磷酸二酯酶5抑制剂（PDE5）的新的治疗应用

Title:New Therapeutic Applications of Phosphodiesterase 5 Inhibitors (PDE5-Is)

Volume: 23 Issue: 12

Author(s): Giovanni Ribaudo, Mario Angelo Pagano, Sergio Bova, Giuseppe Zagotto

Affiliation:

关键词: PDE5，sildenafil，抗癌，多目标，囊性纤维化，勃起功能障碍。

摘要: Background: Phosphodiesterase 5 inhibitors (PDE5-Is) sildenafil, vardenafil, tadalafil and the recently approved avanafil represent the first-line choice for both on-demand and chronic treatment of erectile dysfunction (ED). In addition to this, sildenafil and tadalafil, have also been approved for the treatment of pulmonary arterial hypertension. Due to its expression and localization in many tissues, PDE5 and its regulation has been reported to be involved in several other diseases. Objective: We aim to provide an updated overview of the emerging therapeutic applications of PDE5-Is besides ED, taking into account the latest ongoing research reports. Methods: We searched online databases (Pubmed, Reaxys, Scopus) to lay the bases for an accurate, quality criteria-based literature update. We focused our attention on most recent research reports, in particular when supported by pre-clinical and clinical data. Results: The regulation of PDE5 may influence pathological conditions such as, among the others, heart failure, cystic fibrosis, cancer, CNS-related diseases, diabetes and dysfunctions affecting male urinary/reproductive system. Conclusion: Sildenafil, vardenafil, tadalafil and the other chemical entities considered PDE5-Is showed overall positive results and significant improvements in the studied disease, thus some discordant results, in particular when comparing pre-clinical and clinical data, have to be pointed out, suggesting that further insights are needed especially to assess the exact molecular pathway underlying.

Cite this article as:

Giovanni Ribaudo, Mario Angelo Pagano, Sergio Bova, Giuseppe Zagotto , New Therapeutic Applications of Phosphodiesterase 5 Inhibitors (PDE5-Is), Current Medicinal Chemistry 2016; 23 (12) . https://dx.doi.org/10.2174/0929867323666160428110059