The resurgence of thyromimetics as lipid-modifying agents.
The aggressive reduction of LDL-cholesterol levels by treatment with statins is a key component of preventive cardiovascular care; however, additional therapies to prevent atherosclerosis and the associated clinical sequelae are still needed. Thyromimetic compounds selective for the liver or for the thyroid hormone receptor isoform beta1 constitute a novel approach for the treatment of dyslipidemia. In preclinical studies, selective thyromimetics significantly reduced plasma cholesterol levels and provided protection from atherosclerosis by upregulating the hepatic LDL receptor and promoting reverse cholesterol transport. Importantly, data from ongoing clinical trials have provided the first evidence that selective thyromimetics may also reduce the levels of plasma cholesterol in humans.
Tancevski
Ivan
I
Innsbruck Medical University, Department of Internal Medicine, Anichstrasse 35, Innsbruck 6020, Austria. ivan.tancevski@i-med.ac.at
Eller
Philipp
P
Patsch
Josef R
JR
Ritsch
Andreas
A
D000085:Acetates / Q000737:chemistry / Q000494:pharmacology; D000813:Anilides / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000924:Anticholesteremic Agents / Q000627:therapeutic use; D001161:Arteriosclerosis / Q000188:drug therapy / Q000517:prevention & control; D050197:Atherosclerosis / Q000517:prevention & control; D001692:Biological Transport; D032701:Biomimetics; D008078:Cholesterol, LDL / Q000097:blood / Q000378:metabolism; D002986:Clinical Trials as Topic; D050171:Dyslipidemias / Q000188:drug therapy; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000627:therapeutic use; D000960:Hypolipidemic Agents / Q000627:therapeutic use; D050356:Lipid Metabolism; D008314:Malonates / Q000494:pharmacology; D015394:Molecular Structure; D063065:Organophosphonates / Q000737:chemistry / Q000494:pharmacology; D010636:Phenols / Q000737:chemistry / Q000494:pharmacology; D010647:Phenyl Ethers / Q000494:pharmacology; D010648:Phenylacetates / Q000494:pharmacology; D011422:Propionates / Q000494:pharmacology; D011724:Pyridazines / Q000494:pharmacology; D011973:Receptors, LDL / Q000378:metabolism; D013961:Thyroid Gland / Q000187:drug effects*; D013963:Thyroid Hormones / Q000378:metabolism*
C539547:2-((3,5-dimethyl-4-(4'-hydroxy-3'-isopropylbenzyl)phenoxy)methyl)-4-(3-chlorophenyl)-2-oxido(1,3,2)dioxaphosphonane; C113777:2-amino-3-(3,5-dibromo-4-(4-hydroxy-3-(6-oxo-1,6-dihydro-pyridazin-3-ylmethyl)-phenoxyl)-phenyl)-propionic acid; C526273:3-((3,5-dibromo-4-(4-hydroxy-3-(1-methylethyl)phenoxy)phenyl)amino)-3-oxopropanoic acid; D000085:Acetates; D000813:Anilides; D000924:Anticholesteremic Agents; D008078:Cholesterol, LDL; C413355:GC 1 compound; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D000960:Hypolipidemic Agents; C478108:KB 141; D008314:Malonates; C496199:N-(4-(3-((4-fluorophenyl)hydroxymethyl)-4-hydroxyphenoxy)-3,5-dimethylphenyl) malonamic acid sodium; D063065:Organophosphonates; D010636:Phenols; D010647:Phenyl Ethers; D010648:Phenylacetates; D011422:Propionates; D011724:Pyridazines; D011973:Receptors, LDL; D013963:Thyroid Hormones
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