IDEAYA Biosciences is focused on the development of precision medicine therapeutics, particularly in the field of oncology, leveraging the concept of synthetic lethality. This approach targets specific genetic alterations in tumors, allowing for the identification of patient populations that may benefit from tailored treatments. The company’s pipeline includes several clinical-stage compounds, such as Darovasertib (IDE196), a PKC inhibitor for tumors with GNAQ or GNA11 mutations, IDE397, a MAT2A inhibitor for tumors with MTAP gene deletions, and IDE161, a PARG inhibitor for tumors with homologous recombination deficiencies. By utilizing molecular diagnostics to select patients based on their tumor biology, IDEAYA aims to develop first-in-class and best-in-class therapies that can significantly improve patient outcomes.

The synthetic lethality platform at IDEAYA enables the discovery and validation of novel therapeutic targets and biomarkers. This platform integrates advanced technologies, including CRISPR-based screening and bioinformatics, to identify genetic interactions that can be exploited for therapeutic benefit. For instance, the company is investigating the synthetic lethality relationship between various gene mutations and their corresponding drug targets, such as the relationship between BRCA mutations and PARP inhibitors. IDEAYA's commitment to precision medicine is further exemplified by its collaborations with leading research institutions, which enhance its capabilities in biomarker discovery and translational research, ultimately aiming to deliver impactful therapies for cancer patients.

United States

IDEAYA is an oncology-focused precision medicine company. Our teams are committed to the discovery and development of targeted therapeutics for patient populations selected using molecular diagnostics. We are advancing therapeutics that have the potential to be first-in-class and/or best-in-class, with a primary focus in synthetic lethality – an emerging class of precision medicine targets. IDEAYA is headquartered in South San Francisco, California.

Cancer

IDEAYA Biosciences

Solid tumor/s

Uveal melanoma

IDE196, a PKC inhibitor, is a clinical stage development compound for patients with tumors harboring GNAQ or GNA11 mutations, including in metastatic uveal melanoma (MUM) and skin melanoma.

Darovasertib 

Metastatic uveal melanoma

Darovasertib (IDE196) + crizotinib

Ocular melanoma

Darovasertib  

Cutaneous Melanoma

Darovasertib (IDE196) + crizotinib 

Endometrial cancer

ER+/HER2- breast cancer

Ovarian cancer

IDE161 is a potent, selective, small-molecule inhibitor of PARG, a novel and mechanistically-differentiated target in the same clinically validated pathway as poly (ADP-ribose) polymerase (PARP).

IDE161 +/- KEYTRUDA® (pembrolizumab)

GSK101 (IDE705) is a small molecule inhibitor of Pol Theta Helicase, in combination with niraparib, a small molecule inhibitor of poly-(ADP-ribose) polymerase (PARP).

GSK101 (IDE705) + niraparib

Bladder cancer

Non-small cell lung carcinoma

In MTAP null patients, pharmacologically inhibiting MAT2A modulates key protein methylation function, leading to cancer cell death. MTAP-null cells lack the ability to metabolize 5-methylthioadenosine, or MTA, which is an essential step in a biochemical pathway involved in salvaging metabolite S-adenosyl methionine, or SAM. Increased levels of MTA partially inhibit the methyltransferase PRMT5 for which SAM is the substrate. This partial inhibition renders MTAP-null cells more dependent on the activity of methionine adenosyltransferase II alpha or MAT2A, an enzyme that is responsible for the synthesis of SAM. Because of this dependence, loss of MTAP results in synthetic lethality when MAT2A is pharmacologically inhibited.
 
IDE397 (MAT2A) is a small molecule methionine adenosyltransferase 2a (MAT2A) inhibitor, for the treatment of patients having solid tumors with methylthioadenosine phosphorylase (MTAP) deletion.

IDE397 (MAT2A) 

Urothelial cancer

IDE397 (MAT2A) + Trodelvy

IDE275 (GSK959) is a potential first-in-class small molecule inhibitor of Werner Helicase that was discovered by IDEAYA in collaboration with GSK. In preclinical studies, IDE275 has demonstrated robust and selective synthetic lethality in the MSI-High biomarker setting, including single-agent tumor regressions in-vivo in MSI-High CDX and PDX models derived from colorectal, endometrial and gastric cancers. Initiation of the Phase 1 trial for IDE275 is projected in the fourth quarter of 2024. GSK is the sponsor of the IND application and plans to develop IDE275 (GSK959) as both a monotherapy agent and in combination with a PD-1 inhibitor in a Phase 1 clinical trial for patients having MSI-High tumors. The percent prevalence of MSI-High in solid tumors, including endometrial, colorectal, and gastric cancers, has been reported at approximately 31%, 20%, and 19%, respectively (JCO Precision Oncology, September 2017).

IDEAYA Biosciences

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