Small Molecule for Treatment-Resistant Lung Cancer

Application

Small molecule agonist for treating cancers involving KRAS mutations.

Key Benefits

Specifically targets mutant KRAS in non-small-cell lung carcinoma (NSCLC).
Selective for mutant KRAS lung cancer cells over normal cells.
Non-toxic to normal cells.

Market Summary

Lung cancer patients with KRAS mutation(s) have a poor prognosis due in part to the development of resistance to currently available therapeutic interventions. Currently, there are no effective targeted therapies for patients with the KRAS mutation. Developing a specific anti-KRAS agent is very challenging. This protein has been considered an "undruggable" target because it is highly difficult to inhibit its intracellular activity. Therefore, there is a need to develop new therapeutic agents that directly target this protein thus increasing the chances of survival of lung cancer patients.

Technical Summary

Overcoming these hurdles, Emory researchers have identified a small molecule KRAS agonist that specifically binds the protein and induces cell death in mutant KRAS lung cancer cells. Lung cancer cell lines with KRAS mutation were relatively more sensitive to the small molecule than cell lines without KRAS mutation. Additionally, this molecule suppresses malignant growth without significant toxicity to normal tissues.