Resmetirom: First Approval

Keam, Susan J.

doi:10.1007/s40265-024-02045-0

Cited by 31 publications

(1 citation statement)

References 15 publications

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“…The prevalence of metabolic dysfunction-associated steatotic liver disease (MASLD) [ 1 ] continues to rise with the increasing obesity epidemic [ 2 ]. Rezdiffra is the only Food and Drug Administration (FDA) approved therapy and works as an activator of a thyroid hormone receptor-beta which partially decreases steatosis [ 3 ]. As such, there is a critical need to improve our understanding of gene expression regulation and signaling transduction in MASLD to develop new therapies.…”

Section: Introductionmentioning

confidence: 99%

Liver matrin-3 protects mice against hepatic steatosis and stress response via constitutive androstane receptor

Cheng,

Baki,

Moran

et al. 2024

Molecular Metabolism

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Section: Introductionmentioning

confidence: 99%

Liver matrin-3 protects mice against hepatic steatosis and stress response via constitutive androstane receptor

Cheng,

Baki,

Moran

et al. 2024

Molecular Metabolism

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Design and Synthesis of Dual Galectin‐3 and EGFR Inhibitors Against Liver Fibrosis

Liu,

He,

Jin

et al. 2024

Chemistry An Asian Journal

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Liver fibrosis, mainly arising from chronic viral or metabolic liver diseases, is a significant global health concern. There is currently only one FDA‐approved drug (Resmetirom) in the market to combat liver fibrosis. Both galectin‐3 and epidermal growth factor receptor (EGFR) play important roles in liver fibrosis, while galectin‐3 may interact with EGFR. Galectin‐3 inhibitors, typically lactose or galactose derivatives may inhibit liver fibrosis. We hypothesized that targeting both galectin‐3 and EGFR may have better effect against liver fibrosis. Here, EGFR inhibitor erlotinib was used in a series of designed galectin‐3 inhibitors after hybridization with the pharmacophore structure in reported galectin‐3 inhibitors to impede hepatic stellate cells (HSCs) activation by a typical method of click chemistry. Bioactivity test results showed that compound 29 suppressed TGF‐β‐induced upregulation of fibrotic markers (α‐SMA, fibronectin‐1, and collagen I). The preferred compound 29 displayed better binding to galectin‐3 (KD = 52.29 μM) and EGFR protein (KD = 3.31 μM) by SPR assay. Further docking studies were performed to clarify the possible binding mode of compound 29 with galectin‐3 and EGFR. Taken together, these results suggested that compound 29 could be a potential dual galectin‐3 and EGFR inhibitor as leading compound for anti‐liver fibrosis new drug development.

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Hepatocellular Interactions of Potential Nutraceuticals in the Management of Inflammatory NAFLD

Ezhilarasan,

Langeswaran

2024

Cell Biochemistry & Function

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Numerous studies highlight the potential of natural antioxidants, such as those found in foods and plants, to prevent or treat nonalcoholic fatty liver disease (NAFLD). Inflammation is a key factor in the progression from high‐fat diet‐induced NAFLD to nonalcoholic steatohepatitis (NASH). Injured liver cells and immune cells release inflammatory cytokines, activating hepatic stellate cells. These cells acquire a profibrogenic phenotype, leading to extracellular matrix accumulation and fibrosis. Persistent fibrosis can progress to cirrhosis. Fatty infiltration, oxidative stress, and inflammation exacerbate fatty liver diseases. Thus, many plant‐derived antioxidants, like silymarin, silibinin, curcumin, resveratrol, berberine, and quercetin, have been extensively studied in experimental models and clinical patients with NAFLD. Experimentally, these compounds have shown beneficial effects in reducing lipid accumulation, oxidative stress, and inflammatory markers by modulating the ERK, NF‐κB, AMPKα, and PPARγ pathways. They also help decrease metabolic endotoxemia, intestinal permeability, and gut inflammation. Clinically, silymarin and silibinin have been found to reduce transaminase levels, while resveratrol and curcumin help alleviate inflammation in NAFLD patients. However, these phytocompounds exhibit poor water solubility, leading to low oral bioavailability and hindering their biological efficacy. Additionally, inconclusive clinical results highlight the need for further trials with larger populations, longer durations, and standardized protocols.

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Resmetirom: First Approval

Cited by 31 publications

References 15 publications

Liver matrin-3 protects mice against hepatic steatosis and stress response via constitutive androstane receptor

Liver matrin-3 protects mice against hepatic steatosis and stress response via constitutive androstane receptor

Design and Synthesis of Dual Galectin‐3 and EGFR Inhibitors Against Liver Fibrosis

Hepatocellular Interactions of Potential Nutraceuticals in the Management of Inflammatory NAFLD

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