Nonclinical genotoxicity and carcinogenicity profile of apremilast, an oral selective inhibitor of PDE4

Wegesser, Teresa C.; Coppi, Aldo; Harper, Tod; Paris, Maria; Minocherhomji, Sheroy

doi:10.1016/j.yrtph.2021.104985

Cited by 3 publications

(1 citation statement)

References 21 publications

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“…As a result, inhibitors of PDE4 have been synthesized. Currently, there are systemic PDE4 inhibitors like apremilast and topical inhibitors like roflumilast and crisaborole [ 44 ].…”

Section: Resultsmentioning

confidence: 99%

New Perspectives in the Management of Chronic Hand Eczema: Lessons from Pathogenesis

Tancredi,

Buononato,

Caccavale

et al. 2023

IJMS

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Chronic hand eczema (CHE) is a common inflammatory skin condition that significantly impacts the quality of life. From work-related disabilities to social embarrassment, pain, and financial costs, the burden on society is substantial. Managing this condition presents challenges such as long-term treatment, poor patient compliance, therapy side effects, and economic feasibility. As a result, significant efforts have been made in this field in recent years. Specifically, the broader understanding of CHE pathogenesis has led to the development of new drugs, both topical and systemic. The aim of this narrative review is to summarize the current available data on hand eczema pathophysiology and explore the resulting developments in drugs for its treatment. A comprehensive search on PubMed and the other main scientific databases was conducted using keywords related to CHE and its pathogenesis. The most relevant pathways targeted by therapies include the JAK-STAT cascade, IL-4, and IL-13 axis, phosphodiesterase 4 enzyme, and chemo-attractant cytokines. In the near future, physicians will have a plethora of therapeutic alternatives. Consequently, they should be well-trained not only in how to use these alternatives but also how to combine these treatments to address the ongoing challenges related to efficacy, tolerability, and safety.

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“…As a result, inhibitors of PDE4 have been synthesized. Currently, there are systemic PDE4 inhibitors like apremilast and topical inhibitors like roflumilast and crisaborole [ 44 ].…”

Section: Resultsmentioning

confidence: 99%

New Perspectives in the Management of Chronic Hand Eczema: Lessons from Pathogenesis

Tancredi,

Buononato,

Caccavale

et al. 2023

IJMS

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Immunological Advancements In Hand Eczema Treatment: Progress With Small Molecules and Biologics

Grafanaki,

Maniatis,

Antonatos

et al. 2024

Curr Treat Options Allergy

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Bioactive compounds from Huashi Baidu decoction possess both antiviral and anti-inflammatory effects against COVID-19

Liu

et al. 2023

Proc. Natl. Acad. Sci. U.S.A.

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The coronavirus disease 2019 (COVID-19) pandemic is an ongoing global health concern, and effective antiviral reagents are urgently needed. Traditional Chinese medicine theory-driven natural drug research and development (TCMT-NDRD) is a feasible method to address this issue as the traditional Chinese medicine formulae have been shown effective in the treatment of COVID-19. Huashi Baidu decoction (Q-14) is a clinically approved formula for COVID-19 therapy with antiviral and anti-inflammatory effects. Here, an integrative pharmacological strategy was applied to identify the antiviral and anti-inflammatory bioactive compounds from Q-14. Overall, a total of 343 chemical compounds were initially characterized, and 60 prototype compounds in Q-14 were subsequently traced in plasma using ultrahigh-performance liquid chromatography with quadrupole time-of-flight mass spectrometry. Among the 60 compounds, six compounds (magnolol, glycyrrhisoflavone, licoisoflavone A, emodin, echinatin, and quercetin) were identified showing a dose-dependent inhibition effect on the SARS-CoV-2 infection, including two inhibitors (echinatin and quercetin) of the main protease (M pro ), as well as two inhibitors (glycyrrhisoflavone and licoisoflavone A) of the RNA-dependent RNA polymerase (RdRp). Meanwhile, three anti-inflammatory components, including licochalcone B, echinatin, and glycyrrhisoflavone, were identified in a SARS-CoV-2-infected inflammatory cell model. In addition, glycyrrhisoflavone and licoisoflavone A also displayed strong inhibitory activities against cAMP-specific 3′,5′-cyclic phosphodiesterase 4 (PDE4). Crystal structures of PDE4 in complex with glycyrrhisoflavone or licoisoflavone A were determined at resolutions of 1.54 Å and 1.65 Å, respectively, and both compounds bind in the active site of PDE4 with similar interactions. These findings will greatly stimulate the study of TCMT-NDRD against COVID-19.

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Nonclinical genotoxicity and carcinogenicity profile of apremilast, an oral selective inhibitor of PDE4

Cited by 3 publications

References 21 publications

New Perspectives in the Management of Chronic Hand Eczema: Lessons from Pathogenesis

New Perspectives in the Management of Chronic Hand Eczema: Lessons from Pathogenesis

Immunological Advancements In Hand Eczema Treatment: Progress With Small Molecules and Biologics

Bioactive compounds from Huashi Baidu decoction possess both antiviral and anti-inflammatory effects against COVID-19

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