Drug intelligence / Profile preview

Eprotirome + ezetimibe

Development stage
Discontinued
Lead developer
Karo Bio
Modality
Small Molecules
Administration
Oral
01

Overview

Eprotirome + ezetimibe is a combination of two lipid-lowering agents. Eprotirome (KB2115) is a liver-selective thyroid hormone receptor beta agonist developed by Karo Bio, designed to lower plasma LDL cholesterol and stimulate bile acid synthesis. Ezetimibe is a cholesterol absorption inhibitor that blocks the Niemann-Pick C1-Like 1 (NPC1L1) protein in the small intestine, reducing intestinal absorption of cholesterol and phytosterols. This combination was investigated for use in patients with familial hypercholesterolemia to further reduce LDL cholesterol when added to statin therapy, but development of eprotirome was discontinued due to safety concerns including potential liver injury and cartilage damage[3][4][8].

02

Targets

THRB (Thyroid hormone receptor beta)NPC1L1 (Niemann-pick C1-Like 1 transporter)

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