Abstract
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.
Keywords: PDE5, sildenafil, anticancer, multi-target, cystic fibrosis, erectile dysfunction.
Current Medicinal Chemistry
Title:New Therapeutic Applications of Phosphodiesterase 5 Inhibitors (PDE5-Is)
Volume: 23 Issue: 12
Author(s): Giovanni Ribaudo, Mario Angelo Pagano, Sergio Bova and Giuseppe Zagotto
Affiliation:
Keywords: PDE5, sildenafil, anticancer, multi-target, cystic fibrosis, erectile dysfunction.
Abstract: 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.
Export Options
About this article
Cite this article as:
Ribaudo Giovanni, Angelo Pagano Mario, Bova Sergio and Zagotto Giuseppe, New Therapeutic Applications of Phosphodiesterase 5 Inhibitors (PDE5-Is), Current Medicinal Chemistry 2016; 23 (12) . https://dx.doi.org/10.2174/0929867323666160428110059
DOI https://dx.doi.org/10.2174/0929867323666160428110059 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Editorial: [Pleiotropic Effects of Statins: Implications for a Wide Range of Diseases]
Current Vascular Pharmacology Emerging Role for Antioxidant Therapy in Protection Against Diabetic Cardiac Complications: Experimental and Clinical Evidence for Utilization of Classic and New Antioxidants
Current Cardiology Reviews Role of Class II Nuclear Receptors in Liver Carcinogenesis
Anti-Cancer Agents in Medicinal Chemistry Keeping the Balance Between Proliferation and Differentiation:The Primary Cilium
Current Genomics Viscosupplementation with Intra-Articular Hyaluronic Acid for Treatment of Osteoarthritis in the Elderly
Current Pharmaceutical Design HR+, HER2– Advanced Breast Cancer and CDK4/6 Inhibitors: Mode of Action, Clinical Activity, and Safety Profiles
Current Cancer Drug Targets Potential Role of Rho Kinase Inhibitors in Combating Diabetes-Related Complications Including Diabetic Neuropathy-A Review
Current Diabetes Reviews Acyclonucleosides, Modified Seco-Nucleosides, and Salicyl- or Catechol- Derived Acyclic 5-Fluorouracil O,N-Acetals: Antiproliferative Activities, Cellular Differentiation and Apoptosis
Current Medicinal Chemistry Herb-Drug Interactions: An Insight into Cardiovascular Diseases Based on Case Reports
Cardiovascular & Hematological Agents in Medicinal Chemistry NTproBNP: An Important Biomarker in Cardiac Diseases
Current Topics in Medicinal Chemistry Recent Progress and Related Patents on the Applications of Bone Marrow-Derived Stem/Progenitor Cells in Regenerative Medicine and Cancer Therapies
Recent Patents on Regenerative Medicine Mini Heme-Proteins: Designability of Structure and Diversity of Functions
Current Protein & Peptide Science Insight γ-Secretase: Structure, Function, and Role in Alzheimer’s Disease
Current Drug Targets Judging Children as Children
Adolescent Psychiatry Do Advanced Glycation End Products (AGEs) Contribute to the Comorbidities of Polycystic Ovary Syndrome (PCOS)?
Current Pharmaceutical Design Structure-Activity Relationships of Flavonoids
Current Organic Chemistry Inflammatory Arthritis and Heart Disease
Current Pharmaceutical Design Apoptosis: Potential Therapeutic Targets for New Drug Discovery
Current Medicinal Chemistry Chronic Inflammatory Diseases: Progress and Prospect with Herbal Medicine
Current Pharmaceutical Design Pancreatic Cancer: Promises and Failures of Target Therapies
Reviews on Recent Clinical Trials