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Table 3 PK parameters for TRO40303 in healthy male and female subjects following single i.v. administration

From: Translation of TRO40303 from myocardial infarction models to demonstration of safety and tolerance in a randomized Phase I trial

Parameter (unit)   Dose level (mg/kg)
   0.5 (n = 6) 1 (n = 6) 2 (n = 6) 3.5 (n = 9) 6 (n = 12) 10 (n = 9) 13 (n = 6)
C max (μg/mL) Mean 3.32 10.3 23.1 51.7 118 194 259
  Min-max 2.31-4.85 6.06-14.1 16.0-31.1 37.7-68.7 59.5-266 130-279 167-371
  CV 28.5% 29.8% 25.4% 20.8% 47.3% 23.2% 29.7%
C 5min (μg/mL) Mean 2.58 9.26 23.6** 50.2 112 193 248
  Min-max 1.59-3.92 5.98-12.5 16.7-26.8 37.1-68.7 51.6-266 120-279 148-371
  CV 32.0% 26.7% 17.7% 22.9% 52.3% 24.3% 31.6%
AUC (0-∞) (μg.h/mL) Mean 15.5* 34.5 68.6 109 229*** 408 651
  Min-max 9.13-20.9 21.0-43.0 50.7-81.5 81.0-163 147-307 303-501 468-814
  CV 35.0% 21.8% 17.1% 23.6% 21.8% 18.8% 21.4%
Terminal t 1/2 (h) Mean 29.5 25.1 26.4 25.1 24.4 25.3 24.4
  Min-max 27.0-31.5 22.9-26.8 24.3-28.7 23.1-27.7 21.2-30.0 19.3-30.2 20.1-28.6
  CV 6.3% 5.6% 6.2% 7.0% 11.1% 12.8% 12.4%
CL (mL/min/kg) Mean 0.598 0.509 0.499 0.560 0.460 0.422 0.347
  Min-max 0.399-0.912 0.388-0.792 0.409-0.657 0.357-0.721 0.326-0.680 0.332-0.549 0.266-0.463
  CV 39.3% 28.6% 18.7% 20.9% 25.3% 20.0% 22.7%
V z (mL/kg) Mean 1.54 1.11 1.14 1.22 0.964 0.929 0.723
  Min-max 1.03-2.49 0.899-1.77 0.910-1.52 0.723-1.52 0.611-1.34 0.624-1.44 0.599-0.989
  CV 43.4% 30.5% 19.7% 20.5% 23.5% 26.8% 20.0%
  1. *n = 4; **n = 5; ***n = 11.