Delving into the Latest Updates on ME3BP-7 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

MCT1

Action

inhibitors

Mechanism

MCT1 inhibitors(Monocarboxylate transporter 1 inhibitors)

Therapeutic Areas

NeoplasmsDigestive System DisordersEndocrinology and Metabolic Disease

Active Indication

Pancreatic Ductal Adenocarcinoma

Inactive Indication-

Originator Organization

The Johns Hopkins University School of Medicine

Active Organization

The Johns Hopkins University School of Medicine

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Author: Azad, Nilofer S. ; Molin, Marco Dal ; Azad, Nilofer S ; Rincon-Torroella, Jordina ; Minn, Il ; Ishiyama, Shun ; Han, Gyuri ; Papadopoulos, Nickolas ; Dal Molin, Marco ; Vogelstein, Bert ; Wyhs, Nicolas ; Zhou, Shibin ; Gabrielson, Kathleen ; Mog, Brian ; Kinzler, Kenneth W. ; Watson, Evangeline ; Bettegowda, Chetan ; Ahmedna, Taha ; Sur, Surojit ; Kinzler, Kenneth W

AbstractNearly 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.One Sentence SummaryME3BP-7 is a novel formulation of 3BP that resists serum degradation and rapidly kills pancreatic cancer cells expressing high levels of MCT1 with tolerable toxicity in mice.

100 Deals associated with ME3BP-7

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