Abstract
Among the drugs targeting microtubule functions by interfering with tubulin subunits, epothilones represent a class of anticancer agents which recently entered clinical development. Although epothilones share mechanisms of action similar to taxanes, they have non-overlapping mechanisms of resistance; in particular, while overexpression of class III β-tubulin plays a major role in taxane resistance, epothilones display their highest efficacy in class III β-tubulin overexpressing malignancies. Three compounds belonging to this family (patupilone, ixabepilone and sagopilone), have been actively investigated in clinical trials, and some of them are at an advanced stage of development.
This review provides a comprehensive analysis of the available literature on epothilones, focusing on their clinical development and potential as an additional weapon in the arsenal against tumors.
Keywords: Epothilones, cytoskeleton, class III β-tubulin, cell survival, ovarian cancer, anticancer agents, taxane resistance, tumors, p-glycoprotein, microtubule
Current Pharmaceutical Design
Title:Novel Drugs Targeting Microtubules: the Role of Epothilones
Volume: 18 Issue: 19
Author(s): Gabriella Ferrandina, Marisa Mariani, Mirko Andreoli, Shohreh Shahabi, Giovanni Scambia and Cristiano Ferlini
Affiliation:
Keywords: Epothilones, cytoskeleton, class III β-tubulin, cell survival, ovarian cancer, anticancer agents, taxane resistance, tumors, p-glycoprotein, microtubule
Abstract: Among the drugs targeting microtubule functions by interfering with tubulin subunits, epothilones represent a class of anticancer agents which recently entered clinical development. Although epothilones share mechanisms of action similar to taxanes, they have non-overlapping mechanisms of resistance; in particular, while overexpression of class III β-tubulin plays a major role in taxane resistance, epothilones display their highest efficacy in class III β-tubulin overexpressing malignancies. Three compounds belonging to this family (patupilone, ixabepilone and sagopilone), have been actively investigated in clinical trials, and some of them are at an advanced stage of development.
This review provides a comprehensive analysis of the available literature on epothilones, focusing on their clinical development and potential as an additional weapon in the arsenal against tumors.
Export Options
About this article
Cite this article as:
Ferrandina Gabriella, Mariani Marisa, Andreoli Mirko, Shahabi Shohreh, Scambia Giovanni and Ferlini Cristiano, Novel Drugs Targeting Microtubules: the Role of Epothilones, Current Pharmaceutical Design 2012; 18 (19) . https://dx.doi.org/10.2174/138161212800626238
DOI https://dx.doi.org/10.2174/138161212800626238 |
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
-
Current Concepts for the IND-Directed Development of Microbicide Products to Prevent the Sexual Transmission of HIV
Current Topics in Medicinal Chemistry Oxidative Stress and Mitochondrial Dysfunction in Type 2 Diabetes
Current Pharmaceutical Design Phytoestrogens: Pharmacological and Therapeutic Perspectives
Current Drug Targets From Bacteria to Antineoplastic: Epothilones A Successful History
Anti-Cancer Agents in Medicinal Chemistry Berberine as a Promising Safe Anti-Cancer Agent- Is there a Role for Mitochondria?
Current Drug Targets Polo-Like Kinases (Plks) are Prognostic Markers for Gynecologic Malignancies
Current Women`s Health Reviews Nanocellulose-based Delivery Systems and Cervical Cancer: Review of the Literature
Current Pharmaceutical Design Peptide-Receptor Ligands and Multivalent Approach
Anti-Cancer Agents in Medicinal Chemistry Inflammation and Thrombophilia in Pregnancy Complications: Implications for Risk Assessment and Clinical Management
Cardiovascular & Hematological Disorders-Drug Targets Postmenopausal Hormone Therapy
Current Women`s Health Reviews Melanoma Immunotherapy: Past, Present, and Future
Current Pharmaceutical Design HPC Analysis of Multiple Binding Sites Communication and Allosteric Modulations in Drug Design: The HSP Case Study
Current Drug Targets Paclitaxel Formulations: Challenges and Novel Delivery Options
Current Drug Delivery Lycopene: A Review of Its Potential as an Anticancer Agent
Current Medicinal Chemistry - Anti-Cancer Agents Targeting Kinases in Cancer Therapies: Adverse Effects on Blood Platelets
Current Pharmaceutical Design Leptin as Clinical Target
Recent Patents on Inflammation & Allergy Drug Discovery Molecular Bases of Liver Cancer Refractoriness to Pharmacological Treatment
Current Medicinal Chemistry Review on Pharmacological and Phytochemical Prospects of Traditional Medicinal Plant: <i>Persicaria hydropiper</i> (Smartweed)
Current Topics in Medicinal Chemistry 1α ,25(OH)2-Vitamin D3 and 17β-Estradiol: Two Steroid Partners Acting in Skeletal Muscle
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Interactions of the Aryl Hydrocarbon Receptor with Inflammatory Mediators:Beyond CYP1A Regulation
Current Drug Metabolism