Pipeline

Precision Medicine Approach

We are applying our capabilities and approach to develop a portfolio of targeted therapeutics for defined patient populations. For each program in our pipeline, we are discovering novel product candidates, identifying biomarkers and pursuing biomarker-driven clinical trials. Biomarker-enabled translational approaches help enhance patient outcomes – by identifying patients likely to respond to particular therapies and by providing clinical insights based on extent of target modulation.

An understanding of tumor biology, in particular genomic alterations that drive cell proliferation and survival, enables an opportunity to develop therapies directly targeting an oncogenic pathway for cancers with limited or no effective treatments. IDEAYA is pursuing small molecule therapeutics with a goal of providing significant impact for patients with such genetically defined tumors. Our lead product candidate, IDE196, has shown clinical activity in metastatic uveal melanoma patients whose tumors harbor mutations in GNAQ or GNA11 that activate the PKC signaling pathway.

IDEAYA Precision Medicine Approach

SL = Synthetic Lethality, DT = Directly Targeting Oncogenic Pathway

Synthetic lethality is emerging as an important therapeutic paradigm in the treatment of cancer. Our pipeline in synthetic lethality comprises multiple preclinical small molecule therapeutics against known and novel targets for defined patient populations, including MAT2A for patients with tumors having MTAP gene deletion. Our other synthetic lethality programs are for patients having tumors with genetic mutations in homologous recombination deficiency (HRD), including BRCA mutations, or base excision repair (BER), and tumors having high microsatellite instability (MSI).

For many of our programs, a diagnostic is commercially available, for example, on a tumor-profiling panel. In some cases, we coordinate or support development of a diagnostic with selected partners.

Precision Medicine Pipeline

Our precision medicine pipeline contains product candidates in distinct classes of biomarker-enabled targeted therapies, including direct targeting of oncogenic pathways and synthetic lethality. This pipeline is supplemented by a proprietary target discovery platform, including our Dual CRISPR combinatorial approach for evaluating potential synthetic lethality relationships between potential drug targets and tumor suppressor genes, or TSG.

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). We are also planning to evaluate IDE196 in a broader patient population in a basket trial in multiple solid tumor types which have GNAQ or GNA11 mutations or PKC gene fusions.

PKC = protein kinase C, MUM = metastatic uveal melanoma, NSCLC = non small cell lung cancer, HRD = homologous recombination deficiency, MSI = microsatellite instability

Our pipeline in synthetic lethality comprises multiple preclinical small molecule therapeutics against known and novel targets for defined patient populations having a prevalence of over 10% in certain solid tumors, including for example MAT2A for patients with tumors having MTAP gene deletion. We are also developing therapeutics for patients having tumors with genetic mutations in homologous recombination deficiency (HRD), including BRCA mutations, or base excision repair (BER), and tumors having high microsatellite instability (MSI).