KIT Program for GIST

We are developing targeted therapies for gastrointestinal cancer designed to address treatment resistance.

Our lead program, THE-630, is a pan-variant KIT inhibitor designed for patients with advanced gastrointestinal stromal tumors (GIST) whose cancer has developed resistance to earlier lines of kinase inhibitor therapy.

Approximately 80% of GIST cases are driven by mutations that activate the tyrosine kinase KIT, and the disease remains KIT dependent through successive lines of therapy. Most patients who receive first-line imatinib as a treatment for GIST experience disease progression due to the emergence of secondary KIT mutations.

Subsequent lines of kinase inhibitor therapy are significantly less effective. Our goal is to develop a truly pan-variant inhibitor that can address the limitations of current therapies.

We believe the broad inhibitory profile of THE-630 has the potential to generate robust and durable responses for advanced GIST patients across the spectrum of previously-treated patient populations.

We compared the activity of THE-630 and current standards of care against a panel of KIT mutations using our predictive resistance assay (PRA) and found that only THE-630 demonstrated activity against all major classes of activating and resistance mutations.

We have submitted an IND for THE-630 with the U.S. Food and Drug Administration (FDA) and, if accepted, we plan to initiate a Phase 1/2 dose escalation and expansion clinical trial in patients with previously-treated GIST.

We are developing a pipeline of TKIs designed to inhibit all major cancer causing and drug resistance mutations in clinically significant protein kinases.

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