Table 3.
Pharmacokinetic parameters of a single oral dose of dersimelagon in healthy adult volunteers
| PK variable | Statistical parameter | Single ascending dose (Part A) |
Effect of sex (Part D) |
Effect of age (Part H) |
Effect of race (Part F) |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
1 mg (N = 6/n = 6) |
3 mg (N = 6/n = 6) |
10 mg (N = /n = 66) |
30 mg (N = 6/n = 6) |
100 mg (N = 6/n = 6) |
300 mg (N = 6/n = 6) |
600 mg (N = 6/n = 6) |
Malea 100 mg (N = 6/n = 6) |
Female 100 mg (N = 6/n = 6) |
≤ 55 yearsa 100 mg (N = 6/n = 6) |
≥ 65 years 100 mg (N = 6/n = 6) |
Whitea 100 mg (N = 6/n = 6) |
Black 100 mg (N = 6/n = 6) |
||
|
AUC0-∞ (ng∙h/mL) |
Mean (SD) | 15.5 (6.82) | 52.7 (11.2) | 313.1 (78.1) | 664.6 (182.3) | 2588.2 (1323.9) | 11,553.6 (3234.4) | 18,836.1 (5814.5) | 2588.2 (1323.9) | 4214.8 (1588.1) | 2588.2 (1323.9) | 3122.2 (1113.5) | 2588.2 (1323.9) | 2633.6 (1293.0) |
| Cmax (ng/mL) | Mean (SD) | 2.50 (0.83) | 8.76 (1.86) | 38.1 (7.56) | 86.5 (23.6) | 339.6 (230.8) | 1183.4 (316.0) | 2103.8 (401.2) | 339.6 (230.8) | 448.7 (220.5) | 339.6 (230.8) | 407.1 (114.1) | 339.6 (230.8) | 316.7 (153.9) |
| Tmax (h) |
Median (range) |
2.50 (1.98, 3.03) |
2.00 (1.00, 2.00) |
2.00 (1.98, 4.00) |
2.00 (1.98, 5.00) |
3.00 (1.00, 6.02) |
1.99 (0.98, 4.98) |
5.00 (0.98, 5.00) |
3.00 (1.00, 6.02) |
5.00 (1.00, 6.00) |
3.00 (1.00, 6.02) |
2.60 (0.98, 4.98) |
3.00 (1.00, 6.02) |
3.99 (1.97, 5.00) |
| t1/2 (h) | Mean (SD) | 5.14 (3.43) | 6.43 (2.17) | 8.27 (2.69) | 7.63 (1.49) | 9.77 (2.26) | 9.49 (1.72) | 10.6 (3.95) | 9.77 (2.26) | 12.1 (5.60) | 9.77 (2.26) | 12.1 (2.80) | 9.77 (2.26) | 9.25 (3.97) |
AUC0-∞ area under the plasma concentration versus time curve from time zero to infinity, Cmax maximum observed plasma concentration, N number of participants, n number of observations, t1/2 terminal elimination half-life, Tmax time to maximum plasma concentration
aComparator group is composed of participants from Part A