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    DRUG CLASS:

    Estrogen receptor alpha degrader

    Related drugs:
    Associations

    News

    Trials
    3ms
    AC699-001: Study of AC699 in Patients With Estrogen Receptor Positive/Human Epidermal Growth Factor Receptor 2 Negative (ER+/HER2-) Locally Advanced or Metastatic Breast Cancer (clinicaltrials.gov)
    P1, N=100, Active, not recruiting, Accutar Biotechnology Inc | Recruiting --> Active, not recruiting | N=60 --> 100 | Trial completion date: Dec 2024 --> May 2026 | Trial primary completion date: Jul 2024 --> Mar 2026
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
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    ER positive
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    AC699
    7ms
    VERITAC: A Phase 1/2 Trial of ARV-471 Alone and in Combination With Palbociclib (IBRANCE®) in Patients With ER+/HER2- Locally Advanced or Metastatic Breast Cancer (clinicaltrials.gov)
    P1/2, N=217, Active, not recruiting, Arvinas Estrogen Receptor, Inc. | Trial completion date: Mar 2025 --> Aug 2025
    Trial completion date
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    HER-2 (Human epidermal growth factor receptor 2)
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    HER-2 negative
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    Ibrance (palbociclib) • vepdegestrant (ARV-471)
    7ms
    VERITAC-3: A Study of Vepdegestrant (ARV-471, PF-07850327) Plus Palbociclib Versus Letrozole Plus Palbociclib in Participants With Estrogen Receptor Positive, Human Epidermal Growth Factor Negative Advanced Breast Cancer (clinicaltrials.gov)
    P3, N=59, Active, not recruiting, Pfizer | N=1180 --> 59 | Trial completion date: Jul 2030 --> Dec 2026 | Trial primary completion date: Aug 2028 --> Dec 2026
    Enrollment change • Trial completion date • Trial primary completion date
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
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    HER-2 negative
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    Ibrance (palbociclib) • letrozole • vepdegestrant (ARV-471)
    7ms
    A Study to Learn How a Tablet Compared With an IV Infusion of the Study Medicine Called Vepdegestrant is Taken up Into the Blood in Healthy Adults (clinicaltrials.gov)
    P1, N=10, Recruiting, Pfizer | Not yet recruiting --> Recruiting
    Enrollment open
    |
    vepdegestrant (ARV-471)
    8ms
    TACTIVE-K: A Study to Learn About Vepdegestrant When Given With PF-07220060 to People With Advanced or Metastatic Breast Cancer. (clinicaltrials.gov)
    P1/2, N=65, Active, not recruiting, Pfizer | Recruiting --> Active, not recruiting
    Enrollment closed
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    vepdegestrant (ARV-471) • atirmociclib (PF-07220060)
    9ms
    A Study to Learn How a Tablet Compared With an IV Infusion of the Study Medicine Called Vepdegestrant is Taken up Into the Blood in Healthy Adults (clinicaltrials.gov)
    P1, N=10, Not yet recruiting, Pfizer
    New P1 trial
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    vepdegestrant (ARV-471)
    9ms
    Vepdegestrant for the treatment of HR+/HER2- breast cancer. (PubMed, Expert Opin Pharmacother)
    The results of the phase III VERITAC-2 study, comparing vepdegestrant with fulvestrant, are expected to be available in 2025, and will provide the first data on the true clinical significance of vepdegestrant. Several phase III studies of combinations with vepdegestrant including + atirimociclib (a cyclin-dependent kinase 4 inhibitor) have been or are planned to be conducted. The results of these may not only transform the treatment landscape for advanced HR+/HER2- breast cancer but may pave the way for PROTAC as a new class of anti-cancer drugs that may make previously undruggable targets druggable.
    Review • Journal
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HR positive • HER-2 negative • ESR1 mutation
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    fulvestrant • vepdegestrant (ARV-471)
    10ms
    C4891024: TACTIVE-U: A Study to Learn About the Study Medicine (Vepdegestrant) When Given With Other Medicines in People With Advanced or Metastatic Breast Cancer. (Sub-Study C) (clinicaltrials.gov)
    P1/2, N=11, Active, not recruiting, Pfizer | Recruiting --> Active, not recruiting | N=67 --> 11 | Trial completion date: Jan 2027 --> Nov 2025 | Trial primary completion date: Jul 2026 --> Nov 2025
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
    |
    vepdegestrant (ARV-471) • samuraciclib (CT7001)
    11ms
    A Study to Learn About the Study Medicine Called Vepdegestrant (ARV-471, PF-07850327) in People With ER+/HER2- Advanced Breast Cancer in China (clinicaltrials.gov)
    P1, N=9, Completed, Pfizer | Active, not recruiting --> Completed
    Trial completion
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 negative
    |
    vepdegestrant (ARV-471)
    11ms
    Unleashing the Power of Covalent Drugs for Protein Degradation. (PubMed, Med Res Rev)
    Two prominent PROTACs, ARV-471 and ARV-110, are currently undergoing phase III and II clinical trials, respectively. The concept of covalent degradation has also been utilized in various new forms of degraders, including covalent molecule glue (MG), in-cell click-formed proteolysis targeting chimera (CLIPTAC), HaloPROTAC, lysosome-targeting chimera (LYTAC) and GlueTAC. This review focuses on recent advancements in covalent degraders beyond covalent PROTACs and examines obstacles and future directions pertinent to this field.
    Review • Journal
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    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • KEAP1 (Kelch Like ECH Associated Protein 1) • BTK (Bruton Tyrosine Kinase) • DDB1 (Damage Specific DNA Binding Protein 1)
    |
    bavdegalutamide (ARV-110) • vepdegestrant (ARV-471)
    11ms
    C4891038: A Study to Learn How Different Tablets of the Study Medicine Vepdegestrant Are Taken up Into the Blood in Healthy Adults (clinicaltrials.gov)
    P1, N=12, Recruiting, Pfizer | Not yet recruiting --> Recruiting
    Enrollment open
    |
    vepdegestrant (ARV-471)
    1year
    Discovery of ERD-12310A as an Exceptionally Potent and Orally Efficacious PROTAC Degrader of Estrogen Receptor α (ERα). (PubMed, J Med Chem)
    ERD-12310A achieved a DC50 value of 47 pM and is 10 times more potent than ARV-471...Importantly, ERD-12310A achieved strong tumor growth inhibition in MCF-7 xenograft tumors harboring the clinically relevant ESR1Y537S mutation, which confers resistance to traditional antiestrogens. Our data position ERD-12310A as a promising candidate for further development as a potential therapy for ER+ breast cancer.
    Journal
    |
    ER (Estrogen receptor)
    |
    ER positive • ER Y537S
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    vepdegestrant (ARV-471)