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
-
A Molecular Bridge: Connecting Type 2 Diabetes and Alzheimer’s Disease
CNS & Neurological Disorders - Drug Targets G Protein-Coupled Receptors – Potential Roles in Clinical Pharmacology
Cardiovascular & Hematological Agents in Medicinal Chemistry An Update on the Association of Protein Kinases with Cardiovascular Diseases
Current Pharmaceutical Design Standardization of QRS Duration Measurement and LBBB Criteria in CRT Trials and Clinical Practice
Current Cardiology Reviews Sleep Apnea and Coronary Heart Disease: From Dusk Till Dawn and Further
Current Respiratory Medicine Reviews Update on COX-2 Selective Inhibitors: Chemical Classification, Side Effects and their Use in Cancers and Neuronal Diseases
Current Topics in Medicinal Chemistry Enhanced Nitinol Properties for Biomedical Applications
Recent Patents on Biomedical Engineering (Discontinued) Protein Kinase C and Prostate Carcinogenesis: Targeting the Cell Cycle and Apoptotic Mechanisms
Current Drug Targets Distamycins: Strategies for Possible Enhancement of Activity and Specificity
Mini-Reviews in Medicinal Chemistry FOXO and FOXM1 in Cancer: The FOXO-FOXM1 Axis Shapes the Outcome of Cancer Chemotherapy
Current Drug Targets Threes Company: Regulation of Cell Fate by Statins
Current Drug Targets - Cardiovascular & Hematological Disorders Effect of Systemic Inflammation on the Function of Insulin and Glucose Metabolism in Rheumatoid Arthritis
Current Diabetes Reviews High Throughput Metabolomics in Clinical Studies: Review and New Applications to Remote Ischemic Preconditioning
Current Topics in Medicinal Chemistry Perspectives of Protein Kinase C (PKC) Inhibitors as Anti-Cancer Agents
Mini-Reviews in Medicinal Chemistry Transforming Growth Factor-Beta and the Kidney: What We Know and What We Can Do?
Current Enzyme Inhibition Mevalonate Cascade and Neurodevelopmental and Neurodegenerative Diseases: Future Targets for Therapeutic Application
Current Molecular Pharmacology Synthesis and Cytotoxic Activities of Difluoro-Dimethoxy Chalcones
Anti-Cancer Agents in Medicinal Chemistry Hypothetical Role of Growth Factors to Reduce Intervertebral Disc Degeneration Significantly through Trained Biological Transformations
Current Pharmaceutical Design Meet Our Associate Editor
MicroRNA Forkhead Genes: Their Role and Impact on Ocular Developmental Diseases
Current Genomics