Dissecting fibrosis: therapeutic insights from the small-molecule toolbox
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Updated: Apr 4, 2026
Human Dupuytren's Ex Vivo Culture for the Study of Myofibroblasts and Extracellular Matrix Interactions
Published on: April 18, 2015
Carmel B Nanthakumar1, Richard J D Hatley1, Seble Lemma2
1Fibrosis Discovery Performance Unit, Medicines Research Centre, GlaxoSmithKline, Stevenage, SG1 2NY, UK.
Abstract:
Fibrosis, which leads to progressive loss of tissue function and eventual organ failure, has been estimated to contribute to ~45% of deaths in the developed world, and so new therapeutics to modulate fibrosis are urgently needed. Major advances in our understanding of the mechanisms underlying pathological fibrosis are supporting the search for such therapeutics, and the recent approval of two anti-fibrotic drugs for idiopathic pulmonary fibrosis has demonstrated the tractability of this area for drug discovery. This Review examines the pharmacology and structural information for small molecules being evaluated for lung, liver, kidney and skin fibrosis. In particular, we discuss the insights gained from the use of these pharmacological tools, and how these entities can inform, and probe, emerging insights into disease mechanisms, including the potential for future drug combinations.
Insights
New anti-fibrotic drugs are urgently needed as fibrosis contributes to nearly half of all deaths. This review examines small molecules for treating lung, liver, kidney, and skin fibrosis, offering insights for future drug discovery.
Area of Science:
- Pharmacology
- Drug Discovery
- Fibrosis Research
Background:
- Fibrosis causes progressive tissue dysfunction and organ failure, contributing to approximately 45% of deaths in developed nations.
- Significant advancements in understanding fibrotic mechanisms are paving the way for novel therapeutic strategies.
- Recent approvals of anti-fibrotic drugs for idiopathic pulmonary fibrosis highlight the potential for drug development in this field.
Purpose of the Study:
- To review the pharmacology and structural data of small molecules currently under evaluation for treating various fibrotic conditions.
- To explore how pharmacological tools inform and investigate emerging disease mechanisms in fibrosis.
- To discuss the potential for developing future combination therapies for fibrosis.
Main Methods:
- Literature review of pharmacological and structural information on small molecule therapeutics.
- Analysis of drug candidates targeting fibrosis in lung, liver, kidney, and skin.
- Synthesis of insights from current therapeutic approaches to inform future research.
Main Results:
- Identification and examination of key small molecules being developed for fibrotic diseases.
- Discussion of structure-activity relationships and pharmacological profiles of anti-fibrotic agents.
- Highlighting the utility of pharmacological tools in probing disease mechanisms.
Conclusions:
- Small molecules represent a promising avenue for developing new anti-fibrotic therapeutics.
- Understanding drug pharmacology and structure is crucial for effective fibrosis treatment.
- Emerging insights suggest potential for combination therapies to enhance treatment efficacy.
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