Preclinical Evaluation of [¹⁸F]LCATD as a PET Tracer to Study Drug-Drug Interactions Caused by Inhibition of Hepatic Transporters

Table 1

Kinetic parameters for [¹⁸F]LCATD as mean ±1 s.d., .

Group	t_max (s)	Cmax,liver (% ID·mL^−1)	AUCliver 0–5 min (% ID·min·mL^−1)	Kpliver 0−5 min	AUCliver 0–30 min (% ID·min·mL^−1)	AUCbile 0–10 min (% ID·min·mL^−1)	CLuptake,in vivo (mL·min^−1·g^−1)	CLint,bile (mL·min^−1·g^−1)
Control	135	14.3 ± 0.9	58 ± 1	3.64 ± 0.09	110 ± 15	89 ± 1	2.09 ± 0.27	0.17 ± 0.03
Rifamycin SV-treated	225	10.2 ± 0.9	44 ± 4	2.07 ± 0.17	139 ± 9	53 ± 3	0.71 ± 0.05	0.12 ± 0.03
Fusidate-treated	135	11.5 ± 0.3	48 ± 0.3	2.451 ± 0.016	89 ± 11	93 ± 19	1.40 ± 0.13	0.36 ± 0.03

Statistical significance of rifamycin-SV and fusidate-treated rats compared to the control was assessed by two-tailed t-test assuming equal variances, . t_max: time to maximum peak concentration; C_max,liver: maximum measured activity in the liver; AUC_{liver 0–5 min}: area under the curve for the liver from 0 to 5 minutes postinjection; K_{p liver 0–5 min}: apparent liver-to-blood AUC_0–5 min ratio; AUC_{liver 0–30 min}: area under the curve for the liver from 0 to 30 minutes postinjection; AUC_{bile0–10 min}: area under the curve for the bile (as radioactivity measured in the gastrointestinal tract) from 0 to 10 minutes postinjection; CL_{uptake,in vivo}:in vivo uptake clearance; CL_int,bile: intrinsic biliary clearance of the radiotracer.