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Updated: Feb 19, 2026

Development and Maintenance of a Preclinical Patient Derived Tumor Xenograft Model for the Investigation of Novel Anti-Cancer Therapies
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KAT6 inhibitors under investigation for solid tumors: the preclinical and early phase progress

Toru Mukohara1

  • 1Department of Medical Oncology, National Cancer Center Hospital East, Kashiwa, Japan.

Expert Opinion on Investigational Drugs
|February 17, 2026
PubMed
Abstract

Insights

KAT6 inhibitors, like Prifetrastat, show promise for treating advanced breast cancer and other solid tumors. Further research will explore their clinical significance and potential for broader applications.

Area of Science:

  • Oncology
  • Molecular Biology
  • Epigenetics

Background:

  • KAT6A and KAT6B (KAT6) are MYST family histone acetyltransferases.
  • KAT6 regulates cellular processes via histone H3 acetylation.
  • KAT6A is overexpressed in solid tumors; KAT6 is crucial for ESR1 transcription in ER+ breast cancer.

Purpose of the Study:

  • To evaluate the clinical significance of KAT6 inhibitors, specifically Prifetrastat.
  • To explore the application of KAT6 inhibitors in diverse breast cancer subtypes and other solid tumors.
  • To develop strategies for managing side effects like dysgeusia and identify predictive biomarkers.

Main Methods:

  • Phase I trial of Prifetrastat in ER+ breast cancer patients.
  • Phase III trial of Prifetrastat in combination with Fulvestrant for advanced ER+ breast cancer.
  • Preclinical and clinical development of various KAT6 catalytic inhibitors and degraders.

Main Results:

  • Prifetrastat demonstrated promising efficacy and a favorable safety profile in Phase I trials, with dysgeusia as a notable side effect.
  • Ongoing Phase III trials are expected to provide key data on Prifetrastat's clinical impact.
  • Numerous KAT6 inhibitors are advancing through preclinical and clinical development.

Conclusions:

  • KAT6 inhibitors represent a promising therapeutic strategy for ER+ advanced breast cancer and potentially other solid tumors.
  • Future research should focus on expanding KAT6 inhibitor applications, managing side effects, and developing response biomarkers.
  • Investigating KAT6A-selective and KAT6/7 inhibitors may reveal differential efficacy and safety profiles, advancing KAT6-targeted therapy.
Keywords:
Breast cancerHER2-negativeKAT6PF07248144hormone receptor-positiveprifetrastat

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