2. Academic Validation
  3. Discovery and Preclinical Profile of ALG-055009, a Potent and Selective Thyroid Hormone Receptor Beta (THR-β) Agonist for the Treatment of MASH

Discovery and Preclinical Profile of ALG-055009, a Potent and Selective Thyroid Hormone Receptor Beta (THR-β) Agonist for the Treatment of MASH

  • J Med Chem. 2024 Sep 12;67(17):14840-14851. doi: 10.1021/acs.jmedchem.4c01029.
Koen Vandyck 1,  David C McGowan 1,  Xuan G Luong 2,  Sarah K Stevens 2,  Andreas Jekle 2,  Kusum Gupta 2,  Dinah L Misner 2,  Sushmita Chanda 2,  Vladimir Serebryany 2,  Michael Welch 2,  Haiyang Hu 3,  Zhidan Lv 3,  Caroline Williams 2,  Klaus Maskos 4,  Alfred Lammens 4,  Antitsa D Stoycheva 2,  Tse-I Lin 1,  Lawrence M Blatt 2,  Leonid N Beigelman 2,  Julian A Symons 2,  Pierre Raboisson 2,  Jerome Deval 2
Affiliations

Affiliations

  • 1 Aligos Belgium BV, Gaston Geenslaan 1, 3001 Leuven, Belgium.
  • 2 Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • 3 Pharmaron, 6 Taihe Road, BDA, Beijing, 100176, P. R. China.
  • 4 Proteros Biostructures GmbH, Bunsenstraße 7a, 82152 Planegg-Martinsried, Germany.
PMID: 39221768 DOI: 10.1021/acs.jmedchem.4c01029
Abstract

Agonists of Thyroid Hormone Receptor β (THR-β) decreased LDL Cholesterol (LDL-C) and triglyceride (TG) levels in human clinical trials for patients with dyslipidemia. The authors present the highly potent and selective compound ALG-055009 (14) as a potential best in class THR-β agonist. The high metabolic stability and good permeability translated well in vivo to afford a long in vivo half-life pharmacokinetic profile with limited liability for DDI, and it overcomes certain drawbacks seen in recent clinical candidates.

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