Osimertinib

Generic Details

Generic Name

Osimertinib

Other Names

  • Tagrisso

Drug Class

  • Tyrosine Kinase Inhibitor

Chemical Formula

C28H33N7O2S

Molecular Weight

499.67 g/mol

Mechanism of Action

  • Inhibits the activity of epidermal growth factor receptor (EGFR) tyrosine kinase by binding to the ATP-binding site of the enzyme, resulting in the inhibition of EGFR signaling pathways.

Indications

  • Non-small cell lung cancer (NSCLC) with EGFR T790M mutation

Common Dosage Forms

  • Tablet

Typical Dosage

  • 80mg once daily

Pediatric Dosage

  • Not established

Geriatric Dosage

  • Adjust dosage based on individual tolerability

Side Effects

  • Diarrhea
  • Skin rash
  • Nausea
  • Fatigue
  • Decreased appetite

Contraindications

  • Hypersensitivity to osimertinib

Pregnancy Category

  • Category D

Lactation Safety

  • Not recommended during lactation

Drug Interactions

  • Strong CYP3A inducers or inhibitors may affect serum concentrations of osimertinib

Overdose Symptoms

  • Nausea
  • Vomiting
  • Diarrhea
  • Rash
  • Fatigue

Antidote for Overdose

  • There is no specific antidote, treatment should be supportive

Storage Conditions

  • Store at room temperature, protect from light and moisture

Pharmacokinetics

  • Absorption: Well absorbed orally
  • Distribution: Highly bound to plasma proteins
  • Metabolism: Primarily hepatic via CYP3A4
  • Excretion: Mainly through feces and urine

Precautions

  • Monitor for interstitial lung disease
  • Cardiomyopathy
  • Electrolyte abnormalities

Warnings

  • Interstitial lung disease
  • QTc interval prolongation
  • Cardiomyopathy risk

Others

  • Osimertinib is a targeted therapy used for specific types of lung cancer.