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
  • 1. Department of Medicinal Chemistry, Lexicon Pharmaceuticals , 110 Allen Road, Basking Ridge, New Jersey 07920, United States.
PMID: 28045524 DOI: 10.1021/acs.jmedchem.6b01541
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.