Table 2.
Summary plasma pharmacokinetic parameters of roflumilast and roflumilast N-oxide following daily topical administration of roflumilast cream 0.3% at Day 15 (Maximal Usage Pharmacokinetic and Safety Study; Study 107; NCT04279119)
| Analyte | Age group | N | BSA, % (SD) | Tmax, h (min–max) | Cmax, ng/mL (SD) | AUClast, h*ng/mL (SD) | AUClast normalized by dose, h*ng/mL/mg (SD) |
|---|---|---|---|---|---|---|---|
| Roflumilast | Adolescentsa | 5c | 13.6 (3.65) | 10.4 (1.0–24) | 1.27 (1.23) | 25.1 (24.0) | 2.07 (2.17) |
| Adultb | 18 | 26.8 (6.80) | 11.3 (0–24) | 3.72 (2.49) | 72.7 (53.1) | 2.74 (2.12) | |
| N-oxide | Adolescentsa | 6 | 13.0 (3.58) | 16.5 (1.0–24.0) | 7.17 (9.39) | 140 (179) | 11.8 (15.9) |
| Adultb | 18 | 26.8 (6.80) | 12.9 (0–24) | 30.6 (29.4) | 628 (648) | 23.2 (24.8) |
Data are expressed as means unless indicated otherwise
AUClast area under the curve until the last quantifiable timepoint, BSA body surface area, Cmax maximum plasma concentration, SD standard deviation, min minimum, max maximum, Tmax time to reach Cmax
a12–17 years of age
b≥18 years of age
cOne adolescent had less than 3 quantifiable roflumilast concentrations for Day 15 and was excluded from the PK analysis