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    DRUG:

    APR-1051

    i
    Other names: APR-1051, ATRN-1051, ATRN-W1051
    Company:
    Aprea
    Drug class:
    WEE1 inhibitor
    Related drugs:
    5ms
    Targeting WEE1 Kinase for Breast Cancer Therapeutics: An Update. (PubMed, Int J Mol Sci)
    Adavosertib's clinical promise was challenged by inter-individual variations in response and side effects. Because of these promising preclinical outcomes, other WEE1 kinase inhibitors (Azenosertib, SC0191, IMP7068, PD0407824, PD0166285, WEE1-IN-5, Zedoresertib, WEE1-IN-8, and ATRN-1051) are being developed, with several currently being evaluated in clinical trials or as an adjuvant to chemotherapies...Reliable predictors of clinical responses based on mechanistic insights remain an important unmet need. Herein, we review the role of WEE1 inhibition therapy in breast cancer.
    Review • Journal
    |
    STING (stimulator of interferon response cGAMP interactor 1) • CDK2 (Cyclin-dependent kinase 2) • CDC25C (Cell Division Cycle 25C) • CDK1 (Cyclin-dependent kinase 1) • PKMYT1 (Protein Kinase Membrane Associated Tyrosine/Threonine 1) • GNRP (Ras-Specific Guanine Nucleotide-Releasing Factor 1)
    |
    adavosertib (AZD1775) • azenosertib (ZN-c3) • SC0191 • APR-1051 • IMP7068
    over1year
    APR-1051-001: Study of APR-1051 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=79, Recruiting, Aprea Therapeutics | Not yet recruiting --> Recruiting
    Enrollment open
    |
    APR-1051
    almost2years
    Study of APR-1051 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=79, Not yet recruiting, Aprea Therapeutics
    New P1 trial
    |
    APR-1051
    over2years
    ATRN-119 and ATRN-W1051: Novel and potentially well tolerated ATR and WEE1 inhibitors for targeted cancer treatment (AACR 2023)
    Importantly, ATRN-W1051 exhibits low off-target inhibition of the PLK family of kinases (PLK1, PLK2 and PLK3), which are substantially inhibited by the leading WEE1i in the clinic (AZD1775 and ZN-c3)1. These preclinical data suggest that ATRN-W1051 may be a potential therapeutic candidate for CCNE1-overexpressing HGSOC. Together, ATRN-119 and ATRN-W1051 provide promising alternative DNA replication checkpoint inhibitors for the treatment of a variety of cancers.
    BRCA Biomarker • PARP Biomarker
    |
    BRCA2 (Breast cancer 2, early onset) • CCNE1 (Cyclin E1) • PLK1 (Polo Like Kinase 1) • PLK2 (Polo Like Kinase 2)
    |
    CCNE1 amplification • CCNE1 overexpression
    |
    adavosertib (AZD1775) • azenosertib (ZN-c3) • APR-1051 • ATRN-119