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Rezdiffra™ (resmetirom): a THR-β agonist for non-alcoholic steatohepatitis.

作者信息

Brisnovali Niki F, Haney Connor, Goedeke Leigh

机构信息

Department of Medicine (Cardiology), Cardiovascular Research Institute, Icahn School of Medicine at Mount Sinai, New York, NY, USA.

Department of Medicine (Cardiology), Cardiovascular Research Institute, Icahn School of Medicine at Mount Sinai, New York, NY, USA; Department of Medicine (Endocrinology), Diabetes, Obesity, and Metabolism Institute, Icahn School of Medicine at Mount Sinai, New York, NY, USA.

出版信息

Trends Pharmacol Sci. 2024 Nov;45(11):1081-1082. doi: 10.1016/j.tips.2024.08.009. Epub 2024 Sep 19.

DOI:10.1016/j.tips.2024.08.009
PMID:39304473
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11560534/
Abstract
摘要

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Rezdiffra™ (resmetirom): a THR-β agonist for non-alcoholic steatohepatitis.瑞兹迪弗拉™（雷斯美替罗姆）：一种用于非酒精性脂肪性肝炎的甲状腺激素受体-β激动剂。
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2
Budget impact of resmetirom for the treatment of adults with non-cirrhotic non-alcoholic steatohepatitis (NASH) with moderate to advanced liver fibrosis (consistent with stages F2 to F3 fibrosis).治疗伴有中度至进展性肝纤维化（符合 F2 至 F3 纤维化阶段）的非肝硬化非酒精性脂肪性肝炎（NASH）成人患者的雷美替胺的预算影响。
J Med Econ. 2024 Jan-Dec;27(1):1108-1118. doi: 10.1080/13696998.2024.2393952. Epub 2024 Aug 22.
3
Resmetirom's approval: Highlighting the need for comprehensive approaches in NASH therapeutics.雷美替胺获批：凸显 NASH 治疗中全面方法的必要性。
Clin Res Hepatol Gastroenterol. 2024 Aug;48(7):102377. doi: 10.1016/j.clinre.2024.102377. Epub 2024 May 19.
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Resmetirom: First Approval.雷美替胺：首次获批
Drugs. 2024 Jun;84(6):729-735. doi: 10.1007/s40265-024-02045-0. Epub 2024 May 21.
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Resmetirom (Rezdiffra) for metabolic dysfunction-associated steatohepatitis.用于治疗代谢功能障碍相关脂肪性肝炎的雷斯美洛（Rezdiffra）
Med Lett Drugs Ther. 2024 Apr 29;66(1701):65-66. doi: 10.58347/tml.2024.1701a.
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Resmetirom: An Orally Administered, Smallmolecule, Liver-directed, β-selective THR Agonist for the Treatment of Non-alcoholic Fatty Liver Disease and Non-alcoholic Steatohepatitis.瑞美替隆：一种口服的小分子、肝脏靶向、β 选择性甲状腺激素受体激动剂，用于治疗非酒精性脂肪性肝病和非酒精性脂肪性肝炎。
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Estimation of the Eligible Population For Resmetirom Among Adults in the United States for Treatment of Non-Cirrhotic NASH with Moderate-to-Advanced Liver Fibrosis.在美国，为治疗非肝硬化性 NASH 伴中重度肝纤维化的成年人，估算有资格使用雷美替胺的人群。
Adv Ther. 2024 Nov;41(11):4172-4190. doi: 10.1007/s12325-024-02989-5. Epub 2024 Sep 18.
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Resmetirom (Rezdiffra) for the Treatment of Noncirrhotic Nonalcoholic Steatohepatitis With Moderate to Advanced Fibrosis.雷斯美洛（Rezdiffra）用于治疗伴有中度至重度纤维化的非肝硬化非酒精性脂肪性肝炎。
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Activation of thyroid hormone receptor-β improved disease activity and metabolism independent of body weight in a mouse model of non-alcoholic steatohepatitis and fibrosis.甲状腺激素受体-β 的激活可改善非酒精性脂肪性肝炎和肝纤维化小鼠模型的疾病活动度和代谢，而不依赖于体重。
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Ann Med Surg (Lond). 2024 Jul 15;86(9):5447-5454. doi: 10.1097/MS9.0000000000002314. eCollection 2024 Sep.

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Flavone C-Glycosides from L. Attenuate Metabolic Dysfunction-Associated Steatotic Liver Disease (MASLD) via Multi-Pathway Regulations.来自[植物名称]的黄酮碳苷通过多途径调节减轻代谢功能障碍相关脂肪性肝病（MASLD）
Nutrients. 2025 Jul 28;17(15):2456. doi: 10.3390/nu17152456.
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Game Changers: Blockbuster Small-Molecule Drugs Approved by the FDA in 2024.变革者：2024年获美国食品药品监督管理局批准的重磅小分子药物
Pharmaceuticals (Basel). 2025 May 15;18(5):729. doi: 10.3390/ph18050729.
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In Situ Assembly of Fluorogenic RNA for Screening Natural Anti-Liver Fibrosis Products via Dynamic Visualization of COL1A1 mRNA.用于通过COL1A1 mRNA动态可视化筛选天然抗肝纤维化产品的荧光RNA原位组装
Adv Sci (Weinh). 2025 Aug;12(30):e02850. doi: 10.1002/advs.202502850. Epub 2025 May 23.
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Drug Pipeline for MASLD: What Can Be Learned from the Successful Story of Resmetirom.非酒精性脂肪性肝炎的药物研发管线：从瑞美鲁肽的成功案例中能学到什么。
Curr Issues Mol Biol. 2025 Feb 27;47(3):154. doi: 10.3390/cimb47030154.
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Dapansutrile Regulates Mitochondrial Oxidative Stress and Reduces Hepatic Lipid Accumulation in Diabetic Mice.达泮苏曲尔调节糖尿病小鼠的线粒体氧化应激并减少肝脏脂质积累。
Curr Issues Mol Biol. 2025 Feb 25;47(3):148. doi: 10.3390/cimb47030148.

本文引用的文献

1
Resmetirom: First Approval.雷美替胺：首次获批
Drugs. 2024 Jun;84(6):729-735. doi: 10.1007/s40265-024-02045-0. Epub 2024 May 21.
2
Metabolic Messengers: Thyroid Hormones.代谢信使：甲状腺激素。
Nat Metab. 2024 Apr;6(4):639-650. doi: 10.1038/s42255-024-00986-0. Epub 2024 Apr 26.
3
New and emerging treatments for metabolic dysfunction-associated steatohepatitis.代谢功能障碍相关脂肪性肝炎的新型及新兴治疗方法。
Cell Metab. 2024 Jun 4;36(6):1430. doi: 10.1016/j.cmet.2024.04.016. Epub 2024 Apr 25.
4
A Phase 3, Randomized, Controlled Trial of Resmetirom in NASH with Liver Fibrosis.一项评估 Resmetirom 治疗伴有肝纤维化的 NASH 的 3 期随机对照试验。
N Engl J Med. 2024 Feb 8;390(6):497-509. doi: 10.1056/NEJMoa2309000.
5
Resmetirom for nonalcoholic fatty liver disease: a randomized, double-blind, placebo-controlled phase 3 trial.雷美替胺治疗非酒精性脂肪性肝病：一项随机、双盲、安慰剂对照的 3 期临床试验。
Nat Med. 2023 Nov;29(11):2919-2928. doi: 10.1038/s41591-023-02603-1. Epub 2023 Oct 16.
6
Cell-Specific Transport and Thyroid Hormone Receptor Isoform Selectivity Account for Hepatocyte-Targeted Thyromimetic Action of MGL-3196.细胞特异性转运和甲状腺激素受体同工型选择性解释了 MGL-3196 对肝细胞的拟甲状腺作用。
Int J Mol Sci. 2022 Nov 8;23(22):13714. doi: 10.3390/ijms232213714.
7
Regulation of gene transcription by thyroid hormone receptor β agonists in clinical development for the treatment of non-alcoholic steatohepatitis (NASH).甲状腺激素受体 β 激动剂在治疗非酒精性脂肪性肝炎（NASH）的临床开发中对基因转录的调控。
PLoS One. 2020 Dec 11;15(12):e0240338. doi: 10.1371/journal.pone.0240338. eCollection 2020.
8
Thyroid Hormone Signaling and the Liver.甲状腺激素信号转导与肝脏
Hepatology. 2020 Aug;72(2):742-752. doi: 10.1002/hep.31296.
9
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dyslipidemia.2-[3,5-二氯-4-(5-异丙基-6-氧代-1,6-二氢哒嗪-3-基氧基)苯基]-3,5-二氧代-2,3,4,5-四氢[1,2,4]三嗪-6-腈（MGL-3196）的发现，一种在治疗血脂异常的临床试验中具有高度选择性的甲状腺激素受体β激动剂。
J Med Chem. 2014 May 22;57(10):3912-23. doi: 10.1021/jm4019299. Epub 2014 Apr 8.