Drug intelligence / Profile preview

PF-07248144 + PF-07220060 + fulvestrant

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

PF-07248144 + PF-07220060 + fulvestrant is a triple combination investigational regimen being studied in advanced or metastatic solid tumors, most notably in hormone receptor (HR)-positive, HER2-negative breast cancer. PF-07248144 is a small molecule inhibitor targeting epigenetic regulation, specifically the KAT6A/B histone acetyltransferases. PF-07220060 is an oral CDK4/6 inhibitor, designed to block cell cycle progression in cancer cells by inhibiting cyclin-dependent kinase 4/6 activity. Fulvestrant is a selective estrogen receptor degrader (SERD) that binds, blocks, and degrades the estrogen receptor, thereby antagonizing estradiol-driven tumor growth. This combination is being developed by Pfizer for dose escalation and expansion cohorts in post-CDK4/6 inhibitor settings[1][3][7].

Other names
fulvestrant
02

Targets

ER (Estrogen receptor)KAT6A (Lysine acetyltransferase 6A)CDK4 (Cyclin-dependent kinase 4)KAT6B (Histone acetyltransferase KAT6B)

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