^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    DRUG CLASS:

    WEE1 inhibitor

    Related drugs:
    13d
    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)
    13d
    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)
    13d
    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)
    14d
    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)
    19d
    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)
    20d
    WEE1 Stabilizes MYC to Promote Therapeutic Resistance in Esophageal Adenocarcinoma. (PubMed, Cancer Lett)
    These findings reveal a novel cytoplasmic function of WEE1 in sustaining MYC stability and chemoresistance. Targeting WEE1 destabilizes MYC and enhances therapeutic response, supporting the combination of MK-1775 and Panobinostat as a promising treatment strategy for EAC.
    Journal
    |
    ABCC1 (ATP Binding Cassette Subfamily C Member 1) • MSH3 (MutS Homolog 3) • CDK1 (Cyclin-dependent kinase 1)
    |
    adavosertib (AZD1775) • Farydak (panobinostat)
    21d
    NCI-2014-00620: Gemcitabine Hydrochloride With or Without WEE1 Inhibitor MK-1775 in Treating Patients With Recurrent Ovarian, Primary Peritoneal, or Fallopian Tube Cancer (clinicaltrials.gov)
    P2, N=124, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Feb 2026 --> Mar 2027
    Trial completion date • Platinum resistant
    |
    TP53 mutation
    |
    gemcitabine • adavosertib (AZD1775)
    27d
    REFMAL 412: Safety, Tolerability and Pharmacokinetics of AZD1775 (Adavosertib) Plus MEDI4736 (Durvalumab) in Patients With Advanced Solid Tumours (clinicaltrials.gov)
    P1, N=56, Completed, AstraZeneca | Active, not recruiting --> Completed
    Trial completion
    |
    Imfinzi (durvalumab) • adavosertib (AZD1775)
    29d
    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)
    1m
    A Study to Evaluate Safety and Preliminary Anti-tumor Activity of Debio 0123 as Monotherapy in Adult Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=66, Active, not recruiting, Debiopharm International SA | N=155 --> 66 | Trial completion date: Jun 2027 --> Apr 2026
    Enrollment change • Trial completion date
    |
    CCNE1 (Cyclin E1)
    |
    zedoresertib (Debio 0123)
    1m
    ROR1-PI3K/AKT signaling drives adaptive resistance to cell cycle blockade in TP53 mutated ovarian cancer. (PubMed, Cell Death Dis)
    In this study, we developed long-term resistant (lt-res, several months) pre-clinical models of two drugs inducing mitotic arrest in TP53-mutated cells: adavosertib (ADA), an investigational WEE1 inhibitor targeting the DNA damage response and currently evaluated in clinical trials, and paclitaxel (PTX), a widely used chemotherapeutic agent in cancer care targeting microtubules. Notably, upregulation of receptor tyrosine kinases, such as ROR1, was observed in both ADA and PTX lt-res models with activated PI3K/AKT signaling. Targeting ROR1 with zilovertamab-vedotin, a monoclonal antibody-drug conjugate, resulted in enhanced cytotoxicity, demonstrating a new approach against recurrent drug-resistant ovarian cancer.
    Journal
    |
    TP53 (Tumor protein P53) • ROR1 (Receptor Tyrosine Kinase Like Orphan Receptor 1)
    |
    TP53 mutation
    |
    paclitaxel • adavosertib (AZD1775) • zilovertamab vedotin (MK-2140)
    2ms
    A Study to Evaluate Safety and Preliminary Anti-tumor Activity of Debio 0123 as Monotherapy in Adult Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=155, Active, not recruiting, Debiopharm International SA | Trial primary completion date: Jan 2026 --> Apr 2026
    Trial primary completion date
    |
    CCNE1 (Cyclin E1)
    |
    zedoresertib (Debio 0123)