摘要
PDE4酶已被证明是一个治疗不同的疾病如哮喘、慢性阻塞性肺疾病、糖尿病、亨廷顿氏病、以及其他各种炎症性疾病的多功能药物靶点。由于其抑制炎症细胞反应的能力,PDE4抑制剂被广泛研究应用于COPD的治疗。罗氟司特是唯一属于这类治疗COPD和哮喘患者并具有显著的效果的批准药物。这些观点强调了罗氟司特和西洛的药理作用。此外,通过详细比较西洛和罗氟司特的药理学,药代动力学,药效学特性及结构特点,我们证明了该药的药理优势。其他促进PDE4抑制活性的分子也被强调。随着PDE4抑制剂不断地改善治疗指数,这类化合物的副作用、他们的管理以及未来的发展方向也是研究的焦点。本文主要强调了将来的研究方向为抑制其如呕吐等副作用和取得更好的风险比率。
关键词: 哮喘,西洛,COPD,PDE4抑制剂通路,磷酸二酯酶,罗氟司特。
Current Medicinal Chemistry
Title:Phosphodiesterase 4 (PDE4) Inhibitors in the Treatment of COPD: Promising Drug Candidates and Future Directions
Volume: 23 Issue: 2
Author(s): Naisargee Parikh and Asit K. Chakraborti
Affiliation:
关键词: 哮喘,西洛,COPD,PDE4抑制剂通路,磷酸二酯酶,罗氟司特。
摘要: The PDE4 enzyme has been proven to be a versatile drug target for therapeutics to treat diverse disease conditions such as asthma, COPD, diabetes, Huntington’s disease, and various other inflammatory disorders. The treatment of COPD is the most studied utility for PDE4 inhibitors due to their ability to inhibit inflammatory cell responses. Roflumilast is the only approved drug belonging to this class to treat COPD and has shown significant results in the treatment of asthmatic patients. This perspective highlights the pharmacological details of roflumilast and cilomilast. Moreover, efforts have been made to justify the superiority of roflumilast over cilomilast by detailed comparison of their pharmacological, pharmacokinetic, pharmacodynamic properties and structural features. Several other molecules, with promising PDE4 inhibitory activity have also been highlighted. Commonly associated side effects with this class of compounds, their management, and future direction towards the development of PDE4 inhibitors with improved therapeutic index are the focus of this perspective. More emphasis has been given towards the future development strategies to limit the side effects such as emesis and to achieve better benefit to risk ratio.
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Naisargee Parikh and Asit K. Chakraborti , Phosphodiesterase 4 (PDE4) Inhibitors in the Treatment of COPD: Promising Drug Candidates and Future Directions, Current Medicinal Chemistry 2016; 23 (2) . https://dx.doi.org/10.2174/0929867323666151117121334
DOI https://dx.doi.org/10.2174/0929867323666151117121334 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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