Brigatinib (AP26113) is a medicine used to treat cancer that suppresses epidermal growth factor receptor (EGFR) and anaplastic lymphoma kinase (ALK). Brigatinib is a selective agonist against variations of EGFR as opposed to the wild mutant forms. The drug also illustrates selectivity against the ALK-EML4 fusion gene, which is a fundamental aspect of the modification of susceptible lung parenchyma. Brigatinib is prescribed for patients with specific abnormal genes and when the non-small cell lung cancer (NSCLC) is non-responsive to management with other medications. Brigatinib is classified as a kinase inhibitor, whose mechanism of action entails suppressing the action of abnormal proteins that enhance the multiplication of cancer cells.

Function & Application

Brigatinib, also known as AP-26113, is an orally active, potent and selective Dual ALK/EGFR inhibitor. AP26113 binds to and inhibits ALK kinase and ALK fusion proteins as well as EGFR and mutant forms. This leads to the inhibition of ALK kinase and EGFR kinase, disrupts their signaling pathways and eventually inhibits tumor cell growth in susceptible tumor cells. In addition, AP26113 appears to overcome mutation-based resistance. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; ALK dysregulation and gene rearrangements are associated with a series of tumors. EGFR is overexpressed in a variety of cancer cell types.