priority indications for patients having tumors with methylthioadenosine phosphorylase, or MTAP, gene deletion, including squamous non-small cell lung,
bladder, gastric and esophageal cancers. We observed IDE397 monotherapy responses in multiple priority solid tumor types based on experience across several patients in the early phase of the Phase 2 dose expansion.
In collaboration with Amgen Inc., or Amgen, as part of our Clinical Trial Collaboration and Supply Agreement with Amgen, we achieved IND clearance for and are
continuing patient enrollment in the Amgen-sponsored Phase 1/2 clinical trial evaluating IDE397 in combination with AMG 193, the Amgen investigational MTA-cooperative protein arginine methyltransferase 5, or
PRMT5, inhibitor, in patients having tumors with MTAP deletion. This potential first-in-class synthetic lethality combination targets mechanistically complementary nodes
of the MTAP methylation pathwayMAT2A and PRMT5and is supported by compelling preclinical anti-tumor efficacy presented at the 2023 Annual Meeting of the American Association for Cancer Research.
We are also planning to evaluate IDE397 in combination with sacituzumab govitecan-hziy (Trodelvy), the Gilead Sciences, Inc., or
Gilead, Trop-2 directed anti-body conjugate (ADC) in patients having MTAP deletion bladder cancer, in an IDEAYA-sponsored clinical trial pursuant to our Clinical Study Collaboration and Supply Agreement with
Gilead.
IDE161, our small molecule PARG inhibitor, is being evaluated in a Phase 1 clinical trial, which is currently in monotherapy expansion, with a strategic
focus in estrogen receptor positive human epidermal growth factor receptor 2 negative, or Her2(-), breast cancer with homologous recombination deficiency, or HRD, as well as HRD+ ovarian cancer, and other solid tumors with HRD, such as endometrial
cancer and colorectal cancer. We are, in parallel, continuing with Phase 1 dose optimization of IDE161 in patients having tumors with HRD. We have observed multiple partial responses by RECIST 1.1 and tumor shrinkage in priority solid tumor types
early in the Phase 1 dose escalation and at the expansion dose. We received Fast Track Designation from the U.S. Food and Drug Administration, or FDA, for IDE161 for ovarian cancer and breast cancer indications, specifically for the treatment of
(i) adult, pretreated, platinum-resistant advanced or metastatic ovarian cancer patients having tumors with BRCA1/2 mutations and (ii) adult, pretreated, advanced or metastatic hormone receptor positive, Her2(-) and BRCA1/2 mutant breast
cancer patients.
GSK101 (IDE705), our Pol Theta Helicase inhibitor clinical development candidate, is a potential first-in-class small molecule inhibitor of the helicase domain of Polymerase Theta, or Pol Theta. GSK101 was discovered and evaluated in preclinical studies in collaboration with GSK. The IND for GSK101 has
been cleared by the FDA and GSK has dosed a first patient in the Phase 1 clinical trial. GSK plans to evaluate GSK101 under a GSK-sponsored clinical trial in combination with niraparib, the GSK small molecule
inhibitor of poly-(ADP-ribose) polymerase for the treatment of patients having tumors with BRCA, other homologous recombination or HRD.
We have selected a Werner Helicase inhibitor development candidate, or Werner Helicase inhibitor DC, in collaboration with GSK. This Werner Helicase inhibitor DC is
targeting the helicase domain of the Werner protein, for patients having tumors with high microsatellite instability, or MSI. We are, in collaboration with GSK, targeting an IND submission in 2024 to enable first-in-human clinical evaluation of our Werner Helicase inhibitor DC in high MSI tumors.
We have multiple wholly owned
preclinical-stage programs on undisclosed targets to enable the next wave of precision medicine therapeutics in our pipeline. These preclinical programs are focused on opportunities that we believe have the potential to be first-in-class or best-in-class, or both. We are targeting to nominate multiple development
candidates for these programs in 2024.
We have established a robust precision medicine research platform with capabilities for identification and validation of new
targets and biomarkers, drug discovery and translational biology. Our approach integrates small molecule drug discovery with extensive capabilities in identifying and validating translational biomarkers