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    DRUG CLASS:

    WEE1 inhibitor

    Related drugs:
    12d
    Debio 0123-SCLC-104: Debio 0123 in Combination With Carboplatin and Etoposide in Adult Participants With Small Cell Lung Cancer That Recurred or Progressed After Previous Standard Platinum-Based Therapy (clinicaltrials.gov)
    P1, N=34, Terminated, Debiopharm International SA | Active, not recruiting --> Terminated; The trial was concluded for strategic reasons.
    Trial termination
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    carboplatin • etoposide IV • zedoresertib (Debio 0123)
    17d
    Testing the Sequential Combination of the Anti-cancer Drugs Olaparib Followed by Adavosertib (AZD1775) in Patients With Advanced Solid Tumors With Selected Mutations and PARP Resistance, STAR Study (clinicaltrials.gov)
    P1, N=13, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Sep 2026 --> Dec 2026
    Trial completion date
    |
    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • FANCA (FA Complementation Group A) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1) • CD4 (CD4 Molecule)
    |
    BRCA2 mutation • BRCA1 mutation • BRIP1 mutation
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    Lynparza (olaparib) • adavosertib (AZD1775)
    17d
    Testing the Addition of an Anti-cancer Drug, Adavosertib, to Radiation Therapy for Patients With Incurable Esophageal and Gastroesophageal Junction Cancers (clinicaltrials.gov)
    P1, N=4, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2025 --> Dec 2026
    Trial completion date
    |
    adavosertib (AZD1775)
    22d
    Testing AZD1775 in Advanced Solid Tumors That Have a Mutation Called SETD2 (clinicaltrials.gov)
    P2, N=18, Active, not recruiting, National Cancer Institute (NCI) | N=60 --> 18 | Trial completion date: Mar 2026 --> Apr 2027
    Enrollment change • Trial completion date
    |
    SETD2 (SET Domain Containing 2, Histone Lysine Methyltransferase)
    |
    adavosertib (AZD1775)
    22d
    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
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    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
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    adavosertib (AZD1775) • azenosertib (ZN-c3)
    24d
    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)
    26d
    Discovery of Naphthyridinone Derivatives as Selective PKMYT1/WEE1 Dual Inhibitors for Cancer Therapy. (PubMed, J Med Chem)
    In colorectal cancer organoids, 24 outperformed our prior PKMYT1 inhibitor (6), RP-6306, and WEE1 inhibitor AZD1775, with efficacy correlating to improved WEE1 activity. Compound 24 also showed favorable in vitro ADME and early safety profiles, supporting dual checkpoint targeting in checkpoint-deficient cancers.
    Journal
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    CDK1 (Cyclin-dependent kinase 1) • PKMYT1 (Protein Kinase Membrane Associated Tyrosine/Threonine 1)
    |
    adavosertib (AZD1775)
    1m
    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
    |
    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)