Ertugliflozin

DB11827ApprovedInvestigationalSmall moleculeSodium-glucose Cotransporter 2 (SGLT2) Inhibitors

Ertugliflozin is an SGLT2 inhibitor used to treat type 2 diabetes mellitus alone or in combination with other antidiabetic drugs. It works to block glucose reabsorption from the glomerulus.

Mechanism: Kidneys play an integral role in glucose homeostasis. After being filtered into urine within the nephron, most of the plasma glucose is reabsorbed through two types of sodium-dependent glucose cotransporters (SGLTs), SGLT1 and SGLT2, expressed in proximal renal tubules. More specifically, SGLT2 is responsible for 80–90% of renal glucose reabsorption while SGLT1 is responsible for the remaining 10-20%. Under physiological conditions, less than one percent of glucose is excreted in urine. In the case of hyperglycemia, SGLTs become saturated and the renal threshold for urinary glucose excretion is increased. Kidneys respond to an elevated threshold for glycosuria by elevating glucose reabsorption and increasing maximum glucose reabsorptive capacity.
Ertugliflozin is an inhibitor of SGLT2 that reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, thereby increasing urinary glucose excretion.
Curator reviewed · 6 references
Primary indication: Ertugliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adult patients with type 2 diabetes mellitus (T2DM).Curator reviewed · 4 structured indications
Formula / weight: C₂₂H₂₅ClO₇ · 436.89 g/mol (avg)
First approval: Canada, 2018 · United States, 2017 · European Union, 2020
Also known as: (1S,2S,3S,4R,5S)-5-(4-Chloro-3-(4-ethoxybenzyl)phenyl)-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol · 1,6-Anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-5-C-(hydroxymethyl)-β-L-idopyranose · β-L-Idopyranose, 1,6-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-5-C-(hydroxymethyl)-
Code names: MK-8835 · PF-04971729 · PF-04971729-00
Brand names: Segluromet
Steglatro
Steglujan