1. Academic Validation
  2. Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restricted to the Intestinal Lumen, for the Treatment of Diabetes

Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restricted to the Intestinal Lumen, for the Treatment of Diabetes

  • J Med Chem. 2017 Jan 26;60(2):710-721. doi: 10.1021/acs.jmedchem.6b01541.
Nicole C Goodwin 1 Zhi-Ming Ding Bryce A Harrison 1 Eric D Strobel 1 Angela L Harris Melinda Smith Andrea Y Thompson Wendy Xiong Faika Mseeh Debra J Bruce Damaris Diaz Suma Gopinathan Ling Li Emily O'Neill Mary Thiel Alan G E Wilson Kenneth G Carson 1 David R Powell David B Rawlins 1
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Lexicon Pharmaceuticals , 110 Allen Road, Basking Ridge, New Jersey 07920, United States.
Abstract

The increasing number of people afflicted with diabetes throughout the world is a major health issue. Inhibitors of the sodium-dependent glucose cotransporters (SGLT) have appeared as viable therapeutics to control blood glucose levels in diabetic patents. Herein we report the discovery of LX2761, a locally acting SGLT1 Inhibitor that is highly potent in vitro and delays intestinal glucose absorption in vivo to improve glycemic control.

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