IDE161 / Ideaya Biosci - LARVOL DELTA

IDEAYA Biosciences, Inc. Reports First Quarter 2025 Financial Results and Provides Business Update (PRNewswire) - "IDEAYA plans to enable the wholly-owned IDE397 and IDE892 (PRMT5MTA) combination in patients with MTAP-deletion non-small cell lung cancer (NSCLC) in the second half of 2025....Initiation of evaluation of IDE849 and IDE161 combination targeted in the second half of 2025....Targeting to present preclinical combination mechanism and synergy efficacy data of IDE161 with TOP1-payload based ADCs at a medical conference in the third quarter of 2025."

New trial • Preclinical • Non Small Cell Lung Cancer

PARG inhibition provokes a DNA damage-dependent innate immune reaction that enhances ICI-driven anti-tumor immunity (AACR 2025) - P1 | "These cumulative observations suggest that IDE161 can induce an innate-immune-pathway-mediated priming of an antitumor adaptive immune response, and thus may deliver both tumor autonomous and nonautonomous therapeutic benefits. This relationship is currently under evaluation with IDE161/pembrolizumab combination therapy In patients with advanced endometrial cancer who have previously progressed on anti-PD-1 therapy (NCT05787587)"

Endometrial Cancer • Oncology • Solid Tumor • IFNB1

IDEAYA Biosciences, Inc. Reports Fourth Quarter and Full Year 2024 Financial Results and Provides Business Update (PRNewswire) - "Data highlighting IDE275's differentiated potential best-in-class profile will be presented with GSK at a medical conference in the first half of 2025...First patient dosed in the Phase 1 trial evaluating IDE161 in combination with KEYTRUDA in patients with MSI-High and microsatellite stable (MSS) endometrial cancer. Targeting Phase 1 expansion in 2025...Targeting clinical combination(s) of IDE161 with TOP1i ADCs in solid tumors in 2025."

Clinical • New trial • P1 data • Endometrial Cancer • Microsatellite Instability • Solid Tumor

IDEAYA Biosciences, Inc. Reports Fourth Quarter and Full Year 2024 Financial Results and Provides Business Update (PRNewswire) - "Initiation of the Phase 3 registration-enabling trial for darovasertib in neoadjuvant UM is targeted for the first half of 2025...Targeting Phase 1/2 expansion in the first quarter of 2025 and clinical data update for IDE397 in combination with Trodelvy in MTAP-deletion UC in 2025...IDEAYA and Amgen mutually agreed to wind down the IDE397 and AMG 193 clinical combination study in February 2025, and will not pursue dose expansion...IDEAYA plans to submit a U.S. IND for the evaluation of IDE849 as a monotherapy in SCLC in the first half of 2025. Targeting to initiate the evaluation in combination with IDE161 and in NETs in the second half of 2025. Clinical data update targeted in 2025."

Clinical data • IND • New trial • Trial completion • Neuroendocrine Tumor • Small Cell Lung Cancer • Urothelial Cancer • Uveal Melanoma

IDEAYA Biosciences Announces Participation at the 43rd Annual J.P. Morgan Healthcare Conference and 2025 Corporate Guidance (PRNewswire) - "3 IND-filings targeted in 2025, representing IDEAYA's 7th, 8th, and 9th potential clinical stage precision medicine oncology program targeting solid tumors; IDE892, a potential best-in-class MTA-cooperative PRMT5 inhibitor, in mid-year 2025. Combination potential with IDE397; IDE034, a potential first-in-class B7H3/PTK7 TOP1i bispecific ADC, in the second half of 2025. Combination potential with IDE161; IDE251, a potential first-in-class KAT6/7 dual inhibitor development candidate, in the second half of 2025. Combination potential with multiple programs in IDEAYA's pipeline..."

IND • Solid Tumor

IDEAYA Biosciences Enters Exclusive License with Hengrui Pharma for SHR-4849… (PRNewswire) - "IDEAYA Biosciences...announced that it has entered into an exclusive license agreement for SHR-4849, a novel DLL3-targeting Topo-I-payload ADC program with Jiangsu Hengrui Pharmaceuticals..., an innovative global pharmaceutical company headquartered in China focused on unmet clinical needs. Under the terms of the agreement, IDEAYA will develop and commercialize SHR-4849 worldwide outside of Greater China....Under the terms of the agreement, Hengrui Pharma is eligible to receive upfront and milestone payments totaling $1.045 billion, including a $75m upfront fee, up to $200m in development and regulatory milestone payments, plus commercial success-based milestones. Hengrui is also eligible to receive mid-single to low-double digit royalties on net sales outside of Greater China....Rational combination opportunities with IDEAYA's DNA Damage Repair (DDR) clinical pipeline, including Phase 1 PARG inhibitor IDE161."

Licensing / partnership • Solid Tumor

IDEAYA Announces First-Patient-In for Phase 1 Clinical Trial Evaluating IDE161 in Combination with KEYTRUDA (pembrolizumab) in Patients with Endometrial Cancer (PRNewswire) - "IDEAYA Biosciences, Inc...announced that it has dosed the first patient in the IDEAYA-sponsored Phase 1 trial evaluating the combination of IDE161, the company's investigational, potential first-in-class, small molecule poly (ADP-ribose) glycohydrolase, or PARG, inhibitor, in combination with Merck's (known as MSD outside of the US and Canada) anti-PD-1 therapy, KEYTRUDA (pembrolizumab), in endometrial cancer patients with high microsatellite instability (MSI-high) and microsatellite stable(MSS)."

Trial status • Endometrial Cancer • Microsatellite Instability

A Study of PARG Inhibitor IDE161 in Participants with Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=216 | Recruiting | Sponsor: IDEAYA Biosciences | N=68 ➔ 216 | Trial completion date: Sep 2025 ➔ May 2027 | Trial primary completion date: Jun 2025 ➔ Oct 2026

Enrollment change • Trial completion date • Trial primary completion date • Breast Cancer • Colorectal Cancer • Endometrial Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • Head and Neck Cancer • Hepatology • Oncology • Ovarian Cancer • Pancreatic Cancer • Prostate Cancer • Solid Tumor • HRD

IDEAYA Biosciences, Inc. Reports Third Quarter 2024 Financial Results and Provides Business Update (PRNewswire) - "IDE161 in Tumors with Homologous Recombination Deficiency: Targeting Phase 1/2 monotherapy expansion for IDE161 PARG inhibitor in priority solid tumor type(s) in the fourth quarter of 2024. Targeting first-patient-in for the Phase 1 trial evaluating IDE161, IDEAYA's first-in-class potential PARG inhibitor, in combination with Merck's...KEYTRUDA (pembrolizumab), in MSI-High and MSS endometrial cancer (EC) in the fourth quarter of 2024....Targeting Development Candidate nomination for MTAP-deletion, KAT6 pathway and B7H3/PTK7 Topo-Payload Bispecific-ADC programs in Q4 2024."

New molecule • Trial status • Endometrial Cancer • Microsatellite Instability

A novel small molecule inhibitor of PARG, YL-18319, promotes tumor regression in BRCAmutated, Homologous Recombination Deficient, and PARP-inhibitor resistant cancer models (EORTC-NCI-AACR 2024) - "In contrast, niraparib or olaparib PARP inhibitor treatments failed to exhibit sensitivity in tumor cell proliferation assays (IC50, 0.3-4.6 mM). A differentiated tumor regression was observed in BRCAmutant (HCC1428 breast, HCC1395 breast) and HRD (SNU-601 ovarian) in vivo models treated with YL-18319 compared with niraparib or IDE-161 (PARG inhibitor)... The small molecule PARG inhibitor, YL-18319, demonstrated a highly potent activity in vitro and in vivo, as well as favorable pharmacologic properties. The evaluation of YL-18319 in a phase 1 dose escalation clinical trial for patients with advanced cancers is warranted."

Preclinical • Oncology • BRCA • HRD

IDE161, a potential first-in-class clinical candidate PARG inhibitor, selectively targets solid tumors with replication stress and DNA repair vulnerabilities (EORTC-NCI-AACR 2024) - P1 | "Finally, the singular consequences of PARG inhibition, in the context of drug-induced DNA damage, offers mechanism-based combination hypotheses for both approved and investigational new drugs in biomarker populations beyond those responsive to IDE161 monotherapy- several of which have been evaluated in relevant CDX models and demonstrated to deliver deep and durable responses including complete responses. These findings underpin the clinical development strategy currently underway for evaluation of IDE161 in biomarker selected patients with advanced or metastatic cancer."

Clinical • Oncology • Solid Tumor

IDEAYA Biosciences Announces Late-Breaker Oral Presentation of IDE397 Phase 1 Expansion Results in MTAP-Deletion Lung and Urothelial Cancer at the 36th Edition of the EORTC-NCI-AACR Symposium (PRNewswire) - "IDEAYA Biosciences, Inc...announced a late-breaking oral presentation of the Phase 1 expansion results of IDE397, a first-in-class, oral, MAT2A inhibitor in methylthioadenosine phosphorylase (MTAP)-deletion urothelial and non-small cell lung cancer (NSCLC) patients at the 36th edition of the EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics taking place on October 23 to 25, 2024, in Barcelona, Spain. In addition, IDEAYA will also have additional poster presentations at the EORTC-NCI-AACR Symposium highlighting preclinical data for the MAT2A and PARG programs."

P1 data • Preclinical • Non Small Cell Lung Cancer • Urothelial Cancer

IDEAYA Biosciences, Inc. Reports First Quarter 2024 Financial Results and Provides Business Update (PRNewswire) - "IDE161 is currently being evaluated in IDE161-001 (NCT05787587), a Phase 1/2 trial of IDE161 in solid tumors with HRD...Selection of an initial Phase 2 monotherapy expansion dose in HRD solid tumors is targeted in the second half of 2024. The Company is currently validating IDE161 combination opportunities preclinically and targeting identification of additional combination(s) in 2024....The Company is planning to evaluate IDE161 in a combination study with KEYTRUDA in patients with MSI-high and MSS endometrial cancer. A first-patient-in for this study is targeted in the second half of 2024."

New trial • Trial status • Endometrial Cancer • Gynecologic Cancers • Oncology • Solid Tumor • Uterine Cancer • HRD

IDEAYA Announces Clinical Collaboration to Evaluate IDE161 in Combination with KEYTRUDA (pembrolizumab) in Patients with Endometrial Cancer (PRNewswire) - "IDEAYA Biosciences, Inc...announced that it has entered into a clinical trial collaboration and supply agreement with Merck (known as MSD outside the US and Canada) to evaluate IDE161, the company's investigational, potential first-in-class, small molecule poly (ADP-ribose) glycohydrolase, or PARG, inhibitor, in combination with KEYTRUDA (pembrolizumab) Merck's anti-PD-1 therapy, in patients with microsatellite instability-, or MSI-, high and microsatellite stable, or MSS, endometrial cancer, in a Phase 1 clinical trial....Under the clinical trial collaboration and supply agreement, Merck will provide KEYTRUDA to IDEAYA, which will be the sponsor of the Phase 1 clinical combination trial."

Licensing / partnership • Endometrial Cancer • Gynecologic Cancers • Oncology • Solid Tumor

IDEAYA Biosciences, Inc. Reports Fourth Quarter and Full-Year 2023 Financial Results and Provides Business Update (PRNewswire) - "The Phase 1 trial (NCT05787587) is evaluating the safety, tolerability, pharmacokinetic and pharmacodynamic properties and preliminary efficacy of IDE161 in patients having tumors with homologous recombination deficiency (HRD)....The Phase 1 expansion trial continues to enroll in HRD solid tumor types, including ER+ HER-breast, colorectal, endometrial, and prostate cancers. Clinical program update(s) are expected in 2024. IDEAYA is also validating IDE161 combination opportunities preclinically and is targeting identification of potential combination(s) in 2024....IDEAYA, in collaboration with GSK, selected a Werner Helicase inhibitor for further development and IDEAYA earned a $3.0 million milestone from GSK in connection with IND-enabling studies....The companies are targeting IND submission in 2024."

IND • P1 data • Breast Cancer • Colorectal Cancer • Endometrial Cancer • Estrogen Receptor Positive Breast Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • Gynecologic Cancers • HER2 Breast Cancer • HER2 Negative Breast Cancer • Oncology • Prostate Cancer • Solid Tumor

IDEAYA Biosciences Announces Participation at the 42nd Annual J.P. Morgan Healthcare Conference and 2024 Corporate Guidance (PRNewswire) - P1 | N=68 | NCT05787587 | Sponsor: IDEAYA Biosciences | "Targeting IDE161 clinical program update(s) and enabling of clinical combination(s) in 2024; Preliminary IDE161 clinical efficacy observed in HRD solid tumors, including RECIST 1.1 partial responses in priority solid tumor types and >50% PSA reduction in a prostate cancer patient; Targeting ongoing enrollment of IDE161 Phase 1 expansion in HRD solid tumor priority types, including endometrial, colorectal, prostate, and ER+ HER2- breast cancers."

Clinical • P1 data • Trial status • Breast Cancer • Colorectal Cancer • Endometrial Cancer • Estrogen Receptor Positive Breast Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • Gynecologic Cancers • HER2 Breast Cancer • Oncology • Prostate Cancer • Solid Tumor • Uterine Cancer

A Study of PARG Inhibitor IDE161 in Participants With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=68 | Recruiting | Sponsor: IDEAYA Biosciences

Metastases • Trial completion date • Trial primary completion date • Breast Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • Hepatology • Oncology • Ovarian Cancer • Pancreatic Cancer • Prostate Cancer • Solid Tumor • HRD

IDEAYA Biosciences, Inc. Reports Third Quarter 2023 Financial Results and Provides Business Update (PRNewswire) - The IDEAYA Investor R&D Day will include participation from GSK and a key opinion leader that will showcase scientific insights and clinical development opportunities across IDEAYA's synthetic lethality pipeline, including IDE397 (MAT2A) in Phase 2, IDE161 (PARG) in Phase 1, GSK101/IDE705 (Pol Theta Helicase) in Phase 1, and the Werner Helicase program for which an IND submission is planned for 2024. In addition, IDEAYA will highlight its next generation initiatives in MTAP-deletion, including a wholly-owned program where a development candidate nomination is targeted in 2024, further advancing IDEAYA's multi-pronged strategy."

Clinical • IND • Oncology

IDEAYA Biosciences Announces Plans for Investor R&D Day and Participation in Jefferies London Healthcare Conference (PRNewswire) - "IDEAYA Biosciences, Inc...announced its participation in the Jefferies London Healthcare Conference and its plans to host an Investor R&D Day in December 2023....The IDEAYA Investor R&D Day will include participation from GSK and a key opinion leader that will showcase scientific insights and clinical development opportunities across IDEAYA's synthetic lethality pipeline, including IDE397 (MAT2A) in Phase 2, IDE161 (PARG) in Phase 1, and the GSK partnered programs. In addition, IDEAYA will highlight its next generation initiatives in MTAP-deletion, including a wholly-owned program where a development candidate nomination is targeted in 2024, further advancing IDEAYA's multi-pronged strategy."

Clinical • Oncology

IDEAYA Announces Top-Line Phase 2 Results at ESMO 2023 of Darovasertib and Crizotinib Combo in MUM, and Clinical Efficacy Updates for Neoadjuvant UM, GNAQ/11 Cutaneous Melanoma, and Synthetic Lethality Pipeline (PRNewswire) - P1 | N=68 | NCT05787587 | Sponsor: IDEAYA Biosciences | "There have been a total of 7 patients treated at the expansion dose as of the October 13 2023 cut-off date, of which 2 patients have not yet had a first scan tumor assessment. The earlier reported IDE161 partial response at first scan in a BRCA1/2 endometrial cancer patient, is now a confirmed PR by RECIST 1.1 at the second scan. At the IDE161 expansion dose, we have observed no drug-related discontinuations or SAEs as of the October 13, 2023 cut-off date."

P1 data • Endometrial Cancer • Gynecologic Cancers • Oncology • Solid Tumor

IDEAYA Receives Fast Track Designation for Potential First-in-Class PARG Inhibitor, IDE161, for Treatment of Pretreated, Platinum-Resistant Advanced or Metastatic Ovarian Cancer Patients having tumors with BRCA1/2 Mutations (PRNewswire) - "IDEAYA Biosciences...announces that the U.S. Food and Drug Administration (FDA) has granted Fast Track designation to IDEAYA's development program investigating IDE161, a potent and selective inhibitor of poly (ADP-ribose) glycohydrolase (PARG), for the treatment of adult patients having advanced or metastatic ovarian cancer with germline or somatic BRCA 1/2 mutations who are platinum resistant and have received prior antiangiogenic and poly (ADP-ribose) polymerase (PARP) inhibitor therapies."

Fast track designation • Ovarian Cancer • BRCA • BRCA1 • BRCA2

IDEAYA Biosciences Receives Fast Track Designation for IDE161 in a Second Indication for the Treatment of Pretreated, Advanced or Metastatic HR+, Her2-, BRCA1/2 mutant Breast Cancer (PRNewswire) - "IDEAYA Biosciences, Inc...announces that the U.S. Food and Drug Administration (FDA) has granted Fast Track designation to IDEAYA's development program investigating IDE161, a potent and selective inhibitor of poly (ADP-ribose) glycohydrolase (PARG), for the treatment of adult patients having advanced or metastatic hormone receptor positive (HR+), Her2- breast cancer with germline or somatic BRCA 1/2 mutations who have progressed following treatment with at least one line of a hormonal therapy, a CDK4/6 inhibitor therapy and a poly (ADP-ribose) polymerase (PARP) inhibitor therapy."

Fast track designation • Breast Cancer • Oncology • Solid Tumor

IDEAYA Announces Phase 1 Expansion and Preliminary Clinical Proof-of-Concept for Potential First-in-Class PARG Inhibitor IDE161 in HRD Solid Tumors (PRNewswire) - "IDEAYA Biosciences, Inc...announces initiation of a Phase 1 monotherapy expansion in the first-in-human clinical trial evaluating IDE161 (NCT05787587).... The Phase 1 first-in-human clinical trial is evaluating the safety, tolerability, pharmacokinetic and pharmacodynamic properties and preliminary efficacy of IDE161 in patients having tumors with homologous recombination deficiency (HRD)."

Trial status • Breast Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • Gynecologic Cancers • Oncology • Ovarian Cancer • Pancreatic Cancer • Prostate Cancer • Solid Tumor

A Study of PARG Inhibitor IDE161 in Participants With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=68 | Recruiting | Sponsor: IDEAYA Biosciences | Not yet recruiting ➔ Recruiting

Enrollment open • Breast Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • Hepatology • Oncology • Ovarian Cancer • Pancreatic Cancer • Prostate Cancer • Solid Tumor • HRD

IDE161, a potential first-in-class clinical candidate PARG inhibitor, selectively targets homologous-recombination-deficient and PARP inhibitor resistant breast and ovarian tumors (AACR 2023) - "Moreover, studies in cell lines, tumors and tissues revealed that dose and time-dependent accumulation of PAR chains serves as a robust proximal pharmacodynamic biomarker indicative of PARG target engagement. IDE161 is a novel targeted therapy that exploits the synthetic lethal relationship between PARG and genomic instability, thus leading to selective anti-proliferative effects in tumors harboring defects in the HR pathway."

Clinical • Gastric Cancer • Gastrointestinal Cancer • Oncology • Ovarian Cancer • Solid Tumor • HRD