Pharmacokinetics of the Liver‐Specific Contrast Agent Gd‐EOB‐DTPA in Relation to Contrast‐Enhanced Liver Imaging in Humans

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Abstract
This study was performed to evaluate the effect of dose on the pharmacokinetics and efficacy of the gadolinium‐based contrast medium gadoxetic acid, disodium, [gadolinium (4S)‐4‐(4‐ethoxybenzyl)‐3,6,9‐tris(carboxylatomethyl)‐3,6,9‐triazaundecandioic acid‐disodium salt] (Gd‐EOB‐DTPA) as a liver‐specific hepatobiliary contrast medium for computed tomography. Pharmacokinetics in serum and the pattern of elimination were investigated in 18 healthy volunteers up to 6 days after a 10‐minute infusion of 0.2 mmol, 0.35 mmol, and 0.5 mmol of gadolinium per kilogram of body weight. Pharmacokinetic behavior was compared with the compute tomographic attenuation data in the liver parenchyma after the same doses in patients. Urinary and fecal excretion accounted for approximately equal portions of the administered dose. The degree of renal elimination increased with increasing doses, whereas renal clearance and half‐life from urine data were not affected by dose. Dose‐normalized area under the concentration—time curve was significantly increased with increasing doses indicating saturation in liver uptake for the highest dose. This finding was in agreement with the measured net increase in liver attenuation by computed tomography. Hepatic disposition revealed slight saturation phenomena for the highest dose (0.5 mmol gadolinium/kg). Nevertheless, this dose resulted in sufficient uptake by human liver, allowing for computed tomographic imaging.