An evaluation of US patent 2015065565 (A1) for a new class of SGLT2 inhibitors for treatment 1 of type II diabetes mellitus

Meiyan Jiang, Peter S. Steyger

Research output: Contribution to journalReview article

5 Scopus citations

Abstract

Introduction: Type 2 diabetes mellitus (T2DM) is a growing and serious global health problem. Pharmacological inhibition of the sodium-glucose cotransporter-2 (SGLT2; SLC5A2) increases urinary glucose excretion, decreasing plasma glucose levels in an insulin-independent manner. Agents that inhibit SGLT2 have recently become available for clinical therapy of T2DM. Areas covered: The patent claims a new class of SGLT2 inhibitors: derivatives of dioxa-bicyclo[3.2.1]octane-2,3,4-triol (including ertugliflozin; PF-04971729). The invention describes the design, synthesis and pharmacological tests related to ertugliflozin, which could ultimately lead to efficacious therapy for T2DM alone or in combination with other anti-diabetic agents. Expert opinion: Ertugliflozin is likely to be of great clinical significance in the near future. Continued analysis of ertugliflozin derivatives to now validate safe and efficacious treatment of T2DM in a larger number of clinical subjects over an extended period is needed to further support clinical utility. Identification, and discussion, of likely contra-indications is also needed.

Original languageEnglish (US)
Pages (from-to)1349-1352
Number of pages4
JournalExpert Opinion on Therapeutic Patents
Volume25
Issue number11
DOIs
StatePublished - Aug 8 2015

Keywords

  • PF-04971729
  • clinical therapy
  • diabetes
  • dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives
  • ertugliflozin
  • inhibitors
  • sodium-glucose linked co-transporter
  • type 2 diabetes mellitus

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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