Brigatinib | pan-ALK inhibitor

Brigatinib (1197953-54-0) is a potent and selective pan-ALK inhibitor IC₅₀=0.6 nM.¹ Cells with ALK mutation L1196Q² and the double mutation I1171S + G1269³ remain sensitive to brigatinib. Clinically useful in non-small cell lung cancer.⁴

References/Citations

1) Zhang et al. (2016), The potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models; Clin. Cancer Res., 22 5527
2) Ceccon et al. (2013), Crizotinib-resistant NPM-ALK mutants confer differential sensitivity to unrelated Alk inhibitors; Mol. Cancer Res., 11 122
3) Takahashi et al. (2020), Overcoming resistance by ALK compound mutation (I1171S + G1269A) after sequential treatment of multiple ALK inhibitors in non-small cell lung cancer; Thorac. Cancer., 11 581
4) Pinto et al. (2020), Clinical consequences of resistance to ALK inhibitors in non-small cell lung cancer; Respir. Med., 14 385