Ertugliflozin, sold under the brand name Steglatro, is a medication used for the treatment of type 2 diabetes. The most common side effects include fungal infections of the vagina and other infections of the female reproductive system. Ertugliflozin is an orally administered selective sodium glucose cotransporter 2 inhibitor that lowers renal glucose reabsorption to increase urinary glucose excretion and reduce plasma glucose. Marketed tablet strengths are typically 5 mg and 15 mg. The compound is cleared primarily by glucuronidation via UGT1A9 and UGT2B7 with minor cytochrome P450 involvement. Pharmacologically it shows high selectivity for SGLT2 over SGLT1, a plasma half-life compatible with once daily dosing, and predictable dose proportional systemic exposure that supports monotherapy or combination use with metformin, insulin, or other antihyperglycemic agents.
Parent: Ertugliflozin
Parent: Ertugliflozin
Parent: Ertugliflozin
Parent: Ertugliflozin
Typical quality specifications for ertugliflozin active pharmaceutical ingredient used for formulation set the assay at not less than 98.5 percent by HPLC and control related substances according to ICH Q3A/Q3B principles. Typical limits used in regulatory dossiers and commercial specifications are individual known related compounds not more than 0.20 percent w w, individual unidentified impurities not more than 0.10 percent w w, and total impurities not more than 0.50 percent w w. Residual solvents are controlled to ICH Q3C class limits for the solvents used in the process, with methanol for example limited to 3000 ppm when applicable. Water content is usually controlled by Karl Fischer to low single digit percent or lower depending on formulation requirements and heavy metals are limited to pharmacopeial thresholds such as 20 ppm or lower. Process-related intermediates and positional isomers are identified, qualified or limited per stability and toxicological risk assessment and appropriate analytical methods are included in the release and stability testing program.
Ertugliflozin is used to improve glycemic control in adults with type 2 diabetes as monotherapy or in combination with other antihyperglycemic agents; it reduces blood glucose by increasing urinary glucose excretion through inhibition of renal SGLT2.
Ertugliflozin selectively inhibits the sodium glucose cotransporter 2 in the proximal renal tubule, decreasing renal reabsorption of filtered glucose and increasing urinary glucose excretion which lowers plasma glucose levels.
No, ertugliflozin and metformin are different drugs with distinct mechanisms; metformin primarily reduces hepatic glucose production and improves insulin sensitivity while ertugliflozin increases urinary glucose excretion by inhibiting SGLT2.
