Download MendeleyDiscovery and Preclinical Profile of ALG-055009, a Potent and Selective Thyroid Hormone Receptor Beta (THR-beta ) Agonist for the Treatment of MASH.
Vandyck, K., McGowan, D.C., Luong, X.G., Stevens, S.K., Jekle, A., Gupta, K., Misner, D.L., Chanda, S., Serebryany, V., Welch, M., Hu, H., Lv, Z., Williams, C., Maskos, K., Lammens, A., Stoycheva, A.D., Lin, T.I., Blatt, L.M., Beigelman, L.N., Symons, J.A., Raboisson, P., Deval, J.(2024) J Med Chem 67: 14840-14851
- PubMed: 39221768
- DOI: https://doi.org/10.1021/acs.jmedchem.4c01029
- Primary Citation of Related Structures:
8RQN, 8RQO - PubMed 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.
Organizational Affiliation:
Aligos Belgium BV, Gaston Geenslaan 1, 3001 Leuven, Belgium.
