Abstract
Cilostazol (CLZ) was originally developed as a selective inhibitor of cyclic nucleotide phosphodiesterase 3 (PDE3). PDE3 inhibition in platelets and vascular smooth muscle cells (VSMC) was expected to provide an antiplatelet effect and vasodilation. Recent preclinical studies have demonstrated that CLZ also possesses the ability to inhibit adenosine uptake by various cells, a property that distinguishes CLZ from other PDE3 inhibitors, such as milrinone. After extensive preclinical and clinical studies, CLZ has been shown to have unique antithrombotic and vasodilatory properties based upon these novel mechanisms of action. CLZ was approved in 1988 for the treatment of symptoms related to peripheral arterial occlusive disease in Japan (Pletaal®) and in 1999 in the U.S. and in 2001 in the U.K. (Pletal®) for the treatment of intermittent claudication symptoms. Despite its remarkable antiplatelet properties, CLZ is not generally considered an antithrombotic agent in Western countries, perhaps due to the bulk of its antithrombotic preclinical and clinical development being conducted in Japan. In this review, the unique properties of CLZ are reviewed with the focus on CLZ as a unique antiplatelet agent targeting platelets and VSMC, demonstrating synergy with endogenous mediators and showing lowered risk of bleeding risk compared to other antiplatelet drugs.
Keywords: cilostazol, pletaal, adenosine, antithrombotic, intermittent claudication, stroke, and restenosis
Current Pharmaceutical Design
Title: Cilostazol as a Unique Antithrombotic Agent
Volume: 9 Issue: 28
Author(s): Junichi Kambayashi, Yongge Liu, Bing Sun, Yasmin Shakur, Masuhiro Yoshitake and Frank Czerwiec
Affiliation:
Keywords: cilostazol, pletaal, adenosine, antithrombotic, intermittent claudication, stroke, and restenosis
Abstract: Cilostazol (CLZ) was originally developed as a selective inhibitor of cyclic nucleotide phosphodiesterase 3 (PDE3). PDE3 inhibition in platelets and vascular smooth muscle cells (VSMC) was expected to provide an antiplatelet effect and vasodilation. Recent preclinical studies have demonstrated that CLZ also possesses the ability to inhibit adenosine uptake by various cells, a property that distinguishes CLZ from other PDE3 inhibitors, such as milrinone. After extensive preclinical and clinical studies, CLZ has been shown to have unique antithrombotic and vasodilatory properties based upon these novel mechanisms of action. CLZ was approved in 1988 for the treatment of symptoms related to peripheral arterial occlusive disease in Japan (Pletaal®) and in 1999 in the U.S. and in 2001 in the U.K. (Pletal®) for the treatment of intermittent claudication symptoms. Despite its remarkable antiplatelet properties, CLZ is not generally considered an antithrombotic agent in Western countries, perhaps due to the bulk of its antithrombotic preclinical and clinical development being conducted in Japan. In this review, the unique properties of CLZ are reviewed with the focus on CLZ as a unique antiplatelet agent targeting platelets and VSMC, demonstrating synergy with endogenous mediators and showing lowered risk of bleeding risk compared to other antiplatelet drugs.
Export Options
About this article
Cite this article as:
Kambayashi Junichi, Liu Yongge, Sun Bing, Shakur Yasmin, Yoshitake Masuhiro and Czerwiec Frank, Cilostazol as a Unique Antithrombotic Agent, Current Pharmaceutical Design 2003; 9 (28) . https://dx.doi.org/10.2174/1381612033453910
DOI https://dx.doi.org/10.2174/1381612033453910 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
-
TRP Channels as A Newly Emerging Non-Voltage-Gated Ca2+ Entry Channel Superfamily
Current Pharmaceutical Design Adenosine Receptor Ligands in Clinical Trials
Current Topics in Medicinal Chemistry Self-Assembling Peptide Nanofibrous Scaffolds for Tissue Engineering: Novel Approaches and Strategies for Effective Functional Regeneration
Current Protein & Peptide Science Effects of Coenzyme Q and Creatine Supplementation on Brain Energy Metabolism in Rats Exposed to Chronic Cerebral Hypoperfusion
Current Alzheimer Research Marfan Syndrome and Related Heritable Thoracic Aortic Aneurysms and Dissections
Current Pharmaceutical Design Oxidative Stress and Transforming Growth Factor-β<sub>1</sub>-induced Cardiac Fibrosis
Cardiovascular & Hematological Disorders-Drug Targets Growing Collateral Arteries On Demand
Recent Patents on Cardiovascular Drug Discovery A Systematic Review on Levosimendan in Paediatric Patients
Current Vascular Pharmacology Cytokines and Invertebrates: TGF-β and PDGF
Current Pharmaceutical Design Cellular Membrane Microparticles: Potential Targets of Combinational Therapy for Vascular Disease
Current Vascular Pharmacology Persistent Pulmonary Hypertension of the Newborn: Physiology, Hemodynamic Assessment and Novel Therapies
Current Pediatric Reviews Induction of Myocardial Fibrosis and Hypertrophy by Natriuretic Peptides
Vascular Disease Prevention (Discontinued) Granulocyte Colony-Stimulating Factor Attenuates Blood-Brain Barrier Damage and Improves Cognitive Function in Spontaneously Hypertensive Rats
CNS & Neurological Disorders - Drug Targets Tailoring Antiplatelet Therapy: A Step Toward Individualized Therapy to Improve Clinical Outcome?
Current Pharmaceutical Design Fiber-Optic Technologies in Laser-Based Therapeutics: Threads for a Cure
Current Pharmaceutical Biotechnology Hypoperfusion of the Aortic Wall Secondary to Degeneration of Adventitial Vasa Vasorum Causes Abdominal Aortic Aneurysms
Current Drug Targets Algorithms and Criteria for Transcatheter Aortic Valve Replacement Patient Selection: Current Status and Future Trends
Current Pharmaceutical Design MicroRNA-34a Promotes Cardiomyocyte Apoptosis Post Myocardial Infarction Through Down-regulating Aldehyde Dehydrogenase 2
Current Pharmaceutical Design The Roles of MicroRNAs in Heart Diseases: A Novel Important Regulator
Current Medicinal Chemistry Sudden Unexplained Death in Infancy and Long QT Syndrome
Current Pediatric Reviews