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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.
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.
Small molecules bind the acetyl-CoA site of KAT6A/B, blocking histone H3 acetylation at oestrogen receptor target genes and triggering senescence.
Query for this technology: (TITLE:"KAT6 inhibitors" OR ABSTRACT:"KAT6 inhibitors") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about KAT6 inhibitors, not a curated reading list.
Shares Endocrine therapy (SERMs, AIs, SERDs), HR-positive / HER2-negative breast cancer.
Shares Endocrine therapy (SERMs, AIs, SERDs), HR-positive / HER2-negative breast cancer.
Shares Endocrine therapy (SERMs, AIs, SERDs), HR-positive / HER2-negative breast cancer.
Shares Endocrine therapy (SERMs, AIs, SERDs), HR-positive / HER2-negative breast cancer.
Shares Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET), HR-positive / HER2-negative breast cancer.
Shares Endocrine therapy (SERMs, AIs, SERDs), HR-positive / HER2-negative breast cancer.
Shares Endocrine therapy (SERMs, AIs, SERDs), HR-positive / HER2-negative breast cancer.
Shares Endocrine therapy (SERMs, AIs, SERDs), HR-positive / HER2-negative breast cancer.