Potential Impact of Non-Steroidal Mineralocorticoid Receptor Antagonists in Cardiovascular Disease
Inappropriate mineralocorticoid receptor (MR) activation in different cardiovascular cell types has deleterious effects on cardiac remodeling and function. Therefore, MR inhibition is a crucial pharmacological strategy to overcome cardiovascular dysfunction. Despite efficient blockade of MR with ste...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-01-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/24/3/1922 |
| _version_ | 1797624475791917056 |
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| author | Asadur Rahman Nourin Jahan Md Tanvir Rahman Akira Nishiyama |
| author_facet | Asadur Rahman Nourin Jahan Md Tanvir Rahman Akira Nishiyama |
| author_sort | Asadur Rahman |
| collection | DOAJ |
| description | Inappropriate mineralocorticoid receptor (MR) activation in different cardiovascular cell types has deleterious effects on cardiac remodeling and function. Therefore, MR inhibition is a crucial pharmacological strategy to overcome cardiovascular dysfunction. Despite efficient blockade of MR with steroidal MR antagonists (MRAs), their clinical application is unsatisfactory due to the adverse effects. Newer non-steroidal MRAs with greater potency could be suitable for clinical application, especially in patients with type 2 diabetes mellitus and chronic kidney disease. Although clinical evidence has shown the beneficial effects of non-steroidal MRAs on cardiovascular outcomes in patients with heart failure with reduced ejection fraction, clinical trials are ongoing to evaluate the efficacy of heart failure with preserved ejection fraction. Therefore, comparative pharmacological characterization of non-steroidal MRAs over classic steroidal MRAs is crucial. Here, we summarize the pre-clinical evidence of non-steroidal MRAs, which suggests an improvement in cardiac dysfunction, as well as the underlying molecular mechanisms in animal models mimicking different clinical conditions. In addition, we discuss up-to-date information from clinical trials regarding the beneficial effects of non-steroidal MRAs on meaningful cardiovascular outcomes. Both pre-clinical and clinical evidence support treatment with non-steroidal MRAs in patients with cardiovascular disease. |
| first_indexed | 2024-03-11T09:42:52Z |
| format | Article |
| id | doaj.art-73b2c0fde3c5467980545e31cf1c419b |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-11T09:42:52Z |
| publishDate | 2023-01-01 |
| publisher | MDPI AG |
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| series | International Journal of Molecular Sciences |
| spelling | doaj.art-73b2c0fde3c5467980545e31cf1c419b2023-11-16T16:49:45ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672023-01-01243192210.3390/ijms24031922Potential Impact of Non-Steroidal Mineralocorticoid Receptor Antagonists in Cardiovascular DiseaseAsadur Rahman0Nourin Jahan1Md Tanvir Rahman2Akira Nishiyama3Department of Pharmacology, Faculty of Medicine, Kagawa University, 1750-1 Ikenobe, Miki-cho, Kita-gun, Kagawa 761-0793, JapanDepartment of Pharmacology, Faculty of Medicine, Kagawa University, 1750-1 Ikenobe, Miki-cho, Kita-gun, Kagawa 761-0793, JapanDepartment of Microbiology and Hygiene, Faculty of Veterinary Science, Bangladesh Agricultural University, Mymensingh 2202, BangladeshDepartment of Pharmacology, Faculty of Medicine, Kagawa University, 1750-1 Ikenobe, Miki-cho, Kita-gun, Kagawa 761-0793, JapanInappropriate mineralocorticoid receptor (MR) activation in different cardiovascular cell types has deleterious effects on cardiac remodeling and function. Therefore, MR inhibition is a crucial pharmacological strategy to overcome cardiovascular dysfunction. Despite efficient blockade of MR with steroidal MR antagonists (MRAs), their clinical application is unsatisfactory due to the adverse effects. Newer non-steroidal MRAs with greater potency could be suitable for clinical application, especially in patients with type 2 diabetes mellitus and chronic kidney disease. Although clinical evidence has shown the beneficial effects of non-steroidal MRAs on cardiovascular outcomes in patients with heart failure with reduced ejection fraction, clinical trials are ongoing to evaluate the efficacy of heart failure with preserved ejection fraction. Therefore, comparative pharmacological characterization of non-steroidal MRAs over classic steroidal MRAs is crucial. Here, we summarize the pre-clinical evidence of non-steroidal MRAs, which suggests an improvement in cardiac dysfunction, as well as the underlying molecular mechanisms in animal models mimicking different clinical conditions. In addition, we discuss up-to-date information from clinical trials regarding the beneficial effects of non-steroidal MRAs on meaningful cardiovascular outcomes. Both pre-clinical and clinical evidence support treatment with non-steroidal MRAs in patients with cardiovascular disease.https://www.mdpi.com/1422-0067/24/3/1922cardiovascular diseasenon-steroidal mineralocorticoid receptor antagonistheart failure |
| spellingShingle | Asadur Rahman Nourin Jahan Md Tanvir Rahman Akira Nishiyama Potential Impact of Non-Steroidal Mineralocorticoid Receptor Antagonists in Cardiovascular Disease International Journal of Molecular Sciences cardiovascular disease non-steroidal mineralocorticoid receptor antagonist heart failure |
| title | Potential Impact of Non-Steroidal Mineralocorticoid Receptor Antagonists in Cardiovascular Disease |
| title_full | Potential Impact of Non-Steroidal Mineralocorticoid Receptor Antagonists in Cardiovascular Disease |
| title_fullStr | Potential Impact of Non-Steroidal Mineralocorticoid Receptor Antagonists in Cardiovascular Disease |
| title_full_unstemmed | Potential Impact of Non-Steroidal Mineralocorticoid Receptor Antagonists in Cardiovascular Disease |
| title_short | Potential Impact of Non-Steroidal Mineralocorticoid Receptor Antagonists in Cardiovascular Disease |
| title_sort | potential impact of non steroidal mineralocorticoid receptor antagonists in cardiovascular disease |
| topic | cardiovascular disease non-steroidal mineralocorticoid receptor antagonist heart failure |
| url | https://www.mdpi.com/1422-0067/24/3/1922 |
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