The activity, safety, and evolving role of brigatinib in patients with ALK-rearranged non-small cell lung cancers.

ABSTRACT: Brigatinib (AP26113) is a dimethylphosphine oxide group-containing tyrosine kinase inhibitor (TKI) constructed around a bisanilinopyrimidine scaffold with potent activity against the anaplastic lymphoma kinase (ALK) and several other targets. Despite the activity of first- and second-generation ALK inhibitors in advanced ALK-rearranged lung cancers, the development of acquired resistance represents an ongoing challenge. Later generation ALK inhibitors such as brigatinib are important potential tools in the management of patients with acquired resistance characterized by continued dependency on ALK. Brigatinib is active in vitro against many ALK kinase domain mutations that may mediate acquired resistance to other ALK TKIs, with reported activity (IC₅₀ <50 nM) again

SUBMITTER: Sabari JK 

PROVIDER: S-EPMC5388194 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature