Nilotinib

Generic Details

Generic Name

Nilotinib

Other Names

  • Tasigna

Drug Class

  • Tyrosine Kinase Inhibitor (TKI)

Chemical Formula

C28H22F3N7O

Molecular Weight

529.51 g/mol

Mechanism of Action

  • Inhibits BCR-ABL kinase activity

Indications

  • Chronic Myeloid Leukemia (CML)
  • Acute Lymphoblastic Leukemia (ALL)

Common Dosage Forms

  • Capsules

Typical Dosage

  • 300 mg twice daily

Pediatric Dosage

  • Dosage based on body weight and age, under physician supervision

Geriatric Dosage

  • Usually similar to adult dosage, individualized based on health status

Side Effects

  • Nausea
  • Fatigue
  • Skin Rash
  • Headache
  • Low Blood Counts
  • Liver Problems

Contraindications

  • Hypersensitivity to nilotinib
  • Strong CYP3A4 inhibitors/inducers

Pregnancy Category

  • D - Positive evidence of risk

Lactation Safety

  • Not recommended during breastfeeding, may harm the infant

Drug Interactions

  • Strong CYP3A4 inducers/inhibitors
  • Antacids
  • St. John's Wort

Overdose Symptoms

  • Nausea
  • Vomiting
  • Abdominal Pain
  • Myelosuppression

Antidote for Overdose

  • No specific antidote, manage symptoms and provide supportive care

Storage Conditions

  • Store at room temperature (20-25°C)
  • Protect from light and moisture

Pharmacokinetics

  • Absorption: Variable, taken with food increases bioavailability
  • Distribution: Extensively distributed, protein-bound
  • Metabolism: Primarily hepatic via CYP3A4
  • Excretion: Mainly feces

Precautions

  • Cardiac monitoring due to QT prolongation risk
  • Monitor liver function tests regularly

Warnings

  • Risk of myelosuppression
  • Sudden cardiac death potential with QT prolongation

Others

  • Regular monitoring of blood counts and ECG recommended