Eprotirome (KB2115), a synthetic thyroid hormone mimetic, is a thyroid hormone receptor agonist.

In moderately overweight and hypercholesterolemic subjects Eprotirome (KB2115) was found to be safe and well tolerated and elicited up to a 40% lowering of total and LDL cholesterol after 14 days of treatment. Bile acid synthesis was stimulated without evidence of increased cholesterol production [1]. KB2115 treated mice exhibited increased fasting glucose, although KB2115 did not increase fasting insulin levels [2].

A catheter was implanted into the right internal jugular vein before the hyperinsulinemic-euglycemic clamp. After recovery, mice were administered GC-1 (0.03 or 0.3 mg/kg), KB2115 (0.3 mg/kg) or T3 (0.06 mg/kg) via intraperitoneal injection for 10 days. On the day of the clamp experiment, conscious, overnight-fasted mice received a primed (10 μCi) and constant rate intravenous infusion (0.1 uCi/min) of [3-3H] glucose to measure basal glucose turnover. After 60–75 minutes of labeled glucose infusion, the hyperinsulinemic-euglycemic clamp was performed with continuous infusion of insulin (12 mU/kg/min) and variable infusion of 25% glucose to maintain euglycemia (~120 mg/dl). Blood samples were collected by tail bleeding (approximately every 10 min) to measure blood glucose concentrations [2].