eprotirome

Eprotirome is a small molecule, liver-selective thyroid hormone receptor beta agonist (thyromimetic) developed for the treatment of dyslipidemia and obesity. It works by selectively stimulating the thyroid hormone receptor beta in the liver, leading to increased expression of hepatic LDL-receptor genes, which enhances clearance of LDL cholesterol from plasma. Eprotirome also reduces triglycerides and lipoprotein(a), increases energy expenditure, and lowers blood glucose. The drug was designed to minimize uptake in nonhepatic tissues to avoid adverse effects associated with systemic thyroid hormone therapy. Clinical trials demonstrated significant reductions in LDL cholesterol, triglycerides, and Lp(a) when used alone or with statins or ezetimibe. However, development was discontinued after preclinical studies revealed cartilage toxicity in dogs[1][2][3][4][5][6].

Other names

eprotirome [INN]