What is ALUNBRIG (brigatinib)?
Brigatinib: A potent ALK inhibitor1
Brigatinib is a small molecule specifically designed to target ALK rearrangements in NSCLC1,2
- Discovered and developed by Ariad, subsequently acquired by Takeda
Key structural features such as dimethylphosphine oxide contribute to its potency and selectivity2
- Selectively inhibits ALK (IC50=0.6 nM) and ROS1 (IC50=1.9 nM)1*
Brigatinib binds to the ATP-binding site of ALK1,2
- Inhibits 17 different ALK mutants at clinically achievable concentrations1*
*Results were derived from experiments in an invitro panel of ALK-expressing cell lines.
Direct clinical significance of preclinical data is unproven.
- Zhang S, et al. Clin Cancer Res.2016;22(22):5527-5538.
- Huang WS, et al. J Med Chem. 2016;59(10):4948-4964.