Drug intelligence / Profile preview

C6F3-HCB

Development stage
Preclinical
Lead developer
University of Minnesota
Modality
Small Molecules
01

Overview

C6F3-HCB (C6F3-hexyl-(cuban-1-yl-methyl)-biguanide) is a fluorinated hexyl cuban-1-yl biguanide derivative designed to overcome hormone therapy resistance (HTR) and CDK4/6 inhibitor resistance in ER+/HER2- breast cancer. It acts as an inhibitor of Cytochrome P450 3A4 (CYP3A4) arachidonic acid epoxygenase activity, thereby suppressing the biosynthesis of epoxyeicosatrienoic acids (EETs), including (±)8,9-EET, (±)11,12-EET, and (±)14,15-EET. By inhibiting EET biosynthesis, C6F3-HCB suppresses EET-driven mitochondrial oxidative phosphorylation (OXPHOS) and reverses tumor hypoxia. It was developed by researchers at the University of Minnesota and Mayo Clinic.

Other names
C6F3-hexyl cuban-1-yl biguanideC-6F3-hexyl cuban-1-yl biguanideC 6F3-hexyl cuban-1-yl biguanideC6F3-hexyl-(cuban-1-yl-methyl)-biguanide
02

Targets

CYP3A4 (Cytochrome P450 3A4)

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