ME3BP-7 is a targeted cytotoxic agent that rapidly kills pancreatic cancer cells expressing high levels of monocarboxylate transporter MCT1

• DOI: 10.7554/elife.94488.3
• Publication Date: 2025-05-20T10:35:38Z
• Authors: Jordina Rincon-To...; Marco Dal Molin; Brian Mog; Gyuri Han; Evangeline Watson; Nicolas Wyhs; Shun Ishiyama; Taha Ahmedna; Il Minn; Nilofer Azad; Chetan Bettegowda; Nickolas Papadopo...; Kenneth W Kinzler; Shibin Zhou; Bert Vogelstein; Kathleen Gabrielson; Surojit Sur

Nearly 30% of pancreatic ductal adenocarcinomas (PDACs) exhibit a marked overexpression monocarboxylate transporter 1 (MCT1) offering unique opportunity for therapy. However, biochemical inhibitors MCT1 have proven unsuccessful in clinical trials. In this study, we present an alternative approach using 3-bromopyruvate (3BP) to target overexpressing PDACs. 3BP is cytotoxic agent that known be transported into cells via MCT1, but its usefulness has been hampered by difficulties delivering the drug systemically. We describe here novel microencapsulated formulation (ME3BP-7), which effective against variety PDAC vitro and remains stable serum. Furthermore, systemically administered ME3BP-7 significantly reduces cancer growth metastatic spread multiple orthotopic models with manageable toxicity. is, therefore, prototype promising new drug, targeting moiety are both contained within same single small molecule.