Research progress of phosphodiesterase inhibitors in inflammatory bowel disease treatment

Zhejiang Da Xue Xue Bao Yi Xue Ban. 2021 Oct 25;50(5):659-665. doi: 10.3724/zdxbyxb-2021-0170.

Abstract

Inflammatory bowel disease is a recurrent chronic intestinal inflammatory disease with unknown etiology and no effective treatment. Phosphodiesterase (PDE) regulates a variety of physiological and pathophysiological processes by mediating the hydrolysis of intracellular second messengers cyclic adenosine monophosphate and cyclic guanosine monophosphate. In recent years, a series of researches suggest that PDE inhibitors such as several PDE4 inhibitors, PDE5 inhibitors (sildenafil, tadalafil and vardenafil), PDE3 inhibitors (cilostazol), PDE9 inhibitor (PF-04447943) and PDE3/PDE4 double inhibitor (pumafentrine) have ameliorating effect on experimental colitis in animals. In clinical trials, PDE4 inhibitor apremilast showed more therapeutic advantage than tetomilast. This article reviews the recent research progress of PDE inhibitors in treatment of inflammatory bowel disease.

Keywords: Cyclic adenosine monophosphate; Cyclic guanosine monophosphate; Inflammatory bowel disease; Phosphodiesterase; Phosphodiesterase inhibitor; Review.

Publication types

  • Review

MeSH terms

  • Animals
  • Colitis*
  • Inflammatory Bowel Diseases* / drug therapy
  • Phosphodiesterase 4 Inhibitors*

Substances

  • Phosphodiesterase 4 Inhibitors

Grants and funding

国家自然科学基金(81402989); 浙江省基础公益研究计划(LGD20H010002)