Comparative Pharmacology
Head-to-head clinical analysis: INVOKAMET XR versus JARDIANCE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: INVOKAMET XR versus JARDIANCE.
INVOKAMET XR vs JARDIANCE
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 co-transporter 2 (SGLT2) inhibitor; reduces renal glucose reabsorption, lowering blood glucose independent of insulin.
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.
10 mg orally once daily, may increase to 25 mg orally once daily if tolerated and additional glycemic control needed.
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 approximately 12.9 hours in healthy subjects. Steady-state is achieved after 4-5 days of once-daily dosing. Effective half-life for accumulation: ~4-6 hours.
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 renal: approximately 70-80% of absorbed dose excreted unchanged in urine via glomerular filtration and active tubular secretion. Fecal: ~10-20% via biliary and fecal elimination.
Category C
Category C
SGLT2 Inhibitor / Biguanide Combination
SGLT2 Inhibitor