Disease relevance of Caloxetic acid

• Hepatobiliary enhancement with Gd-EOB-DTPA: comparison of spin-echo and STIR imaging for detection of experimental liver metastases [1].
• In this study, Gd-EOB-DTPA was evaluated in a rodent model of metastatic liver disease to measure both relative enhancement and lesion-to-liver contrast [1].
• Gd-EOB-DTPA enhancement pattern of hepatocellular carcinomas in rats: comparison with Tc-99m-IDA uptake [2].
• Either hyperbilirubinemia, induced by common bile duct ligation, or bromosulfophtalein (BSP) infusion inhibited liver uptake of Gd-EOB-DTPA, resulting in a preferential elimination via the kidney [3].
• Changes in scintigraphic liver activity or MR liver signal intensity were intraindividually monitored over time after intravenous injection of 50 mumol Gd/kg of Gd-EOB-DTPA in controls and rats with common bile duct obstruction or L-ethionine-induced fatty liver (n = 6) [4].

High impact information on Caloxetic acid

• In this study, we demonstrated saturable uptake of gadoxetate by Oatp1 cRNA-injected Xenopus laevis oocytes (Km approximately 3.3 mM) [5].
• 31P spectroscopy of the excised and perfused rat livers was used to monitor the uptake of Gd-EOB-DTPA by the hepatocytes where it enhances the nuclear relaxation of the intracellular metabolites without impairing the adenosine triphosphate metabolism of the cells [6].
• Livers with severed gallbladders behave as the group internalizing more contrast agent, whereas Gd-EOB-DTPA uptake looks impaired in the case of a clamped gallbladder [7].
• In conclusion, Gd-DTPA-DeA and Gd-EOB-DTPA showed stronger contrast enhancement for the rat abdominal aorta and provided MR angiograms of higher image quality when compared with Gd-DTPA at the same injection dose [8].
• CONCLUSION: Gd-DTPA-DeA may be used as a hepatobiliary contrast agent and shows different pharmacokinetics from Gd-EOB-DTPA [9].

Chemical compound and disease context of Caloxetic acid

• METHODS: Eleven rats with chemically induced hepatocellular carcinoma underwent unenhanced T2-weighted fast spin-echo imaging followed by T1-weighted spin-echo imaging before and at 5 minutes, 30 minutes, 3 hours, 1 day, and 3 days after intravenous administration of 60 micromol/kg gadoxetate disodium at 4.7 tesla [10].

Biological context of Caloxetic acid

• Michaelis-Menten kinetics in the extrarenal elimination was therefore considered as the rate-limiting process of Gd-EOB-DTPA, the binding to plasma protein of which is small (10.3 +/- 1.4%) [11].
• Comparison between Gd-DTPA, Gd-EOB-DTPA, and Mn-DPDP in induced HCC in rats: a correlation study of MR imaging, microangiography, and histology [12].

Anatomical context of Caloxetic acid

• In contrast, gadoxetate was not taken up by Oatp2 or OATP cRNA-injected oocytes [5].
• Twelve normal rats, 33 rats treated with agents designed to inhibit biliary excretion of the agent, and 6 rats with surgically ligated common bile ducts received Gd-EOB-DTPA intravenously [3].
• Most of the Gd-EOB-DTPA was rapidly cleared from the body: 89.4% +/- 7.5% of the injected dose within 4 hours after bile duct ligation (group A) and 87.0% +/- 6.0% within 1 hour after ligation of renal vessels (group B) [13].
• In basolateral rat hepatocyte plasma membrane vesicles, Gd-DTPA uptake was indistinguishable from non-specific binding to vesicles; Gd-BOPTA and Gd-EOB-DTPA entered plasma membrane vesicles following a linear, concentration-dependent mechanism up to 1.5 mM of substrate [14].
• Hyperintense visualization of normal extrahepatic bile ducts as well as the GB is regularly achieved with the hepatobiliary contrast agent Gd-EOB-DTPA [15].

Associations of Caloxetic acid with other chemical compounds

• Both Resovist Injection and Eovist Injection have exhibited acceptable safety profiles in clinical trials, and have the potential to provide additional information regarding lesion detection, classification, and characterization [16].
• Gadolinium chelates with hepatobiliary excretion are in clinical trials (Gd BOPTA and Gd EOB-DTPA) [17].

Gene context of Caloxetic acid

• Injection into Xenopus laevis oocytes of 5 ng of human OATP cRNA resulted, after 3 days, in a >/=2-fold stimulation (p < 0.001) of transport of Gd-B 20790 but not of Gd-BOPTA or Gd-EOB-DTPA [14].
• Imaging characteristics of hepatocellular carcinoma using the hepatobiliary contrast agent Gd-EOB-DTPA [18].

Analytical, diagnostic and therapeutic context of Caloxetic acid

• Hepatocyte targeting with Gd-EOB-DTPA: potential application for gene therapy [19].
• Although liver enhancement has been investigated in a number of animal models, tolerance evaluations of Gd-EOB-DTPA injection have been limited [20].
• The Gd-EOB-DTPA polycation conjugates, such as polyethyleneimine-Gd-EOB-DTPA, could serve as transfer vectors of interest for gene targeting imagery at the early stage of hepatocarcinogenesis [19].
• Like liver scintigraphy, functional MR liver imaging using Gd-EOB-DTPA is feasible and can differentiate normal controls from models of biliary and hepatocyte disease [4].
• This finding supports the choice of optimal imaging time post contrast agent administration (for delayed scans) in clinical trials of 20-45 min post injection with Gd-EOB-DTPA and 60-120 min post injection with Gd-BOPTA [21].

References