Preclinical evaluation of Gd-EOB-DTPA as a contrast agent in MR imaging of the hepatobiliary system

Radiology. 1992 Apr;183(1):59-64. doi: 10.1148/radiology.183.1.1549695.


Gadolinium diethylenetriaminepentaacetic acid (DTPA) covalently linked to the lipophilic ethoxybenzyl moiety (Gd-EOB-DTPA) was designed for use as a contrast agent in hepatobiliary magnetic resonance imaging. With T1 relaxivity values of 8.7 L/mmol.second in plasma and 16.6 L/mmol.second in rat liver tissue and a median lethal dose of 10 mmol/kg when administered intravenously in mice and rats, Gd-EOB-DTPA has a fairly high margin of safety. In rats and monkeys, biodistribution studies performed 7 days after administration of 0.25 mmol/kg revealed very little retention of gadolinium (less than 1%) in the tissues, indicating complete elimination via renal and biliary excretion. Biliary excretion was inhibited by coadministration of sulfobromophthalein, indicating the involvement of a carrier-mediated transport system based on the enzyme glutathione-S-transferase. In rats, the biliary transport maximum was 5 mumol gadolinium/ High T1 relaxivity of Gd-EOB-DTPA in rat liver in vivo can be explained by transient interaction with intracellular components and by increased microviscosity inside the hepatocyte.

MeSH terms

  • Animals
  • Bile / metabolism
  • Biliary Tract / anatomy & histology*
  • Contrast Media* / pharmacokinetics
  • Contrast Media* / toxicity
  • Drug Evaluation
  • Female
  • Gadolinium DTPA*
  • Humans
  • Liver / anatomy & histology*
  • Macaca fascicularis
  • Magnetic Resonance Imaging*
  • Organometallic Compounds* / pharmacokinetics
  • Organometallic Compounds* / toxicity
  • Pentetic Acid* / pharmacokinetics
  • Pentetic Acid* / toxicity
  • Rats
  • Tissue Distribution


  • Contrast Media
  • Organometallic Compounds
  • gadolinium ethoxybenzyl DTPA
  • Pentetic Acid
  • Gadolinium DTPA