AUM302
Macrocyclic multi-kinase inhibitor
AUM302 is a first-in-class oral kinase inhibitor rationally designed to uniquely combine pan-PIM kinase, pan-PI3K and mTOR inhibition in a single agent. This multi-targeting ability has been engineered into a single molecule that has the ability to inhibit multiple key intracellular pathways, increasing its ability to inhibit cancer cell growth and prevent resistance emergence. It has potent efficacy, good tolerability and favorable drug properties. AUM302 is a unique multi-targeted cancer therapeutic that targets not only PI3K, but also key resistance mechanisms such as PIM and mTOR. AUM302 is a single molecule therapeutic that has been optimized to inhibit these key pathways.
MECHANISM OF ACTION
The complexity of the PI3K/AKT/mTOR signaling network involves numerous feedback loops, extensive crosstalk nodes with other signaling pathways and compensatory pathways, providing ample opportunities for circumventing the effects of PI3K inhibition. Oncogenic activation of the PI3K pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy. Critically, PI3K pathway activation often occurs alongside pro-tumorigenic aberrations in other signaling networks, thereby enabling a tumor cell to resist the effects of PI3K inhibition and/or to readily develop such resistance.
