Abstract
Ovarian hormone deficiency status is associated with increased cardiovascular morbidity and mortality, suggesting that estrogen might exhibit a favorable cardiovascular effect. Estrogen has a multitude of beneficial biological effects on surrogate markers of cardiovascular disease that may account for this hypothesis. However, none of the randomized trials already conducted with hormone replacement therapy showed overall benefit by means of reducing clinical ischemic cardiovascular events and/or suppressing atherogenesis. Moreover, the Womens Health Initiative study (WHI) has suggested a possible detrimental effect for hormone replacement therapy including increased cardiovascular morbidity, ovarian and breast cancer. Hence, any beneficial effect of estrogen must be carefully weighed against its carcinogenic properties together with its side effects. The need for a more efficient and specific molecule led to the development of the selective estrogen receptor modulators (SERMs). This new generation of drugs mimick the effect of estrogen in some tissues while antagonize several estrogen effects in other tissues. These unique properties offer the possibility to attain the beneficial effects of estrogen while avoiding its carcinogenic effect and the accompanying adverse reactions. Here we review the different effects of raloxifene- a protype second generation SERM on the cardiovascular system. We discuss raloxifenes role at different levels of the atherothrombotic cascade addressing each level separately; trying to clarify the net effect of raloxifene in modulating thrombosis in the arterial tree.
Keywords: Raloxifene, lipids, estradiol, myocardial infarction
Mini-Reviews in Medicinal Chemistry
Title: Raloxifene: Cardiovascular Considerations
Volume: 7 Issue: 8
Author(s): R. Abu Fanne, A. Brzezinski and H.D. Danenberg
Affiliation:
Keywords: Raloxifene, lipids, estradiol, myocardial infarction
Abstract: Ovarian hormone deficiency status is associated with increased cardiovascular morbidity and mortality, suggesting that estrogen might exhibit a favorable cardiovascular effect. Estrogen has a multitude of beneficial biological effects on surrogate markers of cardiovascular disease that may account for this hypothesis. However, none of the randomized trials already conducted with hormone replacement therapy showed overall benefit by means of reducing clinical ischemic cardiovascular events and/or suppressing atherogenesis. Moreover, the Womens Health Initiative study (WHI) has suggested a possible detrimental effect for hormone replacement therapy including increased cardiovascular morbidity, ovarian and breast cancer. Hence, any beneficial effect of estrogen must be carefully weighed against its carcinogenic properties together with its side effects. The need for a more efficient and specific molecule led to the development of the selective estrogen receptor modulators (SERMs). This new generation of drugs mimick the effect of estrogen in some tissues while antagonize several estrogen effects in other tissues. These unique properties offer the possibility to attain the beneficial effects of estrogen while avoiding its carcinogenic effect and the accompanying adverse reactions. Here we review the different effects of raloxifene- a protype second generation SERM on the cardiovascular system. We discuss raloxifenes role at different levels of the atherothrombotic cascade addressing each level separately; trying to clarify the net effect of raloxifene in modulating thrombosis in the arterial tree.
Export Options
About this article
Cite this article as:
R. Abu Fanne , A. Brzezinski and H.D. Danenberg , Raloxifene: Cardiovascular Considerations, Mini-Reviews in Medicinal Chemistry 2007; 7 (8) . https://dx.doi.org/10.2174/138955707781387911
DOI https://dx.doi.org/10.2174/138955707781387911 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...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
Related Articles
-
Targeted Therapies in Solid Tumours: Pinpointing the Tumours Achilles Heel
Current Pharmaceutical Design Prostate Cancer Prevention in the Developing World - What are we Waiting for?
Current Pharmacogenomics and Personalized Medicine Nitrogen Containing Privileged Structures and their Solid Phase Combinatorial Synthesis
Combinatorial Chemistry & High Throughput Screening Recent Patents on MicroRNA-Induced Pluripotent Stem Cell Generation
Recent Patents on Regenerative Medicine Neurochemical Markers in the Mammalian Brain: Structure, Roles in Synaptic Communication, and Pharmacological Relevance
Current Medicinal Chemistry FK506-Binding Proteins and Their Diverse Functions
Current Molecular Pharmacology Pharmacogenetics of Thiopurines in Inflammatory Bowel Disease
Current Pharmaceutical Design Recapitulation of Cancer Nanotherapeutics
Current Nanomedicine Non-canonical Molecular Targets for Novel Analgesics: Intracellular Calcium and HCN Channels
Current Neuropharmacology Editorial (Thematic Issue: The Crosstalk between Non-Pharmaceutical and Pharmaceutical Approaches to Prevention and Treatment of Chronic Diseases: Current Concepts and Perspectives)
Current Pharmaceutical Design The Role of YY1 in Oncogenesis and Its Potential as a Drug Target in Cancer Therapies
Current Cancer Drug Targets Targeted Delivery of Montelukast for the Treatment of Alzheimer’s Disease
CNS & Neurological Disorders - Drug Targets Conjugation Approaches for Construction of Aptamer-Modified Nanoparticles for Application in Imaging
Current Topics in Medicinal Chemistry Molecular Docking and In Silico ADMET Study Reveals Flavonoids as a Potential Inhibitor of Aromatase
Letters in Drug Design & Discovery Identification of Novel Prognostic Biomarkers in Head and Neck Squamous Cell Carcinoma using Bioinformatics Analysis
Combinatorial Chemistry & High Throughput Screening Targeting Anti-Cancer Active Compounds: Affinity-Based Chromatographic Assays
Current Pharmaceutical Design Radiolabeled Nucleoside Analogues for PET Imaging of HSV1-tk Gene Expression
Current Topics in Medicinal Chemistry Role of Secretory Phospholipase A2 in CNS Inflammation: Implications in Traumatic Spinal Cord Injury
CNS & Neurological Disorders - Drug Targets Ghrelin and Energy Balance: Focus on Current Controversies
Current Drug Targets Radiolabeled Peptides in Imaging and Therapy: Basic and Clinical Perspectives
Current Medicinal Chemistry