Inhibition of lysine acetyltransferase KAT6 in ER⁺HER2^- metastatic breast cancer: a phase 1 trial.

ABSTRACT: Inhibition of histone lysine acetyltransferases (KATs) KAT6A and KAT6B has shown antitumor activity in estrogen receptor-positive (ER⁺) breast cancer preclinical models. PF-07248144 is a selective catalytic inhibitor of KAT6A and KAT6B. In the present study, we report the safety, pharmacokinetics (PK), pharmacodynamics, efficacy and biomarker results from the first-in-human, phase 1 dose escalation and dose expansion study (n = 107) of PF-07248144 monotherapy and fulvestrant combination in heavily pretreated ER⁺ human epidermal growth factor receptor-negative (HER2^-) metastatic breast cancer (mBC). The primary objectives of assessing the safety and tolerability and determining the recommended dose for expansion of PF-07248144, as monotherapy and in combinat

SUBMITTER: Mukohara T 

PROVIDER: S-EPMC11333285 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature