针对MASLD的THR-β:机制和药物开发
Yunlong Hua1, Yang Liu2, Lianjun Xing3
1Institute of Digestive Diseases, Longhua Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai, 200032, People's Republic of China.
Drug design, development and therapy
|December 1, 2025
概括
与代谢功能障碍相关的脂肪性肝病 (MASLD) 是常见的,治疗方法很少. 甲状腺激素受体β (THR-β) 激动剂,如Resmetirom,通过向肝脏新陈代谢,对MASLD有希望,但需要进一步研究.
科学领域:
- 肝病学 肝病学是一种肝病学.
- 内分泌学 在内分泌学.
- 药理学 药理学是指药理学的学科.
背景情况:
- 与代谢功能障碍相关的脂肪性肝病 (MASLD) 是全球慢性肝病的主要原因,缺乏有效的治疗方法.
- 甲状腺激素 (TH) 和其受体THR-β是肝脏新陈代谢的关键调节剂,使THR-β成为MASLD的关键治疗点.
研究的目的:
- 审查MASLD中TH/THR-β的机制.
- 总结一下针对MASLD的THR-β向药物治疗的最新进展.
- 讨论THR-β激动剂在MASLD治疗中的治疗潜力和挑战.
主要方法:
- 关于甲状腺激素在肝脏中的作用研究的文献综述.
- 对MASLD中THR-β激动剂的临床前和临床数据的分析.
- 讨论疾病异质性和药物不良反应.
主要成果:
- THR-β激动剂在减少MASLD中的肝硬化,炎症和纤维化方面表现出有效性.
- 选择性THR-β激动剂Resmetirom在2024年获得了FDA的批准.
- 目前对其他THR-β激动剂的持续研究显示了治疗的前景.
结论:
- 针对THR-β的药物治疗代表了MASLD治疗的重大进展.
- 进一步全面评估临床疗效和安全性至关重要.
- 持续的研究对于优化药物开发和治疗MASLD的THR-β激动剂的临床应用至关重要.
相关概念视频
Transducer Mechanism: Enzyme-Linked Receptors
3.8K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Major types that are helpful drug targets include:
3.8K
Targeted Cancer Therapies
8.6K
The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
There are several types of targeted therapies against...
8.6K
Targets for Drug Action: Overview
10.0K
Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
10.0K
Therapeutic Drug Monitoring: Affecting Factors
182
Therapeutic Drug Monitoring (TDM) is the clinical practice of measuring specific drug levels in a patient's blood or body tissues to manage and optimize therapy. TDM is crucial for drugs with narrow therapeutic windows, like warfarin and phenytoin, where incorrect doses can lead to treatment failure or severe side effects. This monitoring ensures the dosage administered is within a safe and effective range. The factors affecting therapeutic drug monitoring include:Patient-Specific Factors:a.
182
Therapeutic Drug Monitoring: Overview and Classification
275
Therapeutic Drug Monitoring (TDM) is a clinical practice that measures specific drug levels in a patient's blood at designated intervals to ensure the drug concentration stays within a therapeutic range. This monitoring is crucial for optimizing individual dosage regimens, enhancing therapeutic efficacy, and minimizing drug-related toxicity. TDM is vital for drugs with narrow therapeutic windows, significant variability in pharmacokinetics, and a clear correlation between plasma levels and...
275
Therapeutic Drug Monitoring: Drug Analysis Methods
164
Therapeutic Drug Monitoring (TDM) is a clinical practice that measures specific drug levels in a patient's blood or body tissues to tailor drug therapy effectively. This monitoring is critical for managing drugs with narrow therapeutic indices like digoxin and phenytoin, ensuring they are both safe and effective. For instance, monitoring theophylline levels in asthma patients involves precision and sensitivity to adjust doses according to individual responses to therapy, ensuring efficacy and...
164


