The need for new and effective treatments for dementia remains indisputably high. Phosphodiesterase inhibitors (PDE-Is) have proven efficacy as cognitive enhancers based on their positive effects in numerous preclinical studies. Especially the PDE4 subfamily is of interest due to its expression in the hippocampus, the key structure for memory formation. The current study investigates the memory...

BACKGROUND Chronic obstructive pulmonary disease (COPD) is a chronic inflammatory disease mediated by an array of inflammatory cells and mediators, but above all, CD8+ T-lymphocytes, macrophages and neutrophils are important players in disease pathogenesis. Roflumilast, a first-in-class, potent and selective phosphodiesterase 4 (PDE4) inhibitor, reduces the rate of exacerbations in patients wit...

RATIONALE There is a need for new agents capable of suppressing the inflammatory response in chronic obstructive pulmonary disease. OBJECTIVES This study evaluated the effects of roflumilast, a phosphodiesterase 4 (PDE4) inhibitor on acute lung inflammation and chronic lung changes in models of cigarette exposure in mice. METHODS Roflumilast was given orally either at 1 mg/kg (R1) or at 5 m...

OBJECTIVE The specific inhibition of phosphodiesterase (PDE)4 and dual inhibition of PDE3 and PDE4 has been shown to decrease inflammation by suppression of pro-inflammatory cytokine synthesis. We examined the effect of roflumilast, a selective PDE4 inhibitor marketed for severe COPD, and the investigational compound pumafentrine, a dual PDE3/PDE4 inhibitor, in the preventive dextran sodium sul...

Roflumilast (Daxas® [EU], Daliresp® [USA]) is the first phospho diesterase 4 inhib itor approved in Europe to be used in severe chronic obstructive pulmonary disease (COPD). Its preclinical evaluation streamed its subsequent clinical development towards COPD based on the prominent anti-inflammatory activities demonstrated in various preclinical models of COPD. Its clinical development was based...

Clinical utility of phosphodiesterase 4 (PDE4) inhibitors as anti-inflammatory agents has, to date, been limited by adverse effects including nausea and emesis, making accurate assessment of emetic versus anti-inflammatory potencies critical to the development of inhibitors with improved therapeutic indices. In the present study we determined the in vitro and in vivo anti-inflammatory potencies...

BACKGROUND Recent studies show that mitophagy, the autophagy-dependent turnover of mitochondria, mediates pulmonary epithelial cell death in response to cigarette smoke extract (CSE) exposure and contributes to the development of emphysema in vivo during chronic cigarette smoke (CS) exposure, although the underlying mechanisms remain unclear. METHODS In this study, we investigated the role of...

BACKGROUND This trial aimed to evaluate the efficacy and safety of roflumilast for treating Chinese patients with chronic obstructive pulmonary disease (COPD). METHODS A total of 120 patients with COPD were recruited and were randomly divided into 2 groups (an intervention group and a placebo group) at a 1:1 ratio. Patients received either roflumilast or placebo 500 μg once daily for a total ...

Asthma is a heterogeneous disease characterized by chronic inflammation of the airways induced reversible obstruction resulting in mortality and morbidity. Roflumilast second-generation selective inhibitor phosphodiesterase-4 targeting PDE type 4 isoenzymes, disturbing breakdown cyclic AMP (cAMP) reducing inflammation. However, it has not been recommended for asthma patients because insufficien...

Introduction: Seborrheic dermatitis (SD) is a common, chronic, inflammatory dermatosis that affects patients of all ages with global prevalence ≥5%. Treatments usually consist topical therapies, including antifungals and low potency corticosteroids; however, current treatments have limitations such as side effects long-term use and/or vehicles can be difficult to on both hair-bearing non-hair-b...