Pharmacokinetics | Rx | Ex vivo pharmacodynamica | Combined P + M | Ex vivo potency | % AUC0–20 | |||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Parameter | Unit | Median | 25th IQT | 75th IQT | pb | Median | 25th IQT | 75th IQT | pb | ePD/PK | AS/AL | AUC0–∞ | ||
C cmax | mM | IV AL | 7.76 | 7.09 | 8.13 | <0.001 | 64.6 | 62.7 | 68.5 | <0.001 | 0.120 | Â | Â | |
IV AS | 20.7 | 15.3 | 30.5 | 35.2 | 31.3 | 44.4 | 0.587 | 4.89 | Â | |||||
t d1/2 | min | IV AL | 29.6 | 26.3 | 38.0 | 0.7 | 36.3 | 30.6 | 44.8 | 0.02 | 0.815 | Â | Â | |
IV AS | 29.9 | 23.4 | 33.2 | 29.1 | 23.7 | 31.4 | 1.028 | 1.26 | Â | |||||
AUC e0–∞ | mM min | IV AL | 426 | 365 | 521 | 0.8 | 4911 | 3997 | 5827 | <0.001 | 0.088 |  |  | |
IV AS | 485 | 297 | 586 | 764 | 698 | 926 | 0.643 | 7.31 | Â | |||||
AUC f0–20 | mM min | IV AL | 115 | 109 | 121 | <0.001 | 1051 | 1007 | 1107 | <0.001 | 0.110 |  | 21.4 | |
IV AS | 242 | 172 | 348 | 404 | 373 | 502 | 0.598 | 5.44 | 52.9 | |||||
Clg | L kg−1 min−1 | IV AL | 48.5 | 39.5 | 57.0 | 0.83 |  | |||||||
IV AS | 43.0 | 35.7 | 70.6 | |||||||||||
V hz | L kg−1 | IV AL | 2.14 | 1.91 | 2.32 | 0.57 |  | |||||||
IV AS | 1.84 | 1.41 | 2.87 |