Pharmacology and chemistry of adapalene

Shroot, Braham; Michel, Serge

doi:10.1016/s0190-9622(97)70050-1

Cited by 140Acne and Rosacea Treatments and EffectsRetinoids in leukemia and cellular processesDermatology and Skin Diseases

Pharmacology and chemistry of adapalene

Shroot, Braham, Michel, Serge·1997·Journal of the American Academy of Dermatology

DOI 10.1016/s0190-9622(97)70050-1

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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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From Efficacy and safety of a fixed-dose clindamycin phosphate 1.2%, benzoyl peroxide 3.1%, and adapalene 0.15% gel for moderate-to-severe acne: a randomized phase II study of the first triple-combination drug (2022) · cites this paper as [18]

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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)
DOI: 10.1016/s0190-9622(97)70050-1
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
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
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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