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
-
Pleiotropic Effect of Statins as Antioxidants on Cardiac Hypertrophy
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Epigenetic and Disease Targets by Polyphenols
Current Pharmaceutical Design Hypertension in Children After Renal Transplantation
Current Hypertension Reviews Cell Cycle Dependent Regulation of Intracellular Calcium Concentration in Vascular Smooth Muscle Cells: A Potential Target for Drug Therapy
Current Drug Targets - Cardiovascular & Hematological Disorders Cyano Acrylate Polymers in Medical Applications
Recent Patents on Materials Science Antioxidant Activity of Plant Phenols: Chemical Mechanisms and Biological Significance
Current Organic Chemistry An Arylidene-Thiazolidinedione Derivative, GPU-4, without PPARγ Activation, Reduces Retinal Neovascularization
Current Neurovascular Research Mitochondria: the Headquarters in Ischemia-Induced Neuronal Death
Central Nervous System Agents in Medicinal Chemistry Pharmacological and Cellular Therapies to Prevent Restenosis after Percutaneous Transluminal Angioplasty and Stenting
Cardiovascular & Hematological Agents in Medicinal Chemistry Animal Models of Systemic Sclerosis
Current Pharmaceutical Design Recent Advances of Poly(ether-ether) and Poly(ether-ester) Block Copolymers in Biomedical Applications
Current Drug Metabolism Vascular Resection in Pancreaticoduodenectomy: Is it Worthwhile?
Current Drug Targets Folate Based Radiopharmaceuticals for Imaging and Therapy of Cancer and Inflammation
Current Pharmaceutical Design Chlorella vulgaris: A Multifunctional Dietary Supplement with Diverse Medicinal Properties
Current Pharmaceutical Design Statin Therapy
Current Pharmaceutical Design Gene Therapy in In Vivo Isolated Perfusion Models
Current Gene Therapy Therapeutic Exploitation of Endogenous Anti-Inflammatory Mechanisms:Old and New Leads
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Ischemic Colitis: Current Diagnosis and Treatment
Current Drug Targets Neuritin, A Neurotrophic Factor in Nervous System Physiology
Current Medicinal Chemistry Chemical and Bioactive Diversities of the Genus Chaetomium Secondary Metabolites
Mini-Reviews in Medicinal Chemistry