Management of Acne Vulgaris With Trifarotene

Tan, Jerry; Chavda, Rajeev; Baldwin, Hilary; Dréno, Brigitte

doi:10.1177/12034754231163542

Cited by 9 publications

(4 citation statements)

References 29 publications

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“…The structure of the RARγ agonist CD437 and its binding to the receptor in the ligand binding pocket was used to design a drug candidate for treating acne. A new RARγ agonist CD5789 (trifarotene) has been identified [ 54 ]. Trifarotene combines the potency and selectivity of RARγ agonists.…”

Section: Targeting Of Therapies To Rarγ Agonismmentioning

confidence: 99%

“…Trifarotene combines the potency and selectivity of RARγ agonists. It received its first international approval for topical use to treat acne vulgaris in patients nine years and older [ 42 , 54 , 55 ].…”

Section: Targeting Of Therapies To Rarγ Agonismmentioning

confidence: 99%

“…These findings make CD437 a good prototype for new drugs that may be clinically more effective than ones with just one type of activity [48]. The structure of the RARγ agonist CD437 and its binding to the receptor in the ligand binding pocket was used to design a drug candidate for treating A new RARγ agonist CD5789 (trifarotene) has been identified [54]. Trifarotene combines the potency and selectivity of RARγ agonists.…”

Section: Cd437 a Selective Rarγ Agonistmentioning

confidence: 99%

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Molecular Interactions of Selective Agonists and Antagonists with the Retinoic Acid Receptor γ

Powała,

Żołek,

Brown

et al. 2024

IJMS

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All-trans retinoic acid (ATRA), the major active metabolite of all-trans retinol (vitamin A), is a key hormonal signaling molecule. In the adult organism, ATRA has a widespread influence on processes that are crucial to the growth and differentiation of cells and, in turn, the acquisition of mature cell functions. Therefore, there is considerable potential in the use of retinoids to treat diseases. ATRA binds to the retinoic acid receptors (RAR) which, as activated by ATRA, selectively regulate gene expression. There are three main RAR isoforms, RARα, RARβ, and RARγ. They each have a distinct role, for example, RARα and RARγ regulate myeloid progenitor cell differentiation and hematopoietic stem cell maintenance, respectively. Hence, targeting an isoform is crucial to developing retinoid-based therapeutics. In principle, this is exemplified when ATRA is used to treat acute promyelocytic leukemia (PML) and target RARα within PML-RARα oncogenic fusion protein. ATRA with arsenic trioxide has provided a cure for the once highly fatal leukemia. Recent in vitro and in vivo studies of RARγ have revealed the potential use of agonists and antagonists to treat diseases as diverse as cancer, heterotopic ossification, psoriasis, and acne. During the final drug development there may be a need to design newer compounds with added modifications to improve solubility, pharmacokinetics, or potency. At the same time, it is important to retain isotype specificity and activity. Examination of the molecular interactions between RARγ agonists and the ligand binding domain of RARγ has revealed aspects to ligand binding that are crucial to RARγ selectivity and compound activity and key to designing newer compounds.

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Section: Targeting Of Therapies To Rarγ Agonismmentioning

confidence: 99%

Section: Targeting Of Therapies To Rarγ Agonismmentioning

confidence: 99%

Section: Cd437 a Selective Rarγ Agonistmentioning

confidence: 99%

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Molecular Interactions of Selective Agonists and Antagonists with the Retinoic Acid Receptor γ

Powała,

Żołek,

Brown

et al. 2024

IJMS

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“…Currently, acne vulgaris represents one of the most prevalent chronic inflammatory diseases affecting not only adolescents but also adults [1]. Different features of acne patients are seborrhea, inflammatory and non-inflammatory lesions.…”

Section: Introductionmentioning

confidence: 99%

Squalene Peroxidation and Biophysical Parameters in Acne-Prone Skin: A Pilot “In Vivo” Study

Condrò,

Sciortino,

Perugini

2023

Pharmaceuticals

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Nowadays, acne vulgaris therapies are often unsuccessful. One of the responsible factors for the formation of comedones and inflammatory lesions could be the peroxidation of squalene, a hydrocarbon representing one of the major components of human sebum. This peroxidation is increased by solar irradiation. The purpose of this work was to set up an in vivo method for the extraction and quantification of squalene from acne skin and to correlate the results with biophysical skin parameters such as sebum amount, protein content and TEWL. Healthy volunteers were used as control. The results obtained demonstrated that acne-prone skin had a major quantity of squalene, and, in the stratum corneum area, its peroxide form is present. Moreover, Spearman’s rank correlation showed a positive correlation between sebum content and peroxide squalene and between porphyrin intensity and peroxide squalene.

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Chemometrics‐Empowered Optimization of a Reliable Reversed Phase–High Performance Liquid Chromatography Method for the Simultaneous Estimation of Erythromycin and Adapalene in Pharmaceutical Nanoformulation

Shirkoli,

Mastiholimath

2024

Separation Science Plus

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An innovative, simple, economical, and sensitive reversed phase–high performance liquid chromatography (RP–HPLC) chromatographic method for simultaneous analysis of erythromycin (ERY) and adapalene (ADP) in bulk and pharmaceutical nanoformulation was developed by analytical quality‐by‐design (AQbD) avenue. According to published research, there is no strategy that integrates RP–HPLC with AQbD for estimating ERY and ADP. The analysis was carried out with Box–Behnken design, which reduced trial runs and design points. Acetonitrile: orthophosphoric acid (OPA) (0.1% triethanolamine) in pH 6.2 water was used as the mobile phase. The ratio was set to 35:65 (v/v) at 0.8 mL/min flow rate to detect the analytes at 231 nm. As per the guidelines in International Conference on Harmonization Q1A (R2), the developed approach was validated. ERY and ADP regression coefficients (r2) were found to be 0.9998 and 0.9999, respectively, over 5–25 µg/mL range. Validation parameters comprising linearity, sensitivity, system suitability, precision, robustness, and accuracy were performed. To assess stability, the drugs were subjected to stress conditions (hydrolytic, oxidative, thermal, and photolytic), and drugs were most vulnerable to degrade in alkaline and oxidative conditions. A new technique successfully analyzed novel drug carriers loaded with ERY and ADP.

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Management of Acne Vulgaris With Trifarotene

Cited by 9 publications

References 29 publications

Molecular Interactions of Selective Agonists and Antagonists with the Retinoic Acid Receptor γ

Molecular Interactions of Selective Agonists and Antagonists with the Retinoic Acid Receptor γ

Squalene Peroxidation and Biophysical Parameters in Acne-Prone Skin: A Pilot “In Vivo” Study

Chemometrics‐Empowered Optimization of a Reliable Reversed Phase–High Performance Liquid Chromatography Method for the Simultaneous Estimation of Erythromycin and Adapalene in Pharmaceutical Nanoformulation

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