Pipeline

Precision Medicine Approach

IDEAYA’s personalized medicine approach comprises novel therapeutics having clinically actionable biomarkers. Our small molecule therapeutics are directed to synthetic lethal (SL), targeted therapies (TT) and immune oncology (IO) targets. We apply our translational expertise and platform for discovery, validation and clinical development of biomarkers to each of these areas.

Targeted therapies (TT) act on targets directly in an oncogenic pathway. Particular genomic mutations which drive proliferation in cancer cells also create susceptibilities – targets in the direct mechanistic pathways – that are druggable using small molecule therapeutics.

Synthetic lethality (SL) approaches exploit cancer cell genetic dependencies – i.e., where genetic mutations in cancer cells make them more susceptible than healthy cells to small molecule inhibition of a (synthetic lethal) target protein.

Immune oncology (IO) opportunities are focused on small molecule therapeutics enhanced by diagnostic and pharmacodynamic biomarker strategies. IDEAYA is currently pursuing pathways known to produce an immune suppressed tumor microenvironment, enabling tumors to escape recognition by the host immune system.

Precision Medicine Pipeline

IDEAYA’s precision medicine pipeline includes small molecule therapeutics and associated biomarker diagnostics targeting PKC (TT), AhR (IO), and various synthetic lethality (SL) targets.

We are developing IDE196, a protein kinase C (PKC) inhibitor, for the treatment of cancers with GNAQ and GNA11 mutations. This targeted therapeutic is a potent and selective small molecule inhibitor of PKC. IDE196 is demonstrating early clinical activity and tolerability in an ongoing Phase 1 clinical study being conducted by Novartis in patients with metastatic uveal melanoma (MUM). In the ongoing trial, IDE196 is being studied as a single-agent and in combination therapy with HDM201, Novartis’ human double minute 2 (HDM2) inhibitor, an important negative regulator of the p53 tumor suppressor.

IDEAYA’s precision medicine pipeline includes small molecule therapeutics and associated biomarker diagnostics targeting PKC (TT), AhR (IO), and various synthetic lethality (SL) targets.

IDEAYA is also developing an aryl hydrocarbon receptor (AhR) antagonist for treatment of various solid tumors. Our development candidate, IDE697, is a highly potent and selective small-molecule antagonist of AhR. In vivo, IDE697 demonstrates tumor growth inhibition in mouse models. The compound inhibits activation of its target AhR receptor by endogenous and exogenous ligands in-vitro and in-vivo. In ex-vivo human cell cultures, IDE697 demonstrates an immune response profile evidencing a mode of action consistent with the mechanistic understanding of this immune suppression pathway – including increase in tumor infiltrated activated CD8 T-cells, and inhibition of Treg cell and M2 macrophage cell suppressive activities.

IDEAYA’s pipeline also includes small molecule therapeutics and biomarker diagnostics for several synthetic lethal targets. Our synthetic lethality programs are focused on patients having tumors defined by genetic mutations in TSG (Tumor Suppressor Genes), HRD (Homologous Recombination Deficiency), BER (Base Excision Repair) and MSI (Microsatellite Instability).