ArticleDrugs in R&D2019
Apremilast Normalizes Gene Expression of Inflammatory Mediators in Human Keratinocytes and Reduces Antigen-Induced Atopic Dermatitis in Mice.
Article in Drugs in R&D, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers, 1 of them a synthesis that pooled it.
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Who cites it
16 citing papers in PubMed, 1 synthesis or guideline pooled it, 31 citations in OpenAlex.
- A systematic review of novel Phosphodiesterase-4 inhibitors in the treatment of psoriasis.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2025Pooled it
- A phase IIb single-center study to assess the efficacy of apremilast for the treatment of nummular eczema.Journal der Deutschen Dermatologischen Gesellschaft = Journal of the German Society of Dermatology : JDDG · 2025Trial
- Balancing efficacy and hepatotoxicity: a comprehensive review of oral medications in psoriasis management.Naunyn-Schmiedeberg's archives of pharmacology · 2025Review
- Cyclic nucleotide phosphodiesterases as drug targets.Pharmacological reviews · 2025Review
- Apremilast treatment of immune-mediated inflammatory skin diseases: a narrative review.Frontiers in pharmacology · 2025Review
- Th Pathways in Immune-Mediated Skin Disorders: A Guide for Strategic Treatment Decisions.Immune network · 2024Review
- Phosphodiesterase 4 is overexpressed in keloid epidermal scars and its inhibition reduces keratinocyte fibrotic alterations.Molecular medicine (Cambridge, Mass.) · 2024Article
- Difamilast, a Topical Phosphodiesterase 4 Inhibitor, Produces Soluble ST2 via the AHR-NRF2 Axis in Human Keratinocytes.International journal of molecular sciences · 2024Article
- Novel Therapeutic Targets for the Treatment of Atopic Dermatitis.Biomedicines · 2023Review
- IL-20 promotes cutaneous inflammation and peripheral itch sensation in atopic dermatitis.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2022Article
- Regulatory T Cells: Therapeutic Opportunities in Uveitis.Frontiers in ophthalmology · 2022Review
- The Keratinocyte as a Crucial Cell in the Predisposition, Onset, Progression, Therapy and Study of the Atopic Dermatitis.International journal of molecular sciences · 2021Review
- Quantitative Image Analysis for Tissue Biomarker Use: A White Paper From the Digital Pathology Association.Applied immunohistochemistry & molecular morphology : AIMM · 2021Article
- Apremilast prevents IL‑17‑induced cellular senescence in ATDC5 chondrocytes mediated by SIRT1.International journal of molecular medicine · 2021Article
- Experimental Pharmacological Management of Psoriasis.Journal of experimental pharmacology · 2021Review
- Apremilast Regulates the Teff/Treg Balance to Ameliorate UveitisFrontiers in immunology · 2020Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundApremilast, an oral phosphodiesterase (PDE) 4 inhibitor, has demonstrated efficacy in psoriasis, while its efficacy in atopic dermatitis (AD) was found to be modest. AD is a chronic inflammatory skin disease associated with activation of T helper (Th) 2 and Th17 immunity and a compromised epidermal barrier.
objectiveThe objectives of this study were to examine the expression of PDE4 isoforms in skin from healthy subjects and AD patients, and to determine the effects of apremilast on AD-related inflammatory markers in vitro and in murine models of AD.
methodsThe expression of PDE4 isoforms (A, B, C, and D) in skin biopsies from healthy subjects and AD patients was evaluated using immunohistochemistry and digital image analysis. Using quantitative real-time reverse-transcriptase polymerase chain reaction, we evaluated the effects of apremilast on gene expression in adult human epidermal keratinocytes (HEKa) stimulated by Th2 and Th17 cytokines, and in two mouse models of antigen-induced AD.
resultsExpression of PDE4 isoforms increased up to three-fold in the epidermis of AD patients versus healthy skin. In interleukin (IL)-4 and IL-17-stimulated HEKa cells, apremilast significantly changed the expression of ILs, including IL-12/IL-23p40 and IL-31, and alarmins S100A7, S100A8, and S100A12. In mouse models of AD, apremilast significantly reduced ear swelling and monocyte chemoattractant protein-1 expression.
conclusionPDE4 is overexpressed in AD skin compared with normal skin, and inflammatory gene expression by human keratinocytes and mouse dermatitis can be modulated by apremilast.
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