Briganix 90 Mg (Brigatinib) is a tyrosine kinase inhibitor with in vitro activity at clinically achievable concentrations
against multiple kinases including ALK, ROS1, insulin-like growth factor-1 receptor (IGF-1R), and
FLT-3 as well as EGFR deletion and point mutations. Briganix 90 Mg (Brigatinib) inhibited autophosphorylation of
ALK and ALK-mediated phosphorylation of the downstream signaling proteins STAT3, AKT,
ERK1/2, and S6 in in vitro and in vivo assays.
Briganix 90 Mg (Brigatinib) also inhibited the in vitro proliferation of cell lines expressing EML4-ALK and NPM-ALK
fusion proteins and demonstrated dose-dependent inhibition of EML4-ALK-positive NSCLC
xenograft growth in mice. At clinically achievable concentrations (500 nM), brigatinib inhibited
the in vitro viability of cells expressing EML4-ALK and 17 mutant forms associated with resistance
to ALK inhibitors including Crizotinib, as well as EGFR-Del (E746-A750), ROS1-L2026M,
FLT3-F691L, and FLT3-D835Y.
Briganix 90 Mg (Brigatinib) exhibited in vivo anti-tumor activity against 4 mutant forms of EML4-ALK, including
G1202R and L1196M mutants identified in NSCLC tumors in patients who have progressed on
Crizotinib. Briganix 90 Mg (Brigatinib) also reduced tumor burden and prolonged survival in mice implanted
intracranially with an ALK-driven tumor cell line.