Drug intelligence / Profile preview

Re(CO)3-phenformin

Development stage
Preclinical
Lead developer
University of Texas MD Anderson Cancer Center
Modality
Small Molecules
Administration
Intravenous
01

Overview

Re(CO)3-phenformin (also known as Re-phen) is a rhenium-tricarbonyl biguanide complex being developed as a therapeutic agent for pancreatic ductal adenocarcinoma (PDAC). It serves as the nonradioactive, structurally matched therapeutic counterpart to the diagnostic imaging agent [99mTc(CO)3]-phenformin, together forming a theranostic pair. Re(CO)3-phenformin functions by targeting the mitochondria and potently reducing mitochondrial membrane potential, a mechanism that distinguishes it from its parent compound, phenformin. Preclinical studies in murine PDAC models have demonstrated that Re(CO)3-phenformin achieves significantly higher tissue deposition and superior antitumor efficacy compared to phenformin, with measurable in vivo conversion to the parent drug. The compound is currently under investigation by researchers at the University of Texas MD Anderson Cancer Center and the University of Houston.

Other names
rhenium tricarbonyl phenformin
02

Targets

ND1 (Mitochondrial electron transport chain complex I)

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