化学
兴奋剂
体内
药理学
药代动力学
血脂异常
甲状腺激素受体
代谢稳定性
甘油三酯
受体
内分泌学
内科学
体外
胆固醇
生物化学
医学
疾病
生物
生物技术
作者
Koen Vandyck,David C. McGowan,Xuan G. Luong,Sarah Stevens,Andreas Jekle,Kusum Gupta,Dinah Misner,Sushmita Chanda,Vladimir Serebryany,Michael J. Welch,Hai Hu,Zengpeng Lv,Caroline Williams,K. Maskos,Alfred Lammens,Antitsa Stoycheva,Tse–I Lin,Lawrence M. Blatt,Leonid N. Beigelman,Julian Symons,Pierre Raboisson,Jérôme Deval
标识
DOI:10.1021/acs.jmedchem.4c01029
摘要
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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