset of Action

The onset of action of Nilotinib varies but is generally observed within the first 2 to 4 weeks of treatment.

Duration of Action

The drug’s effects last as long as it is taken consistently, as prescribed.

Dosage

• Chronic Phase CML: 300 mg orally twice daily.

• Accelerated Phase CML: 400 mg orally twice daily.

• The tablets should be taken on an empty stomach, avoiding food 2 hours before and 1 hour after the dose.

Side Effects

Common side effects include:

• Headache

• Nausea and vomiting

• Diarrhea

• Rash

• Fatigue

Serious side effects may include:

• Cardiac complications (QT prolongation)

• Pancreatitis

• Hepatic impairment

Precautions

• Regular monitoring of blood counts and heart function is necessary.

• Avoid grapefruit juice as it may increase drug levels.

• Use with caution in patients with liver dysfunction.

Contraindications

• Hypersensitivity to Nilotinib or any component of the formulation.

• Patients with hypokalemia, hypomagnesemia, or long QT syndrome.

Drug Interactions

• Strong CYP3A4 inhibitors (e.g., ketoconazole) may increase Nilotinib levels.

• CYP3A4 inducers (e.g., rifampin) may reduce its effectiveness.

Pregnancy and Lactation

• Not recommended during pregnancy due to potential harm to the fetus.

• Breastfeeding should be avoided.