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. 2023 Jul 19;14:1208780. doi: 10.3389/fphar.2023.1208780

TABLE 1.

PK parameters of brensocatib in C57BL/6 and BALB/c mice during the first 24 h of BID or QD dosing.

BID QD
C57BL/6 Dose (mg/kg/day) 0.5 2 20 0.75 3 30
AUC0–24h (ng•h/mL) 294 ± 49 2012 ± 154 15,866 ± 3505 735 ± 108 2843 ± 302 52,565 ± 6720
AUC(0–24) (µmol•h/L) 0.70 ± 0.12 4.79 ± 0.37 37.73 ± 8.33 1.75 ± 0.26 6.76 ± 0.72 125.01 ± 15.98
t1/2 (h), AM dose 0.71 ± 0.23 2.07 ± 0.42 2.41 ± 0.42 9.62 ± 0.95 6.38 ± 0.56 3.01 ± 0.18
t1/2 (h), PM dose 0.63 ± 0.01 2.35 ± 0.35 2.36 ± 0.05 n/a n/a n/a
BALB/c Dose (mg/kg/day) 0.2 2 20 0.3 3 30
AUC0–24h (ng•h/mL) 124 ± 31 1508 ± 395 24,105 ± 4779 188 ± 31 2964 ± 679 56,303 ± 17,303
AUC(0–24) (µmol•h/L) 0.29 ± 0.07 3.59 ± 0.94 57.32 ± 11.36 0.45 ± 0.07 7.05 ± 1.61 133.90 ± 41.15
t1/2 (h), AM dose 1.58 ± 0.72 3.22 ± 0.35 2.47 ± 0.31 0.97 ± 0.03 0.83 ± 0.03 2.56 ± 0.14
t1/2 (h), PM dose 0.67 ± 0.04 1.19 ± 0.34 1.88 ± 0.06 n/a n/a n/a

AUC, area under the concentration-time curve; t1/2 = half life. Data are presented as mean ± SEM (n = 4, except for C57 20 mg/kg/day where n = 3, C57 3 mg/kg/day and 30 mg/kg/day where n = 6, and Balb/c 2 mg/kg/day where n = 3). n/a, not applicable.