2023年6月24日 · chf6001是一种新型的吸入式pde4抑制剂，对copd具有非常高的效力 （ic 50 = 0.026 nm，可能是文献中最有效的pde4抑制剂） 。它在各种动物模型中显示了临床前的疗效，并且耐受性良好。

2020年10月10日 · β2-肾上腺素能受体拮抗剂、毒蕈碱型乙酰胆碱受体M3激动剂、 糖皮质激素 受体抑制剂是 慢性阻塞性肺疾病 (COPD)治疗领域的明星。 单药、二联、三联组合相继登场，沙丁胺醇、噻托溴铵、富马酸福莫特罗、糠酸氟替卡松等药物那是耳熟能详。 曾经罗氟司特作为首个口服 PDE4 抑制剂上市时，绚烂、星光夺目本应该是它的归途，可现实是不温不火渐渐成了它的主旋律，上市时的光芒不再，好像已经只剩下COPD城中落寞的背影，同时新开发的PDaE4抑制剂接 …

2024年6月27日 · Ensifentrine（恩塞芬汀）是一款由Verona开发的靶向磷酸二酯酶-3 (PDE3)和磷酸二酯酶-4 (PDE4)的双靶点抑制剂，对PDE3的亲和度是PDE4的3440倍。 作为双重PDE3/4抑制剂，ensifentrine能够提供支气管扩张和抗炎双重作用，显著改善患者的呼吸功能和生活质量；除此以外，ensifentrine作为雾化吸入制剂，有助于避免胃肠道相关副作用。 作为COPD领域全新机制的药物，ensifentrine的意义在于在原有的3种传统机制的基础上带来额外的临床获益，而非击败 …

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. Objectives: To evaluate the efficacy and safety of oral PDE 4 inhibitors in the management of stable COPD.

Phosphodiesterase-4 (PDE₄) inhibitors are a relatively new class of medicines marketed to improve COPD. They have both bronchodilator and anti-inflammatory effects. Two currently available medicines - roflumilast and cilomilast - are taken as a tablet.

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。

2024年11月13日 · The current review provides an overview of various PDE4 inhibitors in the treatment of COPD. The possibility of studying different selective PDE4 inhibitors and dual PDE3/4 inhibitors in combination with currently available treatments as a way forward to increase their therapeutic effectiveness is also emphasized.

2014年2月11日 · However, there is growing evidence to suggest that dual inhibition of PDE3 and PDE4 can be additive or even synergistic at suppressing inflammatory mediator release from other cell types which also express PDE3 that are thought to play a role in COPD (e.g. macrophages, dendritic cells, epithelial cells, lymphocytes, airway smooth muscle cells ...

Inhibiting PDE 4 in these cells leads to increased cAMP levels, down-regulating the inflammatory response. Because PDE 4 is also expressed in airway smooth muscle and, in vitro, PDE 4 inhibitors relax lung smooth muscle, selective PDE 4 inhibitors are being developed for …

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 ...