BRIGATINIB
Background and Date of Approval
Brigatinib is an oral targeted therapy developed to overcome resistance that often emerges with earlier ALK inhibitors such as crizotinib. It demonstrated substantial activity in patients with brain metastases and in those with disease progression following first-line ALK therapy.
FDA Approval (US): Brigatinib received accelerated approval in April 2017 for ALK-positive metastatic non-small cell lung cancer (NSCLC) in patients 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): Brigatinib was approved in 2018 for ALK-positive advanced NSCLC.
Uses
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.
Side Effects
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.
Warnings
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.
Precautions
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.
References
https://go.drugbank.com/drugs/DB12267 https://pmc.ncbi.nlm.nih.gov/articles/PMC10386943/ 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/
Frequently Asked Questions
What is Brigatinib used for?
Brigatinib is primarily used for the treatment of ALK-positive non-small cell lung cancer (NSCLC) and managing disease progression in patients previously treated with other ALK inhibitors.
Can Brigatinib be used during pregnancy?
No, Brigatinib is not recommended during pregnancy as it may cause serious harm to the developing fetus. Always consult your doctor before starting treatment if you are pregnant or planning pregnancy.
How should I take Brigatinib?
Take Brigatinib exactly as prescribed by your doctor, usually once daily, with or without food. Do not crush, chew, or split the tablets. Follow your doctor’s dosage schedule carefully.
What should I do if I miss a dose of Brigatinib?
If you miss a dose, take it as soon as you remember, unless it is almost time for your next dose. Do not double the dose to make up for the missed one.
Are there any serious side effects I should watch for?
Yes, report any difficulty breathing, severe rash, swelling, liver issues, or heart problems to your doctor immediately, as these could be serious side effects requiring urgent medical attention.