Table 1.

Chemical and pharmacological characteristics of SGLT2 inhibitors available in Japan

Generic name	Ipragliflozin	Dapagliflozin	Luseogliflozin	Tofogliflozin	Canagliflozin	Empagliflozin
Structural formula
Initial marketing	2014 April	2014 May	2014 May	2014 May	2014 September	2015 Ferbruary
Dosage and administration	50 mg once daily (to 100 mg once daily)	5 mg once daily (to 10 mg once daily)	2.5 mg once daily (to 5 mg once daily)	20 mg once daily	100 mg once daily	10 mg once daily (to 25 mg once daily)
SGLT2/SGLT1	860	610	1,770	2,900	290	2,680–5,000
Half‐life (h)	11.71	12.1	11.2	5.4	10.6	9.88–11.7
Bioavailability	90.20%	78%	90%	97.50%	65%	NA
Protein binding	94.6–96.5%	91%	96.0–96.3%	82.3–82.6%	99%	86.20%
Metabolism	UGT2B7	UGT1A9	CYP3A4/5, 4A11, 4F2, 4F3B, UGT1A1	CYP3A4/5, 4A11, 4F3B	UGT1A9, 2B4, 3A4, CYP2D6	UGT2B7, 1A3, 1A9
Excretion	Urinary ex. 67.9% Fecal ex 32.7%	Urinary ex. 75.0% Fecal ex. 21.0%	Urinary ex. 44.2% Fecal ex. 50.0%	Urinary ex. 76.2% Fecal ex. 21.4%	Urinary ex. 32.5% Fecal ex. 60.4%	Urinary ex. 54.4% Fecal ex. 41.2%

CYP, cytochrome P450 superfamily; N/A, not available; UGT, UDP‐glucosyltransferase.