Selenium ⁷⁵Se tauroselcholic acid Other names: Tauroselcholic acid SE-75

Mechanism of action

Tauroselcholic acid is a bile acid analogue which shows identical physiological behaviour with naturally occurring bile acid conjugates.

Pharmacodynamic properties

Pharmacodynamic effects

At the chemical concentrations and activities used for diagnostic procedures [75Se]tauroselcholic acid does not appear to exert any pharmacodynamic effects.

Paediatric population

No data are available.

Pharmacokinetic properties

Distribution

The distribution of activity is almost entirely confined to the lumen of the biliary ducts, gut and liver.

Organ Uptake

Following oral administration in normal subjects, approximately 95% of the labelled bile acid is absorbed, mainly by the terminal ileum during each enterohepatic cycle.

Elimination

Whole body retention data from normal subjects showed 97 to 100% of [75Se]tauroselcholic was excreted with a biological half-life of 2.6 days and that, in most cases, a small component of about 3% was eliminated with a mean half time of 62 days.

Paediatric population

No data are available.

Preclinical safety data

A single dose study in rats has indicated a safety margin of greater than 10,000 times the maximum human oral dosage. This agent is not intended for regular or continuous administration. Repeat dose toxicity studies, mutagenicity and long-term carcinogenicity studies have not been performed.

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