Table 2.
Descriptive Summarya of Ertugliflozin Pharmacokinetic Parameter Values by Renal Function Group
| T2DM Subjects | |||||
|---|---|---|---|---|---|
| Normal Renal Function | Mild Renal Impairment | Moderate Renal Impairment | Severe Renal Impairment | Healthy Subjects With Normal Renal Function | |
| n | 6 | 8 | 8 | 6 | 8 |
| AUC (ng·h/mL) | 1199 (42) | 1908 (28) | 2075 (19) | 1895 (23) | 1236 (27) |
| CL/F (mL/min) | 209 (42) | 131 (28) | 120 (19) | 132 (23) | 202 (27) |
| Cmax (ng/mL) | 216 (35) | 313 (30) | 306 (23) | 196 (28) | 219 (26) |
| tmax (h) | 1.00 (1.00‐1.50) | 1.50 (1.00‐2.00) | 1.50 (0.50‐2.00) | 1.51 (0.50‐3.02) | 1.00 (1.00‐2.00) |
| t½ (h) | 14.6 ± 6.4 | 25.9 ± 14.0 | 22.9 ± 7.4 | 24.2 ± 6.0 | 17.7± 3.5 |
| Vz/F (L) | 240 (53) | 255 (50) | 228 (27) | 269 (41) | 305 (39) |
| fu | 0.0344 (3) | 0.0346 (8) | 0.0380 (6) | 0.0411 (9) | 0.0348 (4) |
| Ae96 (%) | 0.995 (55) | 0.720 (54) | 0.646 (21) | 0.389 (40) | 0.821 (48) |
| CLR (mL/min) | 2.09 (28) | 0.99 (45) | 0.80 (34) | 0.54 (23) | 1.68 (33) |
Normal renal function, eGFR ≥90 mL/min; mild renal impairment, eGFR 60‐89 mL/min; moderate renal impairment, eGFR 30‐59 mL/min; severe renal impairment eGFR <30 mL/min. %CV, percentage coefficient of variation; Ae96, percentage of dose recovered unchanged in urine from 0 to 96 hours postdose; AUC, area under the plasma concentration‐time profile from time 0 extrapolated to infinite time; CLR, renal clearance; CL/F, apparent clearance; Cmax, maximum observed concentration; fu, fraction unbound; h, hour; n, number of subjects; SD, standard deviation; tmax, time for Cmax, t½, terminal half‐life; Vz/F, apparent volume of distribution following oral administration.
aGeometric mean (geometric %CV) for all except median (range) for tmax; arithmetic mean (±SD) for t½; and arithmetic mean (%CV) for fu.