Brigatinib Application Scope

Treatment of adult patients with ALK-positive metastatic non‑small cell lung cancer (NSCLC), including those who have progressed on or are intolerant to crizotinib.

Brigatinib Characteristics

Ingredients:
- Active: Brigatinib (a small‑molecule ALK/ROS1 tyrosine kinase inhibitor)
Properties: Orally active kinase inhibitor targeting ALK, ROS1, IGF‑1R, FLT‑3, and select EGFR mutations
Packaging Specification: Film‑coated tablets: 30 mg (round, “U3”) & 90 mg (oval, “U7”)
Storage: Store at controlled room temperature: 20 °C to 25 °C (68–77 °F); excursions allowed between 15–30 °C
Expiry Date: As per printed package—refer to individual cartons; typical shelf‑life ~24 months from manufacture (check label for specifics).
Executive Standard: Follows FDA-approved prescribing information (PIs) and USP standards.
Approval Number: NDA 208772 (U.S. FDA); marketed under brand name Alunbrig®.
Date of Revision: Most recent label revision accessed in 2024–2025 (label PDF July 2024)
Manufacturer: Originally Ariad Pharmaceuticals, now Takeda Pharmaceutical Company Limited

Guidelines for the Use of Brigatinib

Dosage and Administration:
- Initial: 90 mg orally once daily for 7 days.
- If tolerated, escalate to 180 mg once daily (maintenance dose)
Adverse Reactions:
- Common AEs (≥25%): diarrhea, fatigue, nausea, rash, cough, myalgia, headache, hypertension, vomiting, dyspnea
  Serious/fatal events: interstitial lung disease/pneumonitis (3–6%), pneumonia, pulmonary embolism, respiratory failure, sudden death (~3.7%)
Contraindications: Unknown.
Precautions:
- Monitor pulmonary symptoms especially first week
- Monitor blood pressure, heart rate (bradycardia), pancreas enzymes, blood glucose, CPK, liver function
- Fetal risk: causes embryo‑fetal toxicity; advise contraception (females: non‑hormonal during treatment + 4 months; males: partners use contraception during + 3 months)

Interactions

Drug Interactions:
CYP3A inducers (e.g., rifampin, carbamazepine, phenytoin): decrease brigatinib exposure; avoid or increase brigatinib dose
CYP3A inhibitors (e.g., ketoconazole, clarithromycin): increase exposure; avoid or reduce dose ~50% .
Brigatinib induces CYP3A → may reduce effectiveness of hormonal contraceptives, midazolam, ethosuximide, etc.; use non‑hormonal birth control
Apart from CYP interactions, severe interactions noted with drugs like doravirine

Note:

If there is a new packaging for the drug, the new packaging shall prevail. The above information is sourced from DengYue Medicine.
It is only for internal discussion among medical staff and does not serve as a basis for medication. For specific medication guidelines, please consult the attending physician.