Comparative Pharmacology
Head-to-head clinical analysis: INVOKANA versus SEGLUROMET.
Head-to-head clinical analysis: INVOKANA versus SEGLUROMET.
INVOKANA vs SEGLUROMET
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Sodium-glucose cotransporter 2 (SGLT2) inhibitor; reduces renal glucose reabsorption, increasing urinary glucose excretion.
SEGLUROMET is a fixed-dose combination of ertugliflozin and metformin. Ertugliflozin is a sodium-glucose co-transporter 2 (SGLT2) inhibitor that reduces renal glucose reabsorption, increasing urinary glucose excretion. Metformin decreases hepatic glucose production, decreases intestinal glucose absorption, and improves insulin sensitivity.
100 mg orally once daily, before the first meal of the day; may increase to 300 mg once daily if tolerated and eGFR is adequate.
Initial: 2.5 mg ertugliflozin/1000 mg metformin twice daily. Titrate based on efficacy and tolerability. Maximum: 5 mg ertugliflozin/2000 mg metformin twice daily.
None Documented
None Documented
Terminal elimination half-life is 10.6 hours (range 9.5–12.5 h) in healthy subjects; allows once-daily dosing. Half-life increases to 16 hours in moderate renal impairment and 22 hours in severe renal impairment.
Ertugliflozin: terminal half-life ~16.6 hours (range 10-20 h), supporting once daily dosing. Metformin: terminal half-life ~6.2 hours (range 4-8.7 h) in patients with normal renal function; prolonged in renal impairment.
Primarily excreted unchanged in urine (33%) and feces (52%) as parent drug and glucuronide metabolites; renal clearance accounts for 70% of total clearance, with 51% renally excreted as unchanged drug.
Segluromet (ertugliflozin and metformin) is primarily excreted via renal (ertugliflozin: ~40.9% unchanged in urine; metformin: ~90% unchanged in urine) and fecal/biliary routes (ertugliflozin: ~50.2% in feces as parent and metabolites; metformin: <1% in bile).
Category C
Category C
SGLT2 Inhibitor
SGLT2 Inhibitor/Biguanide Combination