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Discovery and Preclinical Profile of ALG-055009, a Potent and Selective Thyroid Hormone Receptor Beta (THR-ß) Agonist for the Treatment of MASH.
Vandyck, Koen; McGowan, David C; Luong, Xuan G; Stevens, Sarah K; Jekle, Andreas; Gupta, Kusum; Misner, Dinah L; Chanda, Sushmita; Serebryany, Vladimir; Welch, Michael; Hu, Haiyang; Lv, Zhidan; Williams, Caroline; Maskos, Klaus; Lammens, Alfred; Stoycheva, Antitsa D; Lin, Tse-I; Blatt, Lawrence M; Beigelman, Leonid N; Symons, Julian A; Raboisson, Pierre; Deval, Jerome.
Afiliación
  • Vandyck K; Aligos Belgium BV, Gaston Geenslaan 1, 3001 Leuven, Belgium.
  • McGowan DC; Aligos Belgium BV, Gaston Geenslaan 1, 3001 Leuven, Belgium.
  • Luong XG; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • Stevens SK; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • Jekle A; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • Gupta K; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • Misner DL; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • Chanda S; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • Serebryany V; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • Welch M; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • Hu H; Pharmaron, 6 Taihe Road, BDA, Beijing, 100176, P. R. China.
  • Lv Z; Pharmaron, 6 Taihe Road, BDA, Beijing, 100176, P. R. China.
  • Williams C; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • Maskos K; Proteros Biostructures GmbH, Bunsenstraße 7a, 82152 Planegg-Martinsried, Germany.
  • Lammens A; Proteros Biostructures GmbH, Bunsenstraße 7a, 82152 Planegg-Martinsried, Germany.
  • Stoycheva AD; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • Lin TI; Aligos Belgium BV, Gaston Geenslaan 1, 3001 Leuven, Belgium.
  • Blatt LM; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • Beigelman LN; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • Symons JA; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • Raboisson P; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
  • Deval J; Aligos Therapeutics, Incorporated, 1 Corporate Drive, South San Francisco, California 94080, United States.
J Med Chem ; 67(17): 14840-14851, 2024 Sep 12.
Article en En | MEDLINE | ID: mdl-39221768
ABSTRACT
Agonists of thyroid hormone receptor ß (THR-ß) 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-ß 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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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Receptores beta de Hormona Tiroidea Límite: Animals / Humans / Male Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Bélgica
Texto completo
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Receptores beta de Hormona Tiroidea Límite: Animals / Humans / Male Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Bélgica