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    DRUG CLASS:

    POLQ inhibitor

    Related drugs:
    16h
    A Study to Investigate the Safety, Tolerability, Pharmacokinetics (PK), and Preliminary Anticancer Activity of GSK4524101 Alone or With Niraparib in Participants With Solid Tumors (clinicaltrials.gov)
    P1/2, N=42, Active, not recruiting, GlaxoSmithKline | Recruiting --> Active, not recruiting | N=135 --> 42 | Trial completion date: Jun 2027 --> Jun 2026 | Trial primary completion date: Jun 2027 --> Jun 2026
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    Zejula (niraparib)
    7d
    A Study of ART4215 for the Treatment of Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
    P1, N=93, Completed, Artios Pharma Ltd | N=390 --> 93 | Active, not recruiting --> Completed
    Trial completion • Enrollment change
    |
    HER-2 (Human epidermal growth factor receptor 2) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
    |
    HER-2 negative
    |
    Talzenna (talazoparib) • Zejula (niraparib) • ART4215
    18d
    POLAR: Phase 1 Trial of RP-3467 Alone and in Combination With Olaparib in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=26, Terminated, Repare Therapeutics | Trial completion date: Dec 2028 --> Oct 2025 | Active, not recruiting --> Terminated | Trial primary completion date: Oct 2026 --> Oct 2025; Sponsor decided to terminate study early
    Trial completion date • Trial termination • Trial primary completion date • First-in-human
    |
    Lynparza (olaparib)
    1m
    Discovery of 1-(arylacetyl)-2-phenyl-pyrrolidine Derivatives as Novel POLθ-pol Inhibitors via Structure-Based Virtual Screening and Fragment Fusion. (PubMed, Drug Dev Res)
    The followed similarity research obtained a more potent analogue SS-5, which was hybridized with RP-6685 to get 1-(phenylacetyl)-2-phenyl-pyrrolidine derivative F-1. It showed potent POLθ inhibitory activity with an IC50 value of 170 nM, and good anti-proliferative activity against BRCA2-deficient DLD1 and HCT116 cell lines, with IC50 values of 4.39 μM and 4.79 μM, respectively. Further MD simulations and interaction analysis disclosed the possible binding mode of F-1 with POLθ-pol.
    Journal
    |
    BRCA2 (Breast cancer 2, early onset) • BRCA (Breast cancer early onset)
    1m
    MOMA-313-001: Study of Orally Administered MOMA-313 in Participants With Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
    P1, N=220, Recruiting, MOMA Therapeutics | N=158 --> 220
    Enrollment change
    |
    Lynparza (olaparib)
    4ms
    ART6043C001: Study of ART6043 in Advanced/Metastatic Solid Tumors Patients (clinicaltrials.gov)
    P1/2, N=220, Active, not recruiting, Artios Pharma Ltd | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    Lynparza (olaparib) • ART6043
    5ms
    POLAR: Phase 1 Trial of RP-3467 Alone and in Combination With Olaparib in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=26, Active, not recruiting, Repare Therapeutics | Recruiting --> Active, not recruiting | N=52 --> 26
    Enrollment closed • Enrollment change
    |
    Lynparza (olaparib)
    5ms
    The Discovery of RP-2119: A Potent, Selective, and Orally Bioavailable Polθ ATPase Inhibitor. (PubMed, J Med Chem)
    Further optimization of potency and ADME properties led to the identification of RP-2119 with robust in vitro cellular activity in a wide range of HR-deficient cancer cell lines. In HR-deficient cell line- and patient-derived mouse xenografts, RP-2119 demonstrated strong synergy with the PARP inhibitor, olaparib, without exacerbating its hematological toxicity.
    Journal • BRCA Biomarker • PARP Biomarker
    |
    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
    |
    Lynparza (olaparib) • RP-2119
    5ms
    Study of SYN818 With Olaparib for the Treatment of Locally Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
    P1, N=110, Recruiting, Hangzhou SynRx Therapeutics Biomedical Technology Co., Ltd
    New P1 trial
    |
    Lynparza (olaparib)
    6ms
    SYN-818-101: Study of SYN818 for the Treatment of Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
    P1, N=30, Recruiting, Hangzhou SynRx Therapeutics Biomedical Technology Co., Ltd | Not yet recruiting --> Recruiting
    Enrollment open
    |
    BRCA (Breast cancer early onset)
    8ms
    A Study to Investigate the Safety, Tolerability, Pharmacokinetics (PK), and Preliminary Anticancer Activity of GSK4524101 Alone or With Niraparib in Participants With Solid Tumors (clinicaltrials.gov)
    P1/2, N=135, Recruiting, GlaxoSmithKline | Trial completion date: Nov 2029 --> Jun 2027 | Trial primary completion date: Dec 2027 --> Jun 2027
    Trial completion date • Trial primary completion date
    |
    Zejula (niraparib)
    8ms
    Phase 1 Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of DAT-1604 in Advanced Solid Tumor (clinicaltrials.gov)
    P1, N=228, Not yet recruiting, Danatlas Pharmaceuticals Co., Ltd
    New P1 trial