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 language | English (US) |
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Pages (from-to) | 1349-1352 |
Number of pages | 4 |
Journal | Expert Opinion on Therapeutic Patents |
Volume | 25 |
Issue number | 11 |
DOIs | |
State | Published - 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