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

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