ArticleProceedings of the National Academy of Sciences of the United States of America2017
Small molecule-mediated inhibition of myofibroblast transdifferentiation for the treatment of fibrosis.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 47 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
47 citing papers in PubMed, 84 citations in OpenAlex.
- Urinary proteomic signature of mineralocorticoid receptor antagonism by spironolactone: evidence from the HOMAGE trial.Heart (British Cardiac Society) · 2024Trial
- New approach methodologies: drug screening platform to identify antifibrotic compounds.Nature protocols · 2026Review
- Denoising single-cell RNA-seq data with a deep learning-embedded statistical framework.BMC bioinformatics · 2025Article
- The senescence-like activity of BMS-470539 is associated with anti-fibrotic actions in models of dermal fibrosis.Arthritis research & therapy · 2025Article
- PTEN Regulates Myofibroblast Activation in Valvular Interstitial Cells Based on Subcellular Localization.Advanced biology · 2025Article
- Ablation of LRP6 in alpha-smooth muscle actin-expressing cells abrogates lung inflammation and fibrosis upon bleomycin-induced lung injury.FEBS letters · 2025Article
- Article
- Inhalation of itraconazole mitigates bleomycin-induced lung fibrosis via regulating SPP1 and C3 signaling pathway pivotal in the interaction between phagocytic macrophages and diseased fibroblasts.Journal of translational medicine · 2024Article
- Synthesis at the Interface of Chemistry and Biology.Accounts of chemical research · 2024Review
- Bioactive materials forBioactive materials · 2024Review
- Hedgehog signaling is a promising target for the treatment of hepatic fibrogenesis: a new management strategy using itraconazole-loaded nanoparticles.Frontiers in pharmacology · 2024Article
- MARCH8 downregulation modulates profibrotic responses including myofibroblast differentiation.American journal of physiology. Cell physiology · 2023Article
- Injectable, Drug-Eluting Nanocrystals Prevent Fibrosis and Stricture Formation In Vivo.Gastroenterology · 2023Article
- Experimental Workflow for Preclinical Studies of Human Antifibrotic Therapies.Methods in molecular biology (Clifton, N.J.) · 2023Article
- Editorial: Fibrotic tissue remodeling as a driver of disease pathogenesis.Frontiers in molecular biosciences · 2023Article
- Inhibition of 11β-hydroxysteroid dehydrogenase 1 relieves fibrosis through depolarizing of hepatic stellate cell in NASH.Cell death & disease · 2022Article
- Predictive performance and clinical application of COV50, a urinary proteomic biomarker in early COVID-19 infection: a prospective multicentre cohort study.The Lancet. Digital health · 2022Article
- Inhibition of the cardiac fibroblast-enriched histone methyltransferase Dot1L prevents cardiac fibrosis and cardiac dysfunction.Cell & bioscience · 2022Article
- Prevention of bleomycin-induced pulmonary fibrosis by a RANKL peptide in mice.Scientific reports · 2022Article
- Dysregulated myosin in Hermansky-Pudlak syndrome lung fibroblasts is associated with increased cell motility.Respiratory research · 2022Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Fibrosis, a disease in which excessive amounts of connective tissue accumulate in response to physical damage and/or inflammatory insult, affects nearly every tissue in the body and can progress to a state of organ malfunction and death. A hallmark of fibrotic disease is the excessive accumulation of extracellular matrix-secreting activated myofibroblasts (MFBs) in place of functional parenchymal cells. As such, the identification of agents that selectively inhibit the transdifferentiation process leading to the formation of MFBs represents an attractive approach for the treatment of diverse fibrosis-related diseases. Herein we report the development of a high throughput image-based screen using primary hepatic stellate cells that identified the antifungal drug itraconazole (ITA) as an inhibitor of MFB cell fate in resident fibroblasts derived from multiple murine and human tissues (i.e., lung, liver, heart, and skin). Chemical optimization of ITA led to a molecule (CBR-096-4) devoid of antifungal and human cytochrome P450 inhibitory activity with excellent pharmacokinetics, safety, and efficacy in rodent models of lung, liver, and skin fibrosis. These findings may serve to provide a strategy for the safe and effective treatment of a broad range of fibrosis-related diseases.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.