What is brigatinib/brigatinib?

Brigatinib is an oral drug used to treat adults with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC). Cancer is caused by genetic mutations that cause abnormal cells to grow and replicate uncontrollably. These cells cannot function properly and inhibit the growth and activity of normal cells. Brigatinib is a small molecule targeted therapy that does not kill cancer cells but specifically targets abnormal cells and changes cellular mechanisms to prevent cancer from growing and spreading.

Brigatinib works by inhibiting the activity of several proteins called tyrosine kinases, including abnormalALK fusion proteins that are out of control due to certain genetic mutations and promote the growth and proliferation of cancer cells. Other tyrosine kinases inhibited by brigatinib include ROS1, insulin-like growth factor-1 receptor (IGF-1R), FMS-like tyrosine kinase 3 (FLT-3), and epidermal growth factor receptor (EGFR) deletions and point gene mutations.

ALK is an enzyme encoded by the ALK gene that contributes to the development of the fetal gastrointestinal and nervous systems. The ALK gene produces abnormal ALK fusion proteins. ALK fusion proteins alter cell signaling and gene expression, leading to proliferation and survival of tumor cells expressing the protein. Brigatinib inhibits the activity of ALK and ALK-mediated activation of the downstream signaling protein STAT3.

Brigatinib targets cancer cells that expressALK fusion proteins, including EML4-ALK and 17 mutated forms associated with resistance to other ALK inhibitor drugs, including crizotinib. Brigatinib is only approved to treat non-small cell lung cancer that tests positive for the U.S. Food and Drug Administration (FDA)-approved ALK fusion protein.