Ceritinib

Generic Details

Generic Name

Ceritinib

Other Names

  • Zykadia

Drug Class

  • Anaplastic lymphoma kinase (ALK) inhibitor

Chemical Formula

C28H36ClN5O3S

Molecular Weight

558.14 g/mol

Mechanism of Action

  • Inhibits anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1)

Indications

  • Treatment of ALK-positive metastatic non-small cell lung cancer (NSCLC)

Common Dosage Forms

  • Capsule

Typical Dosage

  • 750 mg orally once daily on an empty stomach

Pediatric Dosage

  • Safety and efficacy not established in children

Geriatric Dosage

  • Dosage adjustments may be needed based on individual patient factors

Side Effects

  • Nausea
  • Diarrhea
  • Vomiting
  • Fatigue
  • Liver enzyme elevation
  • Constipation

Contraindications

  • Hypersensitivity to ceritinib

Pregnancy Category

  • Category D - Risk of fetal harm, use only if potential benefit justifies potential risk to the fetus

Lactation Safety

  • Not recommended to breastfeed during treatment

Drug Interactions

  • Strong CYP3A inhibitors/inducers
  • Proton pump inhibitors
  • QT-prolonging drugs

Overdose Symptoms

  • Nausea
  • Vomiting
  • Fatigue
  • Liver toxicity

Antidote for Overdose

  • There is no specific antidote, provide supportive care

Storage Conditions

  • Store at room temperature (20-25°C), excursions permitted between 15-30°C

Pharmacokinetics

  • Absorption: Rapidly absorbed
  • Distribution: Highly distributed into tissues
  • Metabolism: Primarily hepatic by CYP3A4
  • Excretion: Mainly excreted through feces

Precautions

  • Monitor liver function tests regularly
  • Monitor for interstitial lung disease
  • Cardiac monitoring for QT prolongation

Warnings

  • Hepatotoxicity
  • Interstitial lung disease
  • Bradycardia and QT prolongation
  • Hyperglycemia

Others

  • Patients should be advised to avoid grapefruit and Seville oranges during treatment due to potential drug interactions