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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Anaplastic lymphoma kinase (ALK) inhibitors
brigatinib
L01ED04
Forms & Strengths
- Oral tablets: 30 mg
- Oral tablets: 90 mg
- Oral tablets: 180 mg
Adult Dosing
- Initial dose: 90 mg orally once daily for the first 7 days
- Maintenance dose: If 90 mg is tolerated, increase to 180 mg orally once daily
- Take with or without food; swallow whole without crushing or chewing
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) as detected by an FDA-approved test
Mechanism of Action
- Tyrosine kinase inhibitor targeting ALK, ROS1, and EGFR mutants
- Inhibits autophosphorylation of ALK and ALK-mediated phosphorylation of downstream signaling proteins STAT3, AKT, and ERK1/2
- Induces cell cycle arrest and apoptosis in cell lines expressing EML4-ALK fusion proteins
Contraindications
- Known hypersensitivity to brigatinib or any of its excipients
Adverse Reactions
- Vision adverse reactions (blurred vision, photopsia, visual acuity reduction)
- Interstitial lung disease (ILD) / pneumonitis
- Hypertension and bradycardia
- Creatine phosphokinase (CPK) elevation and lipase/amylase elevation
- Common: diarrhea, fatigue, nausea, rash, cough, myalgia, headache
Drug Interactions
- Strong CYP3A inhibitors (e.g., ketoconazole): Avoid coadministration; if unavoidable, reduce brigatinib dose by approximately 50%
- Strong CYP3A inducers (e.g., rifampin): Avoid coadministration
- Moderate CYP3A inducers: Avoid coadministration
- Drugs that prolong the PR interval (e.g., beta-blockers, non-dihydropyridine calcium channel blockers): Monitor heart rate and PR interval closely
Curated Content: Needs Vetting Before Put to Clinical Use