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
-
Clinical Evaluation of Anti-Obesity Drugs
Current Drug Targets Metformin and Energy Metabolism in Breast Cancer: From Insulin Physiology to Tumour-initiating Stem Cells
Current Molecular Medicine Current Management of In Situ and Invasive Cervical Adenocarcinoma
Current Women`s Health Reviews Regenerative Potential of Stem Cells Derived from Human Exfoliated Deciduous (SHED) Teeth during Engineering of Human Body Tissues
Current Stem Cell Research & Therapy Targeting the Atypical Chemokine Receptor ACKR3/CXCR7: Phase 1 - Phage Display Peptide Identification and Characterization
Current Topics in Medicinal Chemistry The Molecular Mechanisms of TRAIL Resistance in Cancer Cells: Help in Designing New Drugs
Current Pharmaceutical Design Genetic Susceptibility to Endometrial Cancer
Current Women`s Health Reviews From French Paradox to Cancer Treatment: Anti-cancer Activities and Mechanisms of Resveratrol
Anti-Cancer Agents in Medicinal Chemistry Rheumatic Manifestations in Malignancy
Current Rheumatology Reviews Organosulfur Compounds in Cancer Chemoprevention
Mini-Reviews in Medicinal Chemistry Embryonic Morphogenetic Field Induces Phenotypic Reversion in Cancer Cells. Review Article
Current Pharmaceutical Biotechnology Epi-Drugs and Epi-miRs: Moving Beyond Current Cancer Therapies
Current Cancer Drug Targets Genetics of Obesity: What have we Learned?
Current Genomics [6]-gingerol as a Cancer Chemopreventive Agent: A Review of Its Activity on Different Steps of the Metastatic Process
Mini-Reviews in Medicinal Chemistry The Antagonists of Endothelin Receptors: Results and Perspectives
Current Pharmaceutical Analysis The Production of Solid Dosage Forms from Non-Degradable Polymers
Current Pharmaceutical Design The CCL2/CCR2 Axis in the Pathogenesis of HIV-1 Infection: A New Cellular Target for Therapy?
Current Drug Targets Cytoskeletal Alterations that Confer Resistance to Anti-tubulin Chemotherapeutics
Anti-Cancer Agents in Medicinal Chemistry The Adjunctive Value of Diffusion Weighted Imaging in Diagnosis and Follow Up of Uterovaginal Diffuse B-cell Lymphoma: A Case Report and Literature Review
Current Medical Imaging Recent Advances in the Synthesis and Anticancer Activity of Some Molecules Other Than Nitrogen Containing Heterocyclic Moeities
Mini-Reviews in Medicinal Chemistry