Erlotinib

Generic Details

Generic Name

Erlotinib

Other Names

  • Tarceva

Drug Class

  • Tyrosine Kinase Inhibitor

Chemical Formula

C22H23N3O4

Molecular Weight

393.44 g/mol

Mechanism of Action

  • Inhibits the tyrosine kinase activity of the epidermal growth factor receptor (EGFR)

Indications

  • Non-small cell lung cancer
  • Pancreatic cancer

Common Dosage Forms

  • Tablet

Typical Dosage

  • 150mg/day on an empty stomach

Pediatric Dosage

    Geriatric Dosage

      Side Effects

      • Rash
      • Diarrhea
      • Fatigue
      • Anorexia
      • Nausea
      • Vomiting

      Contraindications

      • Hypersensitivity to erlotinib or any component of the formulation

      Pregnancy Category

      • Category D - Positive evidence of risk

      Lactation Safety

      • Lactation not recommended due to potential serious adverse reactions in breastfed infants

      Drug Interactions

      • Strong CYP3A4 inducers/inhibitors

      Overdose Symptoms

      • Diarrhea
      • Rash
      • Fatigue

      Antidote for Overdose

        Storage Conditions

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

        Pharmacokinetics

        • Absorption: Oral bioavailability: ~60%
        • Distribution: Highly protein bound (95%)
        • Metabolism: Primarily by CYP3A4
        • Excretion: Fecal (83%) and renal (13%)

        Precautions

        • Interstitial lung disease
        • Hepatic impairment

        Warnings

        • Risk of severe skin reactions
        • GI perforation

        Others

        • Avoid concomitant use of proton pump inhibitors (PPIs)