Inlexisertib – ULK inhibitor
Advanced gastrointestinal stromal tumor (GIST)
About This Program
Inlexisertib is a potential first-in-class small molecule designed to inhibit autophagy by targeting the ULK1/2 kinase. Advanced cancers driven by mutations at or downstream of receptor tyrosine kinases (RTKs) can activate autophagy as an escape mechanism to promote cell survival. ULK1/2 kinases are key regulators that initiate autophagy in response to stress, such as RTK pathway inhibition. Inhibition of ULK1/2 provides a potential targeted approach to selectively inhibit autophagy and is a potential strategy for combination therapy with RTK pathway inhibitors. Inlexisertib is being investigated in a Phase 1/2 study designed to evaluate the safety, recommended phase 2 dose, and preliminary efficacy in combination with ripretinib in patients with advanced GIST.
To learn more about this study, click here.
References
1 Chandana SR, et al. J Clin Oncol. 2024;42:TPS11587.