Table 2. Pharmacokinetic results.
Patient | Dose (mg m−2) | Cycle | Cmax (μg l−1) | AUClast (ha μg l−1) | T1/2λz (h) | CL (observed) (l h−1) | Vz (observed) (l) |
---|---|---|---|---|---|---|---|
1 | 48 | 1inj2 | 1737 | 463 | 0.54 | 181 | 142 |
2 | 48 | 1inj2 | 2724 | 848 | 0.51 | 94 | 69 |
1inj8 | 2059 | 630 | 0.61 | 125 | 109 | ||
2inj8 | 1629 | 498 | 0.57 | 158 | 131 | ||
3 | 48 | 1inj2 | 2253 | 1143 | 0.61 | 83 | 72 |
1inj8 | 1289 | 816 | 0.42 | 115 | 69 | ||
4 | 65 | 1inj3 | 2074 | 566 | 0.20 | 190 | 55 |
5 | 65 | 1inj2 | 4371 | 1498 | 0.45 | 64 | 41 |
1inj8 | 4105 | 1312 | 0.73 | 74 | 78 | ||
7 | 65 | 1inj2 | 2968 | 2510 | 0.82 | 74 | 88 |
1inj8 | 2914 | 2068 | 0.65 | 89 | 84 | ||
8 | 85 | 1inj2 | 2335 | 1809 | 0.39 | 79 | 45 |
1inj8 | 3672 | 2375 | 0.60 | 60 | 52 | ||
2inj8 | 2804 | 1619 | 0.74 | 88 | 94 | ||
9 | 85 | 1inj2 | 1624 | 1151 | 0.71 | 133 | 136 |
10 | 85 | 1inj2 | 2057 | 2094 | 0.71 | 102 | 104 |
1inj8 | 1354 | 1250 | 2.05 | 151 | 447 | ||
11 | 110 | 1inj2 | 3507 | 4016 | 0.62 | 46 | 41 |
12 | 110 | 1inj2 | 2750 | 2345 | 0.69 | 70 | 70 |
13 | 110 | 1inj2 | 3237 | 3842 | 0.55 | 83 | 66 |
1inj8 | 3578 | 3796 | 0.62 | 84 | 75 | ||
14 | 145 | 1inj2 | 4851 | 4946 | 0.87 | 55 | 69 |
1inj8 | 3922 | 4428 | 0.57 | 62 | 51 | ||
15 | 145 | 1inj2 | 2869 | 3471 | 0.89 | 92 | 119 |
16 | 145 | 1inj2 | 1217 | 2021 | 0.71 | 150 | 153 |
1inj8 | 2080 | 2349 | 0.67 | 169 | 164 | ||
2inj8 | 1342 | 1779 | 0.72 | 224 | 233 | ||
17 | 145 → 190 | 1inj2 | 4159 | 3389 | 0.68 | 64 | 63 |
1inj8 | 3370 | 4467 | 0.62 | 63 | 57 | ||
18 | 145 → 190 | 1inj2 | 2474 | 1928 | 0.50 | 96 | 70 |
1inj8 | 2274 | 2390 | 0.50 | 103 | 74 | ||
3inj2 | 6517 | 7173 | 0.75 | 44 | 48 | ||
19 | 145 → 190 | 1inj2 | 2961 | 3683 | 0.79 | 66 | 75 |
2inj1 | 4002 | 6451 | 0.77 | 49 | 54 | ||
20 | 145 → 190 | 1inj2 | 2774 | 3397 | 0.66 | 89 | 85 |
1inj8 | 2066 | 2611 | 0.81 | 151 | 176 | ||
2inj8 | 3341 | 5044 | 0.72 | 79 | 82 | ||
21 | 145 → 190 | 1inj2 | 2894 | 2621 | 1.36 | 100 | 196 |
1inj8 | 2161 | 2178 | 2.38 | 142 | 488 | ||
22 | 145 → 190 | 1inj2 | 2795 | 2870 | 0.67 | 101 | 97 |
23 | 145 → 190 | 1inj2 | 3202 | 2465 | 1.15 | 72 | 119 |
24 | 145 → 190 | 1inj2 | 1177 | 1267 | 0.38 | 215 | 118 |
1inj8 | 493 | 816 | 0.42 | 352 | 214 | ||
25 | 145 → 190 | 1inj2 | 4508 | 4094 | 0.49 | 55 | 39 |
1inj8 | 4283 | 5360 | 0.58 | 56 | 46 | ||
27 | 145 → 190 | 1inj2 | 2625 | 1578 | 0.69 | 106 | 106 |
Cmax=maximum concentration; Tmax=time of maximum observed concentration, AUClast=area under the curve from time of dosing to the last measurable concentration; AUCinf=area under the curve from the time of dosing to infinity; t1/2λz=terminal half-life ln2/λz, where λz is the first-order rate constant associated with the terminal log-linear portion of the curve; MRTlast=mean residence time from the time of dosing to the last measurable concentration; Vz=volume of distribution based on the terminal phase dose/λz*AUCinf; CL=total body clearance.
Patient 6 and 26 – not evaluable for PK, samples not taken.