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

The Phase 1/2 dose escalation and expansion clinical trial in patients with previously-treated GIST is actively enrolling. For more information visit clinicaltrials.gov (NCT05160168).

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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