Drug intelligence / Profile preview

dextrothyroxine

Development stage
Phase 3
Modality
Small Molecules
Administration
Oral
01

Overview

Dextrothyroxine is the dextrorotary isomer of thyroxine and acts as a synthetic thyroid hormone. It was developed and marketed under the brand name Choloxin as an antihyperlipidemic agent for lowering high circulating cholesterol levels, particularly in hyperlipidemia. Its mechanism of action involves stimulating the formation and catabolism of low-density lipoprotein (LDL) in the liver, leading to increased excretion of cholesterol and bile acids via the biliary route. This results in reduced serum cholesterol and LDL levels without significantly affecting high-density lipoproteins (HDL). As a prohormone, dextrothyroxine also binds to thyroid hormone receptors (alpha and beta) as an agonist and serves as a substrate for iodide peroxidase. The drug was withdrawn from clinical use due to cardiac side effects[1][2][3][5].

Brand names
Choloxin
Other names
D-3,5,3',5'-tetraiodothyronine
02

Targets

THRB (Thyroid hormone receptor beta)TPO (Thyroid peroxidase)THRA (Thyroid hormone receptor alpha)

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