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Ketotifen

Ketotifen

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Substance Overview and History

Ketotifen, a mast cell stabilizer and H1 receptor antagonist, has shown potential as an anti-fibrotic agent by directly targeting fibroblasts, the key cells driving fibrosis. In studies involving human dermal fibroblasts, ketotifen reduced the effects of transforming growth factor-β1 (TGFβ1), including α-smooth muscle actin (αSMA) expression and cytoskeletal proteins linked to fibrosis. It also inhibited fibroblast contractility and mechano-transduction pathways such as Yes-associated protein (YAP) and transcriptional coactivator with PDZ-binding motif (TAZ), disrupting the processes responsible for excessive extracellular matrix deposition.

References:

Leong, E., Al-Bitar, H., Marshall, J.S., & Bezuhly, M. (2024) 'Sci Rep', Scientific Reports

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FAQ
What is Ketotifen?
Ketotifen is a mast cell stabilizer and H1 receptor antagonist commonly used to treat allergies and inflammatory conditions.
References:

Leong, E., Al-Bitar, H., Marshall, J.S., & Bezuhly, M. (2024) 'Sci Rep', Scientific Reports

How is Ketotifen linked to fibrosis treatment?
Ketotifen has demonstrated anti-fibrotic properties by directly targeting fibroblasts, reducing pro-fibrotic markers, and suppressing fibroblast contractility.
References:

Leong, E., Al-Bitar, H., Marshall, J.S., & Bezuhly, M. (2024) 'Sci Rep', Scientific Reports

What are fibroblasts, and why are they important in fibrosis?
Fibroblasts are cells responsible for producing extracellular matrix components like collagen. Dysregulated fibroblasts contribute to excessive tissue scarring in fibrosis.
References:

Leong, E., Al-Bitar, H., Marshall, J.S., & Bezuhly, M. (2024) 'Sci Rep', Scientific Reports