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    DRUG CLASS:

    Selective estrogen receptor α degrader

    Related drugs:
    3d
    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 | Trial completion date: Apr 2026 --> Dec 2026 | Trial primary completion date: Apr 2026 --> Dec 2026
    Trial completion date • Trial primary completion date
    |
    TP53 mutation
    |
    Veppanu (vepdegestrant) • samuraciclib (CT7001)
    10d
    VERITAC-2: A Study to Learn About a New Medicine Called Vepdegestrant (ARV-471, PF-07850327) in People Who Have Advanced Metastatic Breast Cancer (clinicaltrials.gov)
    P3, N=624, Active, not recruiting, Pfizer | N=219 --> 624
    Enrollment change
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 negative
    |
    fulvestrant • Veppanu (vepdegestrant)
    25d
    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, Completed, Arvinas Estrogen Receptor, Inc. | Active, not recruiting --> Completed
    Trial completion
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    Ibrance (palbociclib) • Veppanu (vepdegestrant)
    1m
    A Study to Learn How the Body Processes the Study Medicine Called Vepdegestrant in People With Loss of Liver Function (clinicaltrials.gov)
    P1, N=24, Recruiting, Pfizer | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Veppanu (vepdegestrant)
    2ms
    Insights Into Vepdegestrant (ARV-471): The First-in-Class Estrogen Receptor Proteolysis-Targeting Chimera Approaching Food and Drug Administration Approval for Breast Cancer. (PubMed, ChemMedChem)
    On June 6, 2025, Arvinas and Pfizer submitted a New Drug Application (NDA) for vepdegestrant to the U.S. Food and Drug Administration (FDA), representing an important step in the clinical translation of PROTAC technology. This review summarizes the design, synthesis, degradation mechanism, preclinical pharmacology, and clinical development of vepdegestrant and discusses the broader implications and future prospects of oral PROTAC-based ER degraders in breast cancer therapy.
    Review • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    ER positive • HER-2 negative • ESR1 mutation • EGFR positive
    |
    Veppanu (vepdegestrant)
    2ms
    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=71, Active, not recruiting, Pfizer | Trial completion date: Mar 2026 --> Sep 2026
    Trial completion date
    |
    Veppanu (vepdegestrant) • atirmociclib (PF-07220060)
    3ms
    Effect of carbamazepine on the pharmacokinetics of vepdegestrant, a PROteolysis TArgeting Chimera estrogen receptor degrader, in healthy adults. (PubMed, Br J Clin Pharmacol)
    Coadministration of multiple doses of carbamazepine 200 mg, a strong CYP3A4 inducer, with a single dose of vepdegestrant 200 mg resulted in a modest (36%) decrease in plasma vepdegestrant exposure. A single dose of vepdegestrant 200 mg was well tolerated in healthy adult participants.
    PK/PD data • Journal
    |
    ER (Estrogen receptor) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
    |
    Veppanu (vepdegestrant)
    3ms
    TACTIVE-U Sub-Study A: 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 A) (clinicaltrials.gov)
    P1/2, N=37, Active, not recruiting, Pfizer | Trial completion date: Mar 2026 --> Sep 2026 | Trial primary completion date: Mar 2026 --> Sep 2026
    Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    Verzenio (abemaciclib) • Veppanu (vepdegestrant)
    4ms
    The Effect of Itraconazole on the Pharmacokinetics of Vepdegestrant, a PROteolysis TArgeting Chimera Estrogen Receptor Degrader, in Healthy Adult Participants. (PubMed, Clin Ther)
    Coadministration of multiple doses of itraconazole, a strong CYP3A4 inhibitor, increased vepdegestrant exposure by 69%, suggesting the involvement of CYP3A4-mediated metabolism, albeit not predominantly, in vepdegestrant elimination.
    PK/PD data • Journal • First-in-human
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    ER positive • HER-2 negative • EGFR positive
    |
    Veppanu (vepdegestrant) • itraconazole
    6ms
    A Study to Learn How the Body Processes the Study Medicine Called Vepdegestrant in People With Loss of Liver Function (clinicaltrials.gov)
    P1, N=24, Not yet recruiting, Pfizer
    New P1 trial
    |
    Veppanu (vepdegestrant)
    6ms
    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 | Trial completion date: Nov 2025 --> Apr 2026 | Trial primary completion date: Nov 2025 --> Apr 2026
    Trial completion date • Trial primary completion date
    |
    TP53 mutation
    |
    Veppanu (vepdegestrant) • samuraciclib (CT7001)
    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: Aug 2025 --> Nov 2025
    Trial completion date
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    Ibrance (palbociclib) • Veppanu (vepdegestrant)