Brigatinib is an oral targeted therapy developed by Ariad Pharmaceuticals, later acquired by Takeda Oncology. It was designed to overcome resistance that often develops with earlier ALK inhibitors like crizotinib. Brigatinib showed strong activity in patients whose cancer had spread to the brain and in those with disease progression after first-line ALK therapy.

• FDA Approval (US): April 2017 (accelerated approval) for ALK-positive metastatic non-small cell lung cancer (NSCLC) previously treated with crizotinib.

• Expanded Approval: In May 2020, the FDA approved Brigatinib as a first-line treatment for adults with ALK-positive metastatic NSCLC.

• EMA Approval (EU): 2018, for ALK-positive advanced NSCLC.

Brigatinib is used for:

• First-line treatment of ALK-positive metastatic non-small cell lung cancer (NSCLC).

• Treatment of ALK-positive metastatic NSCLC in patients who have progressed on or are intolerant to crizotinib.

Brigatinib works by selectively inhibiting the activity of the ALK protein and other kinases involved in cancer cell proliferation. Blocking these enzymes helps prevent tumor cells from multiplying, spreading, and surviving, thereby slowing the progression of lung cancer.

• Form: Oral tablets.

• Recommended dosing:

1. Day 1–7: 90 mg once daily.

2. From Day 8 onward: 180 mg once daily (if well tolerated).

• Administration:

1. Take at the same time each day, with or without food.

2. Swallow tablets whole; do not crush, chew, or split.

3. If vomiting occurs after taking a dose, do not take an extra dose; continue with the next scheduled dose.

Common side effects:

• Nausea

• Fatigue

• Diarrhea

• Increased blood pressure

• Cough.

Serious side effects (seek medical help immediately):

• Lung problems (pneumonitis, interstitial lung disease)

• Liver enzyme abnormalities

• Severe allergic reactions (rash, swelling, difficulty breathing)

• High blood pressure

• Visual disturbances.

• Pulmonary toxicity: Risk of early-onset interstitial lung disease/pneumonitis within the first week of therapy. Monitor respiratory symptoms closely.

• Hypertension: Brigatinib can cause significant increases in blood pressure; regular monitoring is required.

• Hepatotoxicity: Elevations in liver enzymes reported; routine liver function tests recommended.

• Bradycardia: May lower heart rate monitor patients with cardiac risk factors.

• Ocular effects: Blurred vision, diplopia. Patients should report visual changes immediately.

• Embryo-fetal toxicity: May cause harm to the unborn baby; contraindicated in pregnancy.

• Avoid pregnancy during treatment and for at least 4 months after the last dose.

• Do not breastfeed during treatment and for at least 1 week after the final dose.

• Use caution in patients with pre-existing lung, liver, or cardiovascular conditions.

• Avoid use of strong CYP3A inhibitors or inducers, as they may alter Brigatinib blood levels.

• Elderly patients and those with poor performance status need close monitoring for side effects.

• Take Brigatinib at the same time every day for consistent effect.

• Keep regular medical follow-ups for monitoring side effects and treatment progress.

• Report any unusual symptoms, especially breathing difficulties, to your doctor immediately.

• Do not stop treatment suddenly without medical advice.

1. https://go.drugbank.com/drugs/DB12267

2. https://pmc.ncbi.nlm.nih.gov/articles/PMC10386943/

3. https://www.takedaoncology.com/news/news-releases/u.s.-fda-approves-takedas-alunbrig-brigatinib-as-a-first-line-treatment-option-for-patients-diagnosed-with-rare-and-serious-form-of-lung-cancer/

The drug information on this page is not a substitute for medical advice. It is meant for educational purposes only. For further details, consult your doctor about your medical condition to know if you can receive this treatment.