Table 4.
Pharmacokinetic parameters of E2 and E1 concentrations at week 6
| E2 | E1 | |||
|---|---|---|---|---|
| Relugolixa | Relugolix + E2/NETAb | Relugolix | Relugolix + E2/NETA | |
| Cmax (pg/mL) | ||||
| n | 21 | 22 | 25 | 22 |
| Mean (SD) | 28.5 (55.3) | 46.8 (17.3) | 25.3 (16.6) | 303 (137) |
| Median (range) | 7.22 (2.74, 255) | 49.2 (13.0, 78.9) | 23.1 (7.98, 93.6) | 270 (80.8, 621) |
| Cavg (pg/mL) | ||||
| n | 19 | 22 | 25 | 22 |
| Mean (SD) | 20.0 (38.2) | 32.6 (10.9) | 19.7 (14.1) | 186 (82.4) |
| Median (range) | 6.17 (2.89, 170) | 31.5 (7.73, 50.2) | 17.2 (6.95, 76.3) | 170 (36.7, 329) |
| Ctrough (pg/mL) | ||||
| n | 22 | 22 | 25 | 22 |
| Mean (SD) | 18.8 (53.2) | 20.8 (7.8) | 20.9 (16.7) | 96.4 (45.0) |
| Median (range) | 5.7 (1.3, 255) | 21.4 (3.6, 39.0) | 16.9 (7.04, 93.6) | 98.6 (20.1, 184) |
Cavg average concentration, Cmax maximum observed plasma concentration, Ctrough trough concentration, E1 estrone, E2 estradiol, NETA norethindrone acetate, SD standard deviation
aRelugolix 40 mg alone
bRelugolix 40 mg with E2 1 mg and NETA 0.5 mg