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    DRUG:

    prifetrastat (PF-07248144)

    i
    Other names: PF-07248144, PF 07248144, PF07248144
    Company:
    Pfizer
    Drug class:
    KAT6 inhibitor
    Related drugs:
    26d
    A Study to Learn About the Study Medicine Called PF-07248144 in Combination With Fulvestrant in People With HR-positive, HER2-negative Advanced or Metastatic Breast Cancer Who Progressed After a Prior Line of Treatment. (clinicaltrials.gov)
    P3, N=400, Recruiting, Pfizer
    Trial initiation date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • BRCA (Breast cancer early onset)
    |
    HER-2 positive • HR positive • HER-2 negative • HR positive + HER-2 negative
    |
    everolimus • fulvestrant • exemestane • prifetrastat (PF-07248144)
    1m
    A Study to Learn About the Study Medicine Called PF-07248144 in Combination With Fulvestrant in People With HR-positive, HER2-negative Advanced or Metastatic Breast Cancer Who Progressed After a Prior Line of Treatment. (clinicaltrials.gov)
    P3, N=400, Recruiting, Pfizer
    Trial initiation date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • BRCA (Breast cancer early onset)
    |
    HER-2 positive • HR positive • HER-2 negative • HR positive + HER-2 negative
    |
    everolimus • fulvestrant • exemestane • prifetrastat (PF-07248144)
    1m
    A Study to Learn if Multiple Doses of the Study Medicine Called Carbamazepine Changes How the Body Processes the Other Study Medicine PF-07248144 (clinicaltrials.gov)
    P1, N=12, Completed, Pfizer | Recruiting --> Completed
    Trial completion
    |
    prifetrastat (PF-07248144)
    1m
    C4551001: Study of PF-07248144 in Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
    P2, N=320, Recruiting, Pfizer | Phase classification: P1 --> P2 | Trial primary completion date: Feb 2028 --> Jul 2029
    Phase classification • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A)
    |
    ER positive • HER-2 negative • HER-2 negative + ER positive
    |
    Ibrance (palbociclib) • fulvestrant • letrozole • Veppanu (vepdegestrant) • atirmociclib (PF-07220060) • prifetrastat (PF-07248144)
    2ms
    A Study to Learn if Itraconazole Changes How the Body Processes PF-07248144 (Study Medicine) (clinicaltrials.gov)
    P1, N=12, Active, not recruiting, Pfizer | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    itraconazole • prifetrastat (PF-07248144)
    3ms
    A Study to Understand What the Body Does to the Study Medicine Called PF-07248144 When Taken by Healthy Adults (clinicaltrials.gov)
    P1, N=8, Completed, Pfizer
    New P1 trial
    |
    prifetrastat (PF-07248144)
    3ms
    C4551007: A Study to Learn if Multiple Doses of the Study Medicine Called Carbamazepine Changes How the Body Processes the Other Study Medicine PF-07248144 (2025-522331-34-00)
    P1, N=12, Completed, Pfizer Inc.
    New P1 trial
    |
    prifetrastat (PF-07248144)
    3ms
    C4551002: A Study to Learn About the Study Medicine Called PF-07248144 in Combination with Fulvestrant in People with HR-positive, HER2-negative Advanced or Metastatic Breast Cancer who Progressed After a Prior Line of Treatment. (2025-520566-22-00)
    P2/3, N=153, Recruiting, Pfizer Inc.
    New P2/3 trial
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • BRCA (Breast cancer early onset)
    |
    HER-2 positive • HR positive • HER-2 negative • HR positive + HER-2 negative
    |
    everolimus • fulvestrant • exemestane • prifetrastat (PF-07248144)
    3ms
    KAT6 inhibitors under investigation for solid tumors: the preclinical and early phase progress. (PubMed, Expert Opin Investig Drugs)
    Prifetrastat in combination with Fulvestrant is now being evaluated in a phase III trial for pretreated ER+ advanced breast cancer. Additionally, mitigation strategies for dysgeusia and clinically available response-predictive biomarkers should be developed. KAT6 inhibitors with different target spectra, including KAT6A-selective and KAT6/7 inhibitors, may exhibit differential efficacy and safety profiles, offering deeper insights into KAT6-targeted therapy.
    Preclinical • Journal
    |
    ER (Estrogen receptor) • KAT6A (Lysine Acetyltransferase 6A) • KAT6B (Lysine Acetyltransferase 6B)
    |
    ER positive
    |
    fulvestrant • prifetrastat (PF-07248144)
    3ms
    Dancing with KAT6A: Current advances and therapeutic potential in oncology of KAT6A inhibitors. (PubMed, Bioorg Chem)
    PF-07248144 has shown antitumor activity in estrogen receptor-positive (ER+) breast cancer models and is currently undergoing clinical evaluation...This review provides a comprehensive overview of the structural and biological functions of KAT6A, its role in tumor progression, and the therapeutic potential of its inhibition. It summarizes the advancements in KAT6A inhibitor development from 2019 to the present, emphasizing the optimization processes from lead compounds to clinical candidates.
    Review • Journal
    |
    ER (Estrogen receptor) • KAT6A (Lysine Acetyltransferase 6A)
    |
    ER positive
    |
    prifetrastat (PF-07248144)
    4ms
    A Study to Learn if Itraconazole Changes How the Body Processes PF-07248144 (Study Medicine) (clinicaltrials.gov)
    P1, N=12, Recruiting, Pfizer | Not yet recruiting --> Recruiting
    Enrollment open
    |
    itraconazole • prifetrastat (PF-07248144)
    4ms
    EPIBREAST: Clinical Trial Evaluating the Biological Activity of a New Drug Identified as Prifetrastat (PF-07248144), Combined With Fulvestrant for the Treatment of Patients With Hormone Receptor Positive (HR+) and HER2 Negative (HER2-) Breast Cancer Extended to Other Organs. (clinicaltrials.gov)
    P2, N=51, Not yet recruiting, UNICANCER
    New P2 trial • Tumor mutational burden
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    ER positive • HER-2 negative • HER-2 mutation • HER-2 negative + ER positive
    |
    fulvestrant • triptorelin • prifetrastat (PF-07248144)