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    DRUG:

    IDE161

    i
    Other names: IDE161, IDE-161, IDE 161
    Company:
    Ideaya Biosci
    Drug class:
    PARG inhibitor
    18d
    A Study of PARG Inhibitor IDE161 in Participants with Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=216, Recruiting, 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
    |
    HRD (Homologous Recombination Deficiency)
    |
    HRD
    |
    Keytruda (pembrolizumab) • IDE161
    11ms
    A Study of PARG Inhibitor IDE161 in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=68, Recruiting, IDEAYA Biosciences
    Trial completion date • Trial primary completion date • Metastases
    |
    HRD (Homologous Recombination Deficiency)
    |
    HRD
    |
    IDE161
    over1year
    A Study of PARG Inhibitor IDE161 in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=68, Recruiting, IDEAYA Biosciences | Not yet recruiting --> Recruiting
    Enrollment open
    |
    HRD (Homologous Recombination Deficiency)
    |
    HRD
    |
    IDE161
    over1year
    A Study of PARG Inhibitor IDE161 in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=68, Not yet recruiting, IDEAYA Biosciences
    New P1 trial • Metastases
    |
    HRD (Homologous Recombination Deficiency)
    |
    HRD
    |
    IDE161
    over1year
    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 • PARP Biomarker
    |
    HRD (Homologous Recombination Deficiency)
    |
    IDE161
    over3years
    [VIRTUAL] Synthetic lethality of PARG inhibition in tumors with homologous recombination deficiencies (AACR 2021)
    Using cellular proliferation assays and xenograft models, we find that PARGi increases the cellular levels of PAR and significantly decreases the viability of HR-deficient cancer cell lines. Furthermore, inhibition of cell proliferation by PARGi is antagonized by PARPi, which is consistent with an on-target cellular mechanism of action (MOA). In conclusion, PARGi induces significant accumulation of PAR chains and decreases cell proliferation both in vitro and in vivo in HR-deficient tumor cells.
    PARP Biomarker • Synthetic lethality
    |
    HRD (Homologous Recombination Deficiency) • XRCC1 (X-Ray Repair Cross Complementing 1)
    |
    HRD
    |
    IDE161