Pharmacology of adapalene

  title={Pharmacology of adapalene},
  author={Michell and Jomard and D{\'e}marchez},
  journal={British Journal of Dermatology},
Adapalene, a synthetic retinoid, is a new drug proposed for the treatment of acne patients. Studies on the in vitro and in vivo pharmacology of adapalene have shown that it is very active on cell and tissue proliferation and differentiation. Furthermore, adapalene has anti‐inflammatory potential as determined by its anti‐AP1 activity. Adapalene interacts selectively with the nuclear receptors RARβ and RARγ, and its activity on proliferation and differentiation can be blocked by a RAR… 
Adapalene biochemistry and the evolution of a new topical retinoid for treatment of acne
The history of the development of adapalene, its unique physical and biochemical properties, and the pharmacological studies that demonstrate a wide range of retinoid‐receptor, genetic and anti‐inflammatory effects are reviewed, all of which contribute to the therapeutic efficacy and improved tolerability of adAPalene observed in the clinical use of this agent for the treatment of acne.
A Review on a Third Generation Retinoidal Agent: Adapalene
The present work reviews the biological and pharmaceutical profile of Adapalene and suggests that it may be an important target for pharmaceutical industries.
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  • Medicine, Biology
    The Journal of dermatological treatment
  • 2016
Abstract The central role of inflammation in acne is now more clearly understood. Adapalene, a third-generation topical retinoid, down-regulates toll-like receptor 2 expression and inhibits activator
Retinoid Therapy for Acne
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  • Medicine
    American journal of clinical dermatology
  • 2005
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In vitro modulation of TLR‐2, CD1d and IL‐10 by adapalene on normal human skin and acne inflammatory lesions
Abstract  The anti‐inflammatory mechanisms of adapalene, a synthetic retinoid used for the treatment of acne patients, are partially understood. They seem particularly related to the modulation of
The synthetic retinoid adapalene inhibits proliferation and induces apoptosis in colorectal cancer cells in vitro
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Adapalene 0.1% and benzoyl peroxide 2.5% combination gel for the treatment of acne vulgaris
Results from clinical trials provide robust evidence that this fixed-dose combination gel is significantly more efficacious than its corresponding monotherapies and has a mild tolerability profile similar to that of adapalene alone.
A comparative trial of two retinoids commonly used in the treatment of acne vulgaris
Both drugs have similar efficacy in the resolution of acne lesions but tretinoin gel microsphere may result in a faster onset of action in the reduction of comedones compared to adapalene.
The Effects of Topical Application of Adapalene and Tretinoin on Tissue Hydroxyproline Content in Wound Model Impaired by Corticosteroid
It is demonstrated that methyl prednisolon acetate significantly decreases the tissue hydroxyproline content of full-thickness wound in rats and topical application of adapalene and tretinoin appreciably reverses this inhibitory effect of corticosteroid.
Transdermal Penetration of Topical Drugs Used in the Treatment of Acne
Topical anti-acne agents are well tolerated and, as would be expected from their limited transdermal uptake, other significant safety concerns have not so far arisen.


Efficacy and safety comparison of adapalene (CD271) gel and tretinoin gel in the topical treatment of acne vulgaris. A European multicentre trial
A multicentre, investigator-masked, parallel-group study included 268 male and female patients with mild to moderate facial acne vulgaris and found that adapalene 0.1% gel with tretinoin 0.025% gel was effective in the treatment of acne patients.
Selective synthetic ligands for human nuclear retinoic acid receptors.
From a series of naphthalene and benzoic acid derivatives, synthetic retinoic acid analogues exhibiting high selectivity for the nuclear retinoIC acid receptors RAR alpha, RAR beta and RAR gamma are identified as well as ligands sharing high affinities for all RAR subtypes.
9-Cis retinoic acid stereoisomer binds and activates the nuclear receptor RXRα
The identification of a stereoisomer of retinoic acid, 9-cis retinol, which directly binds and activates RXRα, which suggests a new role for isomerization in the physiology of natural retinoids.
Differentiation of F9 embryonal carcinoma cells by synthetic retinoids: amplitude of plasminogen activator production does not depend on retinoid potency or affinity for F9 nuclear retinoic acid receptors.
It is shown that various retinoids differ, not only in terms of potency, i.e. the dilution at which they are active, but also in Terms of the amount of PA that they induce.
Characterization of three RXR genes that mediate the action of 9-cis retinoic acid.
Trans-activation analyses show that although all three RXRs respond to a variety of endogenous retinoids, 9-cis RA is their most potent ligand and is up to 40-fold more active than all-trans RA.
A decade of molecular biology of retinoic acid receptors
  • P. Chambon
  • Biology
    FASEB journal : official publication of the Federation of American Societies for Experimental Biology
  • 1996
A review of recent developments in structure‐ function relationships of retinoic acid receptors focuses on recent developments, particularly in the area of structure‐function relationships.
A human retinoic acid receptor which belongs to the family of nuclear receptors
The protein is homologous to the receptors for steroid hormones, thyroid hormones and vitamin D3, and appears to be a retinoic acid-inducible {Tans-acting enhancer factor, suggesting that the molecular mechanisms of the effect of vitamin A (vitamin A) on embryonic development, differentiation and tumour cell growth are similar to those described for other members of this nuclear receptor family.