KC1086 + fulvestrant

KC1086 + fulvestrant is an investigational combination regimen consisting of KC1086, an orally bioavailable, highly selective dual lysine acetyltransferase 6/7 (KAT6/KAT7) inhibitor, and fulvestrant, an approved selective estrogen receptor degrader (SERD). Developed by Beijing Konruns Pharmaceutical, KC1086 targets the MYST-family acetyltransferases KAT6A, KAT6B, and KAT7 to suppress promoter-proximal histone H3 acetylation (such as H3K23ac and H3K14ac), thereby inhibiting lineage transcription in estrogen receptor-positive (ER+) breast cancer. Fulvestrant acts by binding to, antagonizing, and degrading estrogen receptor alpha (ERα). Preclinical studies have demonstrated that the combination of KC1086 and fulvestrant yields robust tumor regressions and survival benefits in ER+ breast cancer models. The combination is in Phase II clinical development for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) locally advanced or metastatic breast cancer.

Other names

KC-1086 + FaslodexKC-1086 + fulvestrantKC-1086 and fulvestrantKC1086 and fulvestrantKC 1086 and fulvestrantKC1086 + Faslodex