Table 5.
Serum PK parameters of BITS7201A for Part B: SC cohorts, after dosing on Day 1 and Day 57
| Parameter | Statistic | Cohort F 150-mg SC | Cohort G 300-mg SC | Cohort H 600-mg SC | Cohort Ia 600-mg SC | |||
|---|---|---|---|---|---|---|---|---|
| Day 1b | Day 57 | Day 1b | Day 57 | Day 1b | Day 57b,c | Day 1 | ||
| AUC0-t (day×ng/mL) | GM Mean (CV%) | 297,258.1d (13.6) | 835,301.5d (25.8) | 497,570.0d (35.6) | 1,602,363.7d (43.1) | 925,665.2 (35.6) | 2,972,662.7 (31.8) | -d |
| Cmax (ng/mL) | GM Mean (CV%) | 13,551.4 (12.9) | 21,512.2 (14.2) | 22,502.2 (37.7) | 39,102.6 (37.4) | 53,814.9 (36.1) | 91,308.0 (33.4) | 43,100.0e |
| tmax (day) | Median (range) | 5.481 (3.95–13.97) | 3.985 (1.94–12.98) | 5.929 (3.07–13.96) | 3.981 (3.97–4.95) | 4.053 (2.96–14.01) | 4.543 (2.98–14.01) | 4.949e |
| kel (1/day) | Mean (CV%) | 0.03240 (22.8) | 0.02589 (20.5) | 0.03348 (12.0) | ||||
| t1/2 (day) | Mean (CV%) | 22.26 (21.8) | 27.64 (19.4) | 20.91 (12.3) | ||||
| Rac(Cmax)f | Mean (CV%) | 1.607 (13.4) | 1.703 (12.3) | 1.956 (22.3) | ||||
aCohort I = 600-mg SC BITS7201A in one subject with mild atopic asthma
bThe terminal elimination phase for the Day 1 profile for all subjects and for the Day 57 profile for one subject in Cohort H could not be characterized because the time spanned was less than twice the estimated t1/2
cDay 57 parameters for two subjects in Cohort H were excluded from the summary statistics and statistical analysis due to a missed dose on Study Day 29
dAUC0-t for one subject each in Cohorts F, G, and I was excluded from the summary statistics due to early termination
eIndividual value is shown
fRac(Cmax) = Cmax(Day 57)/Cmax(Day 1)
AUC0-t, area under the concentration-time curve from time 0 to the last quantifiable concentration, Cmax maximum serum concentration, CV coefficient of variation, GM Mean geometric mean, kel elimination rate constant, Rac(Cmax) accumulation ratio based on Cmax, SC subcutaneous, tmax time to maximum serum concentration, t1/2 half-life