Discovery and\nPreclinical Profile of ALG-055009, a\nPotent and Selective Thyroid Hormone Receptor Beta (THR-β) Agonist\nfor the Treatment of MASH

Agonists of thyroid hormone receptor\nβ (THR-β)\ndecreased\nLDL cholesterol (LDL-C) and triglyceride (TG) levels in human clinical\ntrials for patients with dyslipidemia. The authors present the highly\npotent and selective compound ALG-055009 (<b>14</b>) as a potential\nbest in class THR-β agonist. The high metabolic stability and\ngood permeability translated well in vivo to afford a long in vivo\nhalf-life pharmacokinetic profile with limited liability for DDI,\nand it overcomes certain drawbacks seen in recent clinical candidates.

Publication Details

Journal
Figshare
Published
2024-09-02
DOI
https://doi.org/10.1021/acs.jmedchem.4c01029.s001
Primary Topic
Botanical Research and Chemistry
Type
article
Field-Weighted Citation Impact
0.00
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article

Discovery and\nPreclinical Profile of ALG-055009, a\nPotent and Selective Thyroid Hormone Receptor Beta (THR-β) Agonist\nfor the Treatment of MASH

Figshare
Botanical Research and Chemistry
article

Discovery and\nPreclinical Profile of ALG-055009, a\nPotent and Selective Thyroid Hormone Receptor Beta (THR-β) Agonist\nfor the Treatment of MASH

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Abstract

Agonists of thyroid hormone receptor\nβ (THR-β)\ndecreased\nLDL cholesterol (LDL-C) and triglyceride (TG) levels in human clinical\ntrials for patients with dyslipidemia. The authors present the highly\npotent and selective compound ALG-055009 (<b>14</b>) as a potential\nbest in class THR-β agonist. The high metabolic stability and\ngood permeability translated well in vivo to afford a long in vivo\nhalf-life pharmacokinetic profile with limited liability for DDI,\nand it overcomes certain drawbacks seen in recent clinical candidates.

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Openalex Percentile: Top 47%
Botanical Research and Chemistry
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Discovery and\nPreclinical Profile of ALG-055009, a\nPotent and Selective Thyroid Hormone Receptor Beta (THR-β) Agonist\nfor the Treatment of MASH · Figshare (2024) | TGRS Research Map | TGRS