# KAT6 inhibitors

Source: https://onco.cc/technologies/kat6-inhibitors/  
OnCo record `kat6-inhibitors` (Technology). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

First-in-class drugs against the histone acetyltransferases KAT6A and KAT6B, in late trials for hormone receptor-positive breast cancer that has stopped responding to endocrine therapy.

## Summary

KAT6A is amplified in a subset of breast cancers and cooperates with the oestrogen receptor to drive gene expression. Inhibitors of KAT6A and KAT6B (PF-07248144, now in phase 3 with fulvestrant, and others) induce senescence in oestrogen receptor-positive breast cancer cells and produced durable responses in heavily pretreated patients in early trials, with dysgeusia and neutropenia as the main side effects. The class is also being explored in prostate cancer and lymphoma.

## Fields

- Kind: Technology
- Status: phase-3
- Last checked: 2026-09-04
- Principle: Small molecules bind the acetyl-CoA site of KAT6A/B, blocking histone H3 acetylation at oestrogen receptor target genes and triggering senescence.
- Strengths: New mechanism in endocrine-resistant breast cancer; Oral; Combines with fulvestrant and CDK4/6 inhibitors
- Limitations: Dysgeusia and neutropenia; No approval yet

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/KAT6A
- Wikipedia: https://en.wikipedia.org/wiki/KAT6A

## Connected records

- cancers: [HR-positive / HER2-negative breast cancer](https://onco.cc/cancers/breast-hr-positive/)
- fronts: [Epigenetic & Transcriptional Therapy](https://onco.cc/fronts/epigenetics/), [Targeted Therapy](https://onco.cc/fronts/targeted-therapy/)
- technologies: [Endocrine therapy (SERMs, AIs, SERDs)](https://onco.cc/technologies/endocrine-therapy/), [Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET)](https://onco.cc/technologies/epigenetic-drugs/)

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