PKCδ

Protein Kinase C delta (PKCδ) Inhibitors

Activated PKCδ inhibits RAS degradation which in turn stimulates tumor growth.

Early-Stage Preclinical Program

• 30% of all human malignancies display activating RAS mutations with another 60% showing over-activity of Ras-signaling pathways.
• BriaCell’s novel, proprietary PKCδ inhibitors have shown activity against multiple RAS transformed tumors.
• This target has an attractive safety profile based on in vivo studies and knock out mouse studies.
• PKCδ also has potential activity as an immunotherapeutic by blocking TGFβ signaling.
• PKCδ inhibitors are applicable to specific niche tumor types which provide an accelerated clinical development plan.
• Could be in clinic within 24 months
• Provides Cost-Effective Additional Shot-on-Goal and additional partnership opportunities.

• Structural aspects of first generation inhibitor rottlerin and staurosporine(pan-PKC inhibitor) were combined to create second generation inhibitor KAM1
• Third generation inhibitors such as BJE6-106 have improved potency and selectivity.
• Fourth generation inhibitors under development to optimize drug-like characteristics.
• PKCδinhibitors lack endothelial cell cytotoxicity & PKCδdeficient mice develop normally and are fertile → No marked intrinsic toxicity by inhibiting PKCδ