Intravenous Administration (iv) Compound Cpa (mg/mL) tmax (h) AUClast (h•µg/mL) AUCinf (h•µg/mL) MRTlast (h) Cl (mL/h/kg) V (L/kg) t½ (h)   Free acid 132 ± 28 0.08 ± 0.00 98 ± 8 101 ± 67 1.2 ± 0.2 743 ± 48 2.6 ± 0.6 2.4 ± 0.4   Hippuric acid salt 229 ± 45 0.08 ± 0.00 154 ± 25 157 ± 25 1.1 ± 0.1 488 ± 83 1.3 ± 0.9 1.7 ± 0.9   Succinic acid salt 215 ± 16 0.08 ± 0.00 145 ± 31 146 ± 31 1.0 ± 0.1 527 ± 100 1.1 ± 0.6 1.4 ± 0.5   Meglumine salt 184 ± 33 0.08 ± 0.00 110 ± 26 110 ± 26 0.8 ± 0.2 711 ± 188 1.2 ± 0.2 1.2 ± 0.1   L-Lysine salt 185 ± 15 0.08 ± 0.00 121 ± 12 123 ± 11 1.0 ± 0.1 613 ± 54 1.4 ± 0.7 1.7 ± 1.0   Oral Administration (po) Compound Cmax (ng/mL) tmax (h) AUClast (h•µg/mL)           Fb (%) Free acid NDc ND ND           ND Hippuric acid saltd 227 1 122           0.05 Succinic acid salte 639 0.63 376           0.18 Meglumine saltd 221 0.25 NCf           NC L-Lysine saltd 214 0.50 74           0.04 aCp is the first measurable concentration in plasma after dose administration. bThe bioavailability F is expressed as a percentage. cND = no data; the test article was never detected. dResults derived from samples collected in one animal; no standard deviation is available. eResults derived from samples collected in two animals; no standard deviation is available. fNC = not calculated; only one data point was available.

Table 3. Mean iv and individual po pharmacokinetic parameters of 3,4,3-LI (1,2-HOPO) and four salt forms after a single 100 µmol/kg administration in male Sprague- Dawley rats (n = 3).