RAS Signaling Pathway Program
Ikena is developing oral small molecule ERK5 inhibitors which may address a high unmet medical need by modulating a key target downstream in the RAS signaling pathway.
RAS Signaling Pathway Program
We are developing oral small molecule ERK5 inhibitors which may address a high unmet medical need by modulating the RAS signaling pathway.
ERK5 Inhibitor
KRAS mutations in the RAS signaling pathway occur in approximately 26% of all cancers. Although there has been recent progress with development-stage compounds that are designed to directly inhibit certain KRAS mutations, approximately 85% of KRAS mutations are not being addressed by current product candidates or approved therapies. We believe that inhibiting ERK5 provides an opportunity to address a high unmet medical need by modulating a key target downstream in the RAS signaling pathway.
In preclinical studies, we observed fewer tumors in genetically engineered KRAS mutant lung and pancreatic cancer mouse models where ERK5 was knocked out, as compared to wildtype control. We also observed that inhibition of the target using an ERK5 inhibitor tool compound blocked tumor growth in patient-derived KRAS mutated xenograft models. Additionally, in preclinical studies in KRAS primary human tumor models of lung and pancreatic cancer, we observed synergistic effects on tumor inhibition by combining an ERK5 inhibitor and trametinib, a mitogen- activated protein kinase, or MEK inhibitor.