Table 2.
Pharmacokinetic parameters for BMS-986142 after (a) single-dose administration and (b) at steady state after multiple-dose administration
| a. SAD, day 1 | ||||||
| BMS-986142 treatment dose | Cmax (ng/mL) geometric mean (%CV) | Tmax (h) median (min, max) | AUC(0-T) (ng h/mL) geometric mean (%CV) | AUC(inf) (ng h/mL) geometric mean (%CV) | T1/2 (h) mean (SD) | |
| 5 mg, n = 6 | 9.03 (37) | 2.03 (1.00, 4.00) | 83.1 (51) | 102 (52)a | 6.87 (3.35)a | |
| 15 mg, n = 6 | 36.9 (21) | 2.00 (1.00, 2.00) | 369 (12) | 388 (10) | 8.02 (1.37) | |
| 50 mg, n = 6 | 185 (38) | 1.00 (1.00, 2.05) | 1561 (31) | 1586 (31) | 9.70 (1.65) | |
| 100 mg, n = 6 | 311 (17) | 1.50 (1.00, 2.00) | 2999 (14) | 3019 (14) | 10.3 (1.03) | |
| 300 mg, n = 6 | 1081 (25) | 1.02 (1.00, 2.00) | 11,347 (21) | 11,390 (21) | 10.6 (1.05) | |
| 900 mg, n = 6 | 1878 (31) | 2.00 (1.00, 4.00) | 28,026 (32) | 28,063 (31) | 10.7 (2.01) | |
| b. MAD, day 14 | ||||||
| BMS-986142 treatment dose | Cmax (ng/mL) geometric mean (%CV) | Tmax (h) median (min, max) | Cmin (ng/mL) geometric mean (%CV) | AUC(TAU) geometric mean (%CV) | AI_AUC geometric mean (%CV) | T1/2 (h) mean (SD) |
| 25 mg, n = 6 | 56.0 (25) | 2.00 (2.00, 4.00) | 7.85 (42) | 539 (34) | 1.57 (22) | 10.9 (1.8) |
| 75 mg, n = 6 | 281 (34) | 2.00 (1.00, 2.00) | 27.9 (77) | 2471 (44) | 1.23 (31) | 10.7 (1.6) |
| 200 mg, n = 6 | 592 (37) | 2.00 (1.00, 2.00) | 67.6 (63) | 5527 (41) | 1.23 (40) | 11.0 (4.6) |
| 350 mg, n = 6 | 1024 (14) | 1.50 (1.00, 2.00) | 166 (41) | 10,715 (26) | 0.984 (32) | 10.2 (0.9) |
AI_AUC AUC accumulation index, AUC (0-T) area under the plasma concentration-time curve from time zero to the time of the last quantifiable concentration, AUC (inf) area under the plasma concentration-time curve from time zero extrapolated to infinite time, AUC (TAU) area under the plasma concentration-time curve in one dosing interval, C max maximum observed plasma concentration, C min minimum observed plasma concentration, MAD multiple ascending dose, SAD single ascending dose, T 1/2 terminal plasma half-life, SD standard deviation, T max time to maximum observed plasma concentration
a n = 5