Drug intelligence / Profile preview

PF-07248144 + letrozole + palbociclib

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

Overview

PF-07248144 + letrozole + palbociclib is an investigational **triple-drug combination** evaluated for the treatment of advanced or metastatic hormone receptor–positive, HER2-negative breast cancer. - **PF-07248144** is a novel, selective catalytic inhibitor of **KAT6A/B** (lysine acetyltransferase 6A and 6B), a histone acetyltransferase that regulates lineage-specific gene transcription through H3K23 acetylation. Targeting KAT6 represents a new epigenetic approach in oncology. - **Letrozole** is a nonsteroidal aromatase inhibitor that suppresses estrogen production by inhibiting the aromatase enzyme, reducing tumor growth in estrogen receptor–positive breast cancers. - **Palbociclib** is a small molecule CDK4/6 inhibitor that blocks cyclin-dependent kinases 4 and 6, arresting cancer cells in the G1 phase and preventing proliferation.

02

Targets

KAT6A (Lysine acetyltransferase 6A)ER (Estrogen receptor)CYP19A1 (Aromatase)CDK6 (Cyclin-dependent kinase 6)KAT6B (Histone acetyltransferase KAT6B)CDK4 (Cyclin-dependent kinase 4)

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