Comparative Pharmacology
Head-to-head clinical analysis: INVOKAMET XR versus INVOKANA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: INVOKAMET XR versus INVOKANA.
INVOKAMET XR vs INVOKANA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Combination of canagliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor, which reduces renal glucose reabsorption and lowers blood glucose, and metformin, an activator of AMP-activated protein kinase (AMPK) that decreases hepatic glucose production and improves insulin sensitivity.
Sodium-glucose cotransporter 2 (SGLT2) inhibitor; reduces renal glucose reabsorption, increasing urinary glucose excretion.
Maximum daily dose: canagliflozin 300 mg/metformin ER 2000 mg orally once daily with the morning meal. Initial dose: canagliflozin 50 mg/metformin ER 500 mg orally twice daily or canagliflozin 150 mg/metformin ER 1000 mg orally once daily; for patients not currently on metformin, start with canagliflozin 50 mg/metformin ER 500 mg orally twice daily; for patients on metformin, switch to INVOKAMET XR based on current metformin dose.
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.
None Documented
None Documented
Canagliflozin: mean terminal elimination half-life is 13.1 hours (range 11-16 hours) for the 300 mg dose, consistent with once-daily dosing. Metformin: terminal elimination half-life is approximately 6.2 hours (range 4-9 hours) in patients with normal renal function; prolonged in renal impairment.
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.
Canagliflozin is primarily excreted as unchanged drug in urine (approximately 33%) and feces (approximately 41%), with about 7% as metabolites in urine and 34% as metabolites in feces. Metformin is excreted unchanged in urine (90-100% of absorbed dose) via tubular secretion and glomerular filtration.
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.
Category C
Category C
SGLT2 Inhibitor / Biguanide Combination
SGLT2 Inhibitor