A drug used to treat non-small cell lung cancer that has spread to other parts of the body and is anaplastic lymphoma kinase (ALK) positive. It is used in patients whose cancer has gotten worse during treatment with or who cannot take crizotinib (a type of anticancer drug). Brigatinib blocks certain proteins made by the ALK gene. Blocking these proteins may stop the growth and spread of cancer cells. Brigatinib is a type of tyrosine kinase inhibitor. Also called Alunbrig.
Clinical use of Brigatinib
Brigatinib is a tyrosine kinase receptor inhibitor and antineoplastic agent used in the therapy of selected forms of advanced non-small cell lung cancer.
Liver safety of Brigatinib
Brigatinib is associated with a moderate rate of transient elevations in serum aminotransferase levels during therapy but has yet to be linked to instances of clinically apparent acute liver injury.
Mechanism of action of Brigatinib
Brigatinib (bri ga' ti nib) is a small molecule tyrosine kinase receptor inhibitor with potent activity against anaplastic lymphoma kinase (ALK) that is rearranged and mutated in some cancers including approximately 5% of non-small cell lung cancer (NSCLC). The mutated, rearranged ALK promotes unregulated cell growth and proliferation. Brigatinib has been found to inhibit mutated ALK in cell culture and in several clinical trials was found to induce objective responses in a proportion of patients with refractory, advanced NSCLC that are ALK-positive.
FDA approval information for Brigatinib
Brigatinib was approved for use in the United States in 2017 in patients with ALK-positive, metastatic NSCLC who have progressed despite therapy with first generation ALK inhibitors (such as crizotinib).
Dosage and administration for Brigatinib
Brigatinib is available in tablets of 30, 90 and 180 mg under the brand name Alunbrig. The recommended dose is 90 to 180 mg daily, continued until disease progression or intolerable toxicity occurs. side effects are common and can be dose limiting. Common adverse events include fatigue, nausea, diarrhea, headache and cough. Less common but potentially severe side effects include severe pulmonary toxicity, interstitial lung disease, myopathy, bradycardia and embryo-fetal toxicity.