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    DRUG CLASS:

    WEE1 inhibitor

    Related drugs:
    1d
    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)
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    adavosertib (AZD1775)
    7d
    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
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    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • CCNE1 (Cyclin E1) • BRCA (Breast cancer early onset)
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    BRCA2 mutation • BRCA1 mutation • BRCA mutation
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    azenosertib (ZN-c3)
    15d
    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)
    19d
    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
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    gemcitabine • azenosertib (ZN-c3)
    1m
    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
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    HER-2 positive
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    azenosertib (ZN-c3)
    1m
    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
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    gemcitabine • azenosertib (ZN-c3)
    1m
    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
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    Zejula (niraparib) • azenosertib (ZN-c3)
    1m
    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
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    azenosertib (ZN-c3)
    1m
    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
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    CCNE1 (Cyclin E1)
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    HER-2 amplification • HER-2 expression
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    Enhertu (fam-trastuzumab deruxtecan-nxki) • azenosertib (ZN-c3)
    1m
    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
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    ABCC1 (ATP Binding Cassette Subfamily C Member 1) • MSH3 (MutS Homolog 3) • CDK1 (Cyclin-dependent kinase 1)
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    adavosertib (AZD1775) • Farydak (panobinostat)
    1m
    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
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    TP53 mutation
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    gemcitabine • adavosertib (AZD1775)
    2ms
    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
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    Imfinzi (durvalumab) • adavosertib (AZD1775)