TABLE 1

Summary statistics of BMS-823778 PK parameters in healthy subjects after a single ascending dose of BMS-823778 in the dose range of 0.1–100 mg

PK parameters were estimated using a noncompartment method. PK parameters were not calculated for subjects in the 0.1- and 0.5-mg dose panels owing to insufficient numbers of plasma samples above the bioanalytical LLOQ; AUV(INF), half-life, and CLT/F in the 2- and 5-mg dose panels were not estimated because the percentage of extrapolated AUC for the calculation of AUC(INF) was >20% of the AUC(0-T) values.

Treatment GroupCmax (ng/ml) Mean [n] (CV)Tmax (h) Median [n] (Min-Max)AUC(0-T) (ng⋅h/ml) Mean [n] (CV)AUC(INF) (ng⋅h/ml) Mean [n] (CV)Half-Life (h) Mean [n] (S.D.)CLT/F (ml/min) Mean [n] (CV)
0.1 mgNANANANANANA
0.5 mgNANANANANANA
2 mg1.98 [6] (73)3.25 [4] (2.0–6.0)109 [6] (54)NANANA
5 mg19.0 [6] (22)2.50 [6] (1.0–4.0)612 [6] (47)NANANA
12 mg84.7 [6] (14)1.25 [6] (0.6–2.0)2221 [6] (34)2389 [6] (36)50.4 [6] (6.09)83.7 [6] (41)
25 mg206 [6] (19)1.48 [6] (0.5–3.0)5610 [6] (20)5837 [6] (21)40.3 [6] (5.77)71.4 [6] (21)
50 mg483 [6] (12)1.00 [6] (1.0–2.5)12,031 [6] (41)12,826 [6] (48)43.6 [6] (14.5)65.0 [6] (46)
100 mg990 [6] (29)0.74 [6] (0.5–2.5)23,912 [6] (39)24,544 [6] (40)31.7 [6] (6.56)67.9 [6] (34)
  • CV, percent coefficient of variation; n, number of subjects with evaluable PK data; NA, not applicable.