C5F2-HCB

C5F2-HCB is a fluorinated cuban-1-yl biguanide derivative designed to overcome hormone therapy resistance in ER+HER2- breast cancer. It functions by inhibiting Cytochrome P450 3A4 (CYP3A4)-mediated biosynthesis of epoxyeicosatrienoic acids (EETs), which are epoxy fatty acids that promote oxidative phosphorylation and contribute to resistance against standard-of-care treatments like fulvestrant and palbociclib. Developed by researchers at the University of Minnesota and Mayo Clinic, C5F2-HCB has demonstrated improved pharmacokinetics and reduced toxicity compared to its parent compound, hexyl cuban-1-yl biguanide (HCB). In preclinical models, it has shown synergy when combined with palbociclib and fulvestrant, leading to the reversal of hypoxia and inhibition of tumor growth in multiply resistant breast cancer xenografts.

Other names

fluorinated cuban-1-yl biguanidefluorinated hexyl cuban-1-yl biguanide