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Pharmacology and chemistry of adapalene
Abstract
Background Retinoid research in the field of dermatology has been influenced by the clinical success of topical tretinoin and oral isotretinoin in the treatment of acne, and by the discovery of high-affinity binding proteins for retinoic acid mediating its action and interaction with other vitamins and hormones.Objective We sought molecules with an optimal balance between stability, efficacy, and local tolerance for topical acne therapy.Methods In vitro and in vivo bioassay systems were used to test the ability of retinoids to modulate cell proliferation and differentiation. In addition, antiinflammatory properties were assessed. Binding and transactivation assays were used to compare affinities and transcriptional activities of adapalene and tretinoin for the nuclear transcription factors, retinoic acid receptors (RARs).Results and conclusion Adapalene is a stable naphthoic acid derivative with potent retinoid pharmacology, controlling cell proliferation and differentiation. In addition it has significant antiinflammatory action. The nuclear gene transcription factors RAR beta and RAR gamma mediate the retinoid activity of adapalene.
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“Adapalene—a third-generation retinoid that modulates cellular keratinization, differentiation, and proliferation [8, 18]—has the advantage of being one of the most tolerable retinoids [19] that also retains its stability in the presence of BPO [9].”
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Successful Treatment with Adapalene for EGFR-TKI-induced Acneiform Eruptions
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Retinoid Receptor-Selective Agonists and Their Action in Skin
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Self-citationMultidimensional role of adapalene in regulating cell death in multiple myeloma
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Mechanism of action of adapalene for treating EGFR‐TKI ‐induced skin disorder
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Metadata
- Authors
- Shroot, B., & Michel, S.
- Affiliations
- Galderma (France) (FR)
- ORCID
- Shroot, Braham
- Venue
- Journal of the American Academy of Dermatology
- Publisher
- Elsevier BV
- Published
- 1997-06
- Volume
- 36
- Issue
- 6
- Pages
- S96-S103
- ISSN
- 0190-9622 (ISSN-L)
- OpenAlex
- W2144493708
- Cited by
- 140
- References
- 13
- Citations by year
- 2026: 5 · 2025: 5 · 2024: 8 · 2023: 2 · 2022: 2 · 2021: 7 · 2020: 6 · 2019: 5 · 2018: 2 · 2017: 1 · 2016: 8 · 2015: 4 · 2014: 13 · 2013: 6
- FWCI
- 8.19
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of the American Academy of Dermatology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Dermatology › Acne and Rosacea Treatments and Effects
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Retinoids in leukemia and cellular processes
- Health Sciences › Medicine › Dermatology › Dermatology and Skin Diseases
- Keywords
- adapalene, retinoids, acne treatment, topical retinoids, retinoic acid receptor, RARβ, RARγ, naphthoic acid derivatives, cell proliferation, cell differentiation, anti-inflammatory activity, all-trans retinoic acid, drug stability
- MeSH terms
- Adapalene, Administration, Topical, Animals, Anti-Inflammatory Agents, Non-Steroidal, Cell Differentiation, Cell Division, Cells, Cultured, HeLa Cells, Humans, Naphthalenes, Skin, Signal Transduction, Gene Expression
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