Brigatinib

Generic Details

Generic Name

Brigatinib

Other Names

  • Brigatinib sulfate

Drug Class

  • Antineoplastic agent
  • Tyrosine kinase inhibitor

Chemical Formula

C29H39ClN7O2S

Molecular Weight

584.19 g/mol

Mechanism of Action

  • Inhibits anaplastic lymphoma kinase (ALK)
  • Inhibits receptor tyrosine kinase (RTK)

Indications

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

Common Dosage Forms

  • Tablet

Typical Dosage

  • 90 mg orally once daily for 7 days, then 180 mg orally once daily

Pediatric Dosage

    Geriatric Dosage

    • Use with caution, no specific dosage adjustments recommended

    Side Effects

    • Fatigue
    • Nausea
    • Diarrhea
    • Cough
    • Increased blood creatinine levels
    • Pulmonary embolism

    Contraindications

    • Hypersensitivity to brigatinib or any component of the formulation

    Pregnancy Category

    • Category D - Positive evidence of risk
    • Avoid use in pregnancy

    Lactation Safety

    • Not recommended to breastfeed during treatment with brigatinib

    Drug Interactions

    • Strong CYP3A inhibitors can increase brigatinib levels
    • Strong CYP3A inducers can decrease brigatinib levels

    Overdose Symptoms

    • Bradycardia
    • Hypertension
    • Fatigue
    • Nausea

    Antidote for Overdose

    • No specific antidote, manage symptoms and provide supportive care

    Storage Conditions

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

    Pharmacokinetics

    • Absorption: Well absorbed orally, peak plasma concentrations reached in 4 hours
    • Distribution: Extensively distributed in tissues
    • Metabolism: Metabolized in the liver primarily by CYP2C8 and CYP3A4
    • Excretion: Mainly excreted in feces and urine

    Precautions

    • Monitor for interstitial lung disease
    • Monitor for hypertension
    • Monitor for cardiac function

    Warnings

    • Risk of interstitial lung disease
    • Hypertension
    • Bradycardia
    • Pulmonary embolism

    Others

    • Regular monitoring of liver function tests recommended during treatment