Intellikine has developed a portfolio of novel drug candidates that selectively inhibit the PI3Kα isoform as well as PI3Kα/β dual inhibitors, for the treatment of solid tumor malignancies.
The PI3K/Akt/mTOR pathway is frequently upregulated and/or dysregulated in human tumors and PI3Ks are important regulators of cancer-related signaling pathways involved in cell proliferation, adhesion, survival and motility. The PIK3CA gene encoding the p110α catalytic subunit, represents one of the most highly mutated oncogenes identified in human cancers and is frequently mutated in a broad spectrum of tumors including colon, breast, brain and lung.
Recent studies have delineated specialized functions in tumorigenesis for PI3Kα and PI3Kβ. Specifically, it has been proposed that PI3Kα carries the majority of the PI3K signal driven by PIK3CA mutations and/or oncogenic receptor tyrosine kinases (RTKs)/Ras, whereas p110β responds to GPCRs as well as mediating PTEN-deficient tumorigenesis.
Intellikine currently has a portfolio of PI3Kα/β-Selective inhibitors currently under preclinical evaluation as potential therapies for solid tumor malignancies.