Table 1.
Variable | 0.1 mg LY3045697 (n=6) |
0.3 mg LY3045697 (n=6) |
1 mg LY3045697 (n=6) |
3 mg LY3045697 (n=6) |
10 mg LY3045697 (n=6) |
30 mg LY3045697 (n=6) |
100 mg LY3045697 (n=6) |
300 mg LY3045697 (n=6) |
---|---|---|---|---|---|---|---|---|
After single daily dose of LY3045697 in the fed state | ||||||||
Cmax (ng/ml) | 0.32 (28) | 1.10 (33) | 1.96 (49) | 9.95 (37) | 27.9 (24) | 83.7 (25) | 458 (27) | 951 (20) |
tmax (h)a | 0.75 (0.50–1.00) | 0.50 (0.50–1.00) | 1.00 (0.50–2.00) | 0.50 (0.50–0.50) | 0.75 (0.50–2.00) | 1.00 (0.50–2.00) | 0.50 (0.50–1.00) | 0.50 (0.50–1.00) |
AUC0–inf (h*ng/ml) | nrb | nrb | 12.1 (51)c | 49.1 (31)d | 138 (19) | 482 (32) | 1726 (15) | 6226 (19) |
t1/2 (h) | nrb | nrb | 9.11 (43)c | 8.73 (32)d | 9.99 (20) | 9.57 (20) | 9.62 (28) | 10.8 (30) |
After 8 once-daily doses of LY3045697 in the fed state | ||||||||
(n=12) | (n=12) | (n=12) | (n=12) | |||||
Cmax (ng/ml) | 0.368 (30) | 3.45 (36) | 37.4 (29) | 371 (37) | ||||
tmax (h) a | 0.95 (0.50–3.00) | 0.95 (0.50–3.00) | 0.95 (0.50–2.00) | 0.95 (0.50–0.95) | ||||
AUC0–tau (h*ng/ml) | NC | 19.2 (29) | 195 (22) | 1818 (28) | ||||
t1/2 (h) | e | e | 9.84 (18) | 10.8 (26) |
AUC0–inf : area under the plasma concentration-time curve from time 0 to infinity; AUC0–tau: area under the plasma concentration-time curve during the dosing interval of 24 h; Cmax: maximum observed plasma concentration; CI: confidence interval; h: hour; n: number of subjects exposed; NC: if no quantifiable observations were reported until 24 h post-dose than AUC0–tau was not calculated; nr: not reported; t1/2: terminal elimination half-life; tmax: time to attain Cmax.
Median (range); bhalf-life and other PK parameters that rely on the terminal phase elimination rate constant were not calculable due to inadequate quantifiable observation interval; cn=3; dn=5; enot reported due to inadequate quantifiable terminal phase.