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. 2012 Dec 11;71(3):581–591. doi: 10.1007/s00280-012-2033-5

Table 5.

Pharmacokinetic parameters (a) acadesine, (b) ZMP

Cohort Dose (mg/kg) t max (h) C max (ng/mL) AUC(0→24h) (ng h/mL) t ½ (h)
(A)
Part I
 1 50
 Median 4.0 4,325 14,251 5.2
 Minimum 3.7 2,930 9,800 1.0
 Maximum 4.3 8,139 21,213 45.4
 2 83.5
 Median 4.1 6,888 24,614 35.0
 Minimum 4.1 5,148 15,986 5.2
 Maximum 4.5 10,036 32,534 79.4
 3 139.5
 Median 4.0 12,439 39,503 25.3
 Minimum 3.9 2,449 11,549 3.8
 Maximum 4.0 30,574 89,015 28.5
 4 210
 Median 4.0 38,736 123,125 16.2
 Minimum 4.0 30,431 118,235 10.2
 Maximum 4.1 64,672 240,500 35.7
 5 315
 Median 4.5 35,170 240,403 61.4
 Minimum 4.2 33,855 171,809 2.6
 Maximum 4.7 65,536 275,298 62.0
Part II
 6 2 × 210
 Day 1
  Median 4.1 41,851 195,556 24.6
  Minimum 4.0 7,177 26,315 14.2
  Maximum 4.4 68,366 228,532 25.8
 Day 4
   Median 4.2 28,774 126,430 98.8
   Minimum 4.0 2,213 14,858 18.8
   Maximum 4.5 45,939 149,534 106.2
 7 5 × 210
 Day 1
  Median 4.3 49,533 161,939 3.9
  Minimum 4.3 41,619 117,843 3.0
  Maximum 4.6 54,892 198,014 12.0
 End of treatment
  Median 4.1 51,456 198,646 56.2
  Minimum 4.0 51,160 148,617 3.8
  Maximum 4.2 67,684 231,356 65.1
(B)
Part I
 1 50
 Median 4.3 52,101 312,131 72.3
 Minimum 3.67 7,666 20,438 0.5
 Maximum 5.03 93,198 424,582 239.9
 2 83.5
 Median 4.5 73,023 562,247 35.1
 Minimum 4.08 71,775 360,973 34.5
 Maximum 5.08 76,814 577,760 95.2
 3 139.5
 Median 4.0 114,001 1,023,992 66.4
 Minimum 4.00 94,144 701,177 17.6
 Maximum 4.58 156,663 1,343,691 91.2
 4 210
 Median 4.1 270,988 2,066,170 39.8
 Minimum 4.00 185,258 1,910,548 22.2
 Maximum 5.08 295,124 2,159,142 118.2
 5 315
 Median 4.5 243,540 2,434,242 8.1
 Minimum 4.17 157,154 1,472,810 5.7
 Maximum 4.68 342,195 2,873,273 111.7
Part II
 6 2 × 210
 Day 1
  Median 4.1 275,836 2,610,904 24.3
  Minimum 4.00 152,335 853,666 12.7
  Maximum 4.42 312,929 2,747,816 26.5
 Day 4
  Median 4.7 223,390 2,081,843 81.5
  Minimum 4.00 95,310 738,586 64.4
  Maximum 5.50 229,030 2,538,271 134.1
 7 5 × 210
 Day 1
  Median 5.7 265,536 1,833,232 16.6
  Minimum 5.33 159,539 1,056,891 11.4
  Maximum 6.33 344,686 2,866,182 45.4
End of treatment
 Median 4.2 188,936 1,942,209 71.3
 Minimum 4.00 108,108 870,256 16.2
 Maximum 5.08 265,657 2,152,337 98.1

T max time of maximum drug concentration, C max maximum drug concentration, AUC 0→24 area under the time–concentration curve from 0 to 24 h, and half life