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    DRUG:

    azenosertib (ZN-c3)

    i
    Other names: ZN-c3, ZN c3, ZNc3
    Company:
    Zentalis Pharma
    Drug class:
    WEE1 inhibitor
    Related drugs:
    16d
    Discovery of APO-50815, a potent WEE1 kinase inhibitor with exceptional efficacy against patient-derived colorectal cancer organoids. (PubMed, Eur J Med Chem)
    When tested against TP53-mutated colorectal cancer (CRC) patient-derived organoids (PDOs) grown from peritoneal and liver metastases, 14 exhibited outstanding anticancer efficacy, surpassing previously reported branched alkane counterpart 3, as well as clinical candidates AZD1775 (1) and ZN-c3 (2). Against primary CRC PDOs (TP53-WT, BRAF-V600E, KRAS-WT), 14 profoundly elevated DNA damage and replication stress compared to 1, while amplifying cellular apoptosis, confirming a broadly similar but superior mode of action. Owing to its highly selective and exemplary anticancer efficacy, 14 represents a valuable tool compound for drug testing investigations against primary and metastatic CRCs, especially in the context of PDOs.
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene)
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    TP53 mutation • BRAF V600E • KRAS mutation • BRAF V600 • TP53 wild-type • KRAS wild-type
    |
    adavosertib (AZD1775) • azenosertib (ZN-c3)
    18d
    ASPENOVA: A Study of Azenosertib (ZN-c3) Versus Investigator's Choice Chemotherapy in Subjects With Platinum-Resistant High-Grade Serous Ovarian, Primary Peritoneal, or Fallopian Tube Cancers Positive for Cyclin E1 Protein Expression (clinicaltrials.gov)
    P3, N=420, Not yet recruiting, K-Group, Beta, Inc., a wholly owned subsidiary of Zentalis Pharmaceuticals, Inc
    New P3 trial • Platinum resistant
    |
    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • CCNE1 (Cyclin E1) • BRCA (Breast cancer early onset)
    |
    BRCA2 mutation • BRCA1 mutation • BRCA mutation
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    paclitaxel • azenosertib (ZN-c3)
    25d
    DENALI: A Study of Azenosertib (ZN-c3) in Subjects With Platinum-Resistant High-Grade Serous Ovarian, Fallopian Tube or Primary Peritoneal Cancer (clinicaltrials.gov)
    P2, N=310, Recruiting, K-Group, Beta, Inc., a wholly owned subsidiary of Zentalis Pharmaceuticals, Inc | N=170 --> 310
    Enrollment change • Platinum resistant
    |
    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • CCNE1 (Cyclin E1) • BRCA (Breast cancer early onset)
    |
    BRCA2 mutation • BRCA1 mutation • BRCA mutation
    |
    azenosertib (ZN-c3)
    1m
    ZN-c3-002: A Study of Azenosertib (ZN-c3) in Patients With Ovarian Cancer (clinicaltrials.gov)
    P1, N=172, Recruiting, K-Group, Beta, Inc., a wholly owned subsidiary of Zentalis Pharmaceuticals, Inc | Trial completion date: Feb 2027 --> Jun 2028 | Trial primary completion date: Dec 2024 --> Jun 2028
    Trial completion date • Trial primary completion date
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    Avastin (bevacizumab) • carboplatin • gemcitabine • paclitaxel • pegylated liposomal doxorubicin • azenosertib (ZN-c3)
    1m
    ZN-c3-003: A Study of Azenosertib (ZN-c3) in Combination With Gemcitabine in Subjects With Osteosarcoma (clinicaltrials.gov)
    P1, N=31, Completed, K-Group, Beta, Inc., a wholly owned subsidiary of Zentalis Pharmaceuticals, Inc | Phase classification: P1/2 --> P1
    Phase classification
    |
    gemcitabine • azenosertib (ZN-c3)
    2ms
    TETON: A Study of Azenosertib (ZN-c3) in Women With Recurrent or Persistent Uterine Serous Carcinoma (clinicaltrials.gov)
    P2, N=92, Completed, K-Group, Beta, Inc., a wholly owned subsidiary of Zentalis Pharmaceuticals, Inc | Recruiting --> Completed | Trial completion date: May 2025 --> Oct 2025 | Trial primary completion date: Nov 2024 --> Oct 2025
    Trial completion • Trial completion date • Trial primary completion date
    |
    HER-2 positive
    |
    azenosertib (ZN-c3)
    2ms
    ZN-c3-003: A Study of Azenosertib (ZN-c3) in Combination With Gemcitabine in Subjects With Osteosarcoma (clinicaltrials.gov)
    P1/2, N=31, Completed, K-Group, Beta, Inc., a wholly owned subsidiary of Zentalis Pharmaceuticals, Inc | Active, not recruiting --> Completed | N=84 --> 31
    Trial completion • Enrollment change
    |
    gemcitabine • azenosertib (ZN-c3)
    2ms
    MAMMOTH: A Study of Azenosertib (ZN-c3) and Niraparib in Subjects With Platinum-Resistant Ovarian Cancer (clinicaltrials.gov)
    P1/2, N=117, Completed, K-Group, Beta, Inc., a wholly owned subsidiary of Zentalis Pharmaceuticals, Inc | Active, not recruiting --> Completed | Trial completion date: May 2025 --> Jan 2026 | Trial primary completion date: May 2025 --> Oct 2025
    Trial completion • Trial completion date • Trial primary completion date • Platinum resistant
    |
    Zejula (niraparib) • azenosertib (ZN-c3)
    2ms
    ZN-c3-001: A Study of Azenosertib (ZN-c3) in Participants With Solid Tumors (clinicaltrials.gov)
    P1, N=274, Completed, K-Group, Beta, Inc., a wholly owned subsidiary of Zentalis Pharmaceuticals, Inc | Recruiting --> Completed | N=146 --> 274 | Trial completion date: Aug 2023 --> May 2025 | Trial primary completion date: May 2023 --> May 2025
    Trial completion • Enrollment change • Trial completion date • Trial primary completion date
    |
    azenosertib (ZN-c3)
    2ms
    Testing the Combination of the Anticancer Drugs Trastuzumab Deruxtecan (DS-8201a) and Azenosertib (ZN-c3) in Patients With Stomach or Other Solid Tumors (clinicaltrials.gov)
    P1, N=48, Recruiting, National Cancer Institute (NCI) | Suspended --> Recruiting
    Enrollment open
    |
    CCNE1 (Cyclin E1)
    |
    HER-2 amplification • HER-2 expression
    |
    Enhertu (fam-trastuzumab deruxtecan-nxki) • azenosertib (ZN-c3)
    2ms
    Azenosertib in Uterine Serous Carcinoma: Biomarker Study (clinicaltrials.gov)
    P2, N=25, Recruiting, Joyce Liu, MD | Trial completion date: Jan 2027 --> Jan 2028 | Trial primary completion date: Jan 2026 --> Jan 2027
    Trial completion date • Trial primary completion date
    |
    PD-L1 (Programmed death ligand 1)
    |
    MSI-H/dMMR
    |
    azenosertib (ZN-c3)
    3ms
    Testing the Combination of the Anticancer Drugs Trastuzumab Deruxtecan (DS-8201a) and Azenosertib (ZN-c3) in Patients With Stomach or Other Solid Tumors (clinicaltrials.gov)
    P1, N=48, Suspended, National Cancer Institute (NCI) | Recruiting --> Suspended
    Trial suspension
    |
    CCNE1 (Cyclin E1)
    |
    HER-2 amplification • HER-2 expression
    |
    Enhertu (fam-trastuzumab deruxtecan-nxki) • azenosertib (ZN-c3)