Apremilast, a cAMP phosphodiesterase-4 inhibitor, demonstrates anti-inflammatory activity in vitro and in a model of psoriasis.
Peter H. Schafer,Anastasia Parton,Anita Gandhi,Lori Capone,Mary Adams,Lei Wu,Justin B. Bartlett,Loveland Ma,Amos Gilhar,Cheung Yf,George S. Baillie,Houslay,Man Hw,G. W. Muller,D. I. Stirling +14 more
TLDR
The inhibitory effects of apremilast on pro‐inflammatory responses of human primary peripheral blood mononuclear cells, polymorphonuclear Cells, natural killer cells and epidermal keratinocytes were explored in vitro, and in a preclinical model of psoriasis.Abstract:
Background and purpose:
Apremilast is an orally administered phosphodiesterase-4 inhibitor, currently in phase 2 clinical studies of psoriasis and other chronic inflammatory diseases. The inhibitory effects of apremilast on pro-inflammatory responses of human primary peripheral blood mononuclear cells (PBMC), polymorphonuclear cells, natural killer (NK) cells and epidermal keratinocytes were explored in vitro, and in a preclinical model of psoriasis.read more
Citations
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Journal ArticleDOI
Psoriasis Pathogenesis and Treatment.
Adriana Rendon,Knut Schäkel +1 more
TL;DR: The role of genetics, associated epigenetic mechanisms, and the interaction of the skin flora in the pathophysiology of psoriasis is described, which includes a comprehensive review of well-established widely available therapies and novel targeted drugs.
Journal ArticleDOI
Mammalian Cyclic Nucleotide Phosphodiesterases: Molecular Mechanisms and Physiological Functions
TL;DR: Recent reported x-ray crystallographic structures have defined features that provide for specificity for cAMP or cGMP in PDE catalytic sites or their GAF domains, as well as mechanisms involved in catalysis, oligomerization, autoinhibition, and interactions with inhibitors.
Journal ArticleDOI
Treatment of psoriatic arthritis in a phase 3 randomised, placebo-controlled trial with apremilast, an oral phosphodiesterase 4 inhibitor
Arthur Kavanaugh,Philip J. Mease,Juan J. Gomez-Reino,Adewale Adebajo,Jürgen Wollenhaupt,Dafna D. Gladman,Eric Lespessailles,Stephen Hall,Marla Hochfeld,C. Hu,Douglas R. Hough,R. Stevens,Georg Schett +12 more
TL;DR: Apremilast demonstrated an acceptable safety profile and was generally well tolerated in the treatment of psoriatic arthritis, improving signs and symptoms and physical function.
Journal ArticleDOI
Efficacy and safety of apremilast, an oral phosphodiesterase 4 inhibitor, in patients with moderate-to-severe plaque psoriasis over 52 weeks: a phase III, randomized controlled trial (ESTEEM 2).
Carle Paul,J. Cather,Melinda Gooderham,Yves Poulin,Ulrich Mrowietz,Carlos Ferrándiz,Jeffrey J. Crowley,C. Hu,Rm Stevens,K. Shah,Rm Day,Giampiero Girolomoni,Ab Gottlieb +12 more
TL;DR: Apremilast, an oral phosphodiesterase 4 inhibitor, regulates immune responses associated with psoriasis in women and girls with atypical immune responses to chemotherapy.
Journal ArticleDOI
Apremilast mechanism of action and application to psoriasis and psoriatic arthritis.
TL;DR: Apremilast is an orally available targeted PDE4 inhibitor that modulates a wide array of inflammatory mediators involved in psoriasis and psoriatic arthritis, including decreases in the expression of inducible nitric oxide synthase, TNF-α, and interleukin (IL)-23 and increases IL-10.
References
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Pathogenesis and therapy of psoriasis
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Marco Conti,Joseph A. Beavo +1 more
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Journal ArticleDOI
Dermal injection of immunocytes induces psoriasis.
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