磷酸雙酯酶4型抑制劑（PDE₄）是市場上用於改善COPD相對較新的一類藥物。它們同時具有支氣管擴張劑和抗發炎作用。兩種目前可使用的藥物 - roflumilast和cilomilast - 皆以錠劑服用。我們整理並分析了現有試驗的結果，以確定PDE₄抑製劑在COPD中的效益和風險。

Ensifentrine is a novel, potent, and selective dual inhibitor of phosphodiesterase (PDE)3 and PDE4 designed for delivery by inhalation that combines effects on airway inflammation, bronchodilation and ciliary function in bronchial epithelia.

PDE₄ inhibitors provided a small benefit in improving lung function measurements (forced expiratory volume in one second (FEV₁), forced vital capacity (FVC), and peak expiratory flow (PEF)). PDE₄ inhibitors also reduced the likelihood of COPD-related exacerbations.

Are PDE 4 inhibitors the long‐needed magic pill for COPD patients? The comprehensive, high‐quality systematic review by Chong and colleagues sheds some light on the benefits and harms associated with PDE 4 inhibitors. This Cochrane Review identified 23 published and unpublished placebo‐controlled trials on cilomilast and roflumilast that ...

2004年6月1日 · In this article, I describe the significant role that inflammation appears to play in the pathogenesis of COPD, the impact of PDE4 inhibitors in reducing inflammation via increased accumulation of the cyclic nucleotide, adenosine 3′,5′-cyclic monophosphate (cAMP), and the potential advantages of second generation, selective PDE4 inhibitors ...

PDE 4 inhibitors reduce overproduction of other pro-inflammatory mediators, including arachidonic acid and leukotrienes (Torphy 1998). PDE 4 inhibitors also inhibit cellular trafficking and microvascular leakage, production of reactive oxygen species, and cell adhesion molecule expression in vitro and in vivo (Sanz et al 2005).

2017年9月19日 · Roflumilast and cilomilast are oral phosphodiesterase 4 (PDE 4) inhibitors proposed to reduce the airway inflammation and bronchoconstriction seen in COPD. This is an update of a Cochrane review first published in 2011 and updated in 2013.

Cilomilast and roflumilast are potent and selective phosphodiesterase (PDE)4 inhibitors, with an improved therapeutic index compared with the weak, non-selective PDE inhibitor, theophylline.

2020年9月22日 · This study evaluated the efficacy, safety and tolerability of the novel inhaled phosphodiesterase-4 inhibitor CHF6001 added-on to formoterol in patients with chronic obstructive pulmonary disease (COPD). Randomised, double-blind, placebo- and active-controlled, parallel-group study.

2014年2月11日 · Combined inhibition of PDE3 and PDE4 would appear to be an attractive strategy to treat COPD, and other inflammatory airway diseases given the broad anti-inflammatory and bronchodilator effects of these agents, together with their potential to …