THESEUS PHARMACEUTICALS, INC. Theseus Pharmaceuticals, Inc. announced preclinical data characterizing its fourth-generation epidermal growth factor receptor (EGFR) inhibitor, THE-349, will be detailed in a live poster presentation at the 34th EORTC-NCI-AACR Symposium on molecular targets and cancer therapeutics (ENA), taking place in Barcelona, Spain on October 26 – 28, 2022. THE-349 is currently in preclinical development as a single-molecule inhibitor of all major classes of EGFR activating and resistance mutations consisting of single-, double- and triple-mutant EGFR variants, including T790M and C797X, for treatment of EGFR-mutant non-small cell lung cancer (NSCLC). These preclinical data demonstrate that THE-349, as a single agent, exhibits highly potent inhibition of all major EGFR mutant variants with a high degree of kinome and wild-type EGFR selectivity.
Coupled with excellent oral bioavailability, this drives deep in vivo tumor regressions in osimertinib-resistant models of EGFR-mutant NSCLC, as well as substantial CNS activity in intracranial mouse models. The activity profile achieved by THE-349 positions the asset for development as a single agent and potentially in combination with other, non-EGFR inhibitor modalities.
