Abstract
The evolution of thalidomide as an effective treatment in several neoplasms has led to the search for compounds with increased antiangiogenic and anti-tumor effects, but decreased side-effects. The development of thalidomide analogues which retain the immunomodulatory effects of the parent compound, while minimizing the adverse reactions, brought about a class of agents termed the Immunomodulatory drugs (IMiDs). The IMiDs have undergone significant advances in recent years as evidenced by the recent FDAapprovals of one of the lead compounds, CC-5013 (lenalidomide), for 5q- myelodysplasia and for multiple myeloma (MM). Actimid (CC-4047), another IMiD lead compound, has also undergone clinical testing in MM. Apart from hematologic malignancies, these drugs are actively under investigation in solid tumor malignancies including prostate cancer, melanoma, and gliomas, in which potent activity has been demonstrated. The preclinical and clinical data relating to these analogues, as well as ENMD-0995, are reviewed herein. Encouraging results with these thalidomide analogues brought forth synthesis and screening of additional novel thalidomide analogues in the N-substituted and tetrafluorinated classes, including CPS11 and CPS49. This review also discusses the patents and preclinical findings for these agents.
Keywords: Thalidomide analogues, CC-5013, Lenalidomide, CC-4047, CPS49, CPS11, Multiple Myeloma, Prostate cancer
Recent Patents on Anti-Cancer Drug Discovery
Title: Thalidomide Analogues as Anticancer Drugs
Volume: 2 Issue: 2
Author(s): Jeanny B. Aragon-Ching, Haiqing Li, Erin R. Gardner and William D. Figg
Affiliation:
Keywords: Thalidomide analogues, CC-5013, Lenalidomide, CC-4047, CPS49, CPS11, Multiple Myeloma, Prostate cancer
Abstract: The evolution of thalidomide as an effective treatment in several neoplasms has led to the search for compounds with increased antiangiogenic and anti-tumor effects, but decreased side-effects. The development of thalidomide analogues which retain the immunomodulatory effects of the parent compound, while minimizing the adverse reactions, brought about a class of agents termed the Immunomodulatory drugs (IMiDs). The IMiDs have undergone significant advances in recent years as evidenced by the recent FDAapprovals of one of the lead compounds, CC-5013 (lenalidomide), for 5q- myelodysplasia and for multiple myeloma (MM). Actimid (CC-4047), another IMiD lead compound, has also undergone clinical testing in MM. Apart from hematologic malignancies, these drugs are actively under investigation in solid tumor malignancies including prostate cancer, melanoma, and gliomas, in which potent activity has been demonstrated. The preclinical and clinical data relating to these analogues, as well as ENMD-0995, are reviewed herein. Encouraging results with these thalidomide analogues brought forth synthesis and screening of additional novel thalidomide analogues in the N-substituted and tetrafluorinated classes, including CPS11 and CPS49. This review also discusses the patents and preclinical findings for these agents.
Export Options
About this article
Cite this article as:
Jeanny B. Aragon-Ching , Haiqing Li , Erin R. Gardner and William D. Figg , Thalidomide Analogues as Anticancer Drugs, Recent Patents on Anti-Cancer Drug Discovery 2007; 2 (2) . https://dx.doi.org/10.2174/157489207780832478
DOI https://dx.doi.org/10.2174/157489207780832478 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
Call for Papers in Thematic Issues
Novel anti-cancer drugs in photoimmunotherapy management: from bench to translational research
In recent years, traditional cancer treatments, such as surgery, chemotherapy, and radiation treatment, etc., may damage the pathological tissue and normal cells. The ideal tumor treatment should be noninvasive, eliminating the primary tumor, making the body produce systemic tumor-specific immunity, eliminating metastases, and having less /no side effects. Recent Patents ...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
-
In Vivo Tumor Secretion Probing Via Ultrafiltration and Tissue Chamber:Implication for Anti-Cancer Drugs Targeting Secretome
Recent Patents on Anti-Cancer Drug Discovery Phytochemicals as Adjunctive with Conventional Anticancer Therapies
Current Pharmaceutical Design MicroRNA Functions and Potential Clinical Utility in Glioblastoma
Current Signal Transduction Therapy Xanthohumol: A Metabolite with Promising Anti-Neoplastic Potential
Anti-Cancer Agents in Medicinal Chemistry Benzamides as Melanotropic Carriers for Radioisotopes, Metals, Cytotoxic Agents and as Enzyme Inhibitors
Current Medicinal Chemistry Expression and Function of Organic Cation and Anion Transporters (SLC22 Family) in the CNS
Current Pharmaceutical Design PDGF-D Signaling: A Novel Target in Cancer Therapy
Current Drug Targets Different Treatment Strategies for Pediatric Brain Tumors
Current Pediatric Reviews The Delivery of Biologically Active (Therapeutic) Peptides and Proteins into Cells
Current Medicinal Chemistry Targeting the Akt/PI3K Signaling Pathway as a Potential Therapeutic Strategy for the Treatment of Pancreatic Cancer
Current Medicinal Chemistry Glioblastoma Multiforme and its Cell Interruption
Current Cancer Therapy Reviews Vitamin D Affects the Warburg Effect and Stemness Maintenance of Non- Small-Cell Lung Cancer Cells by Regulating the PI3K/AKT/mTOR Signaling Pathway
Current Cancer Drug Targets Indoleamine 2,3-Dioxygenase, an Emerging Target for Anti-Cancer Therapy
Current Cancer Drug Targets p53: A Guide to Apoptosis
Current Cancer Drug Targets Fluorescence-Guided Malignant Glioma Resections
Current Drug Discovery Technologies Immunostimulatory Oligonucleotides
Recent Patents on Inflammation & Allergy Drug Discovery Radiochemical Evaluation and <i>In Vitro</i> Assessment of the Targeting Ability of a Novel <sup>99m</sup>Tc-HYNIC-RGD for U87MG Human Brain Cancer Cells
Current Radiopharmaceuticals Editorial [Hot Topic: Emerging Therapeutic Targets and Agents for Glioblastoma Therapy – Part I (Guest Editor: Hui-Wen Lo)]
Anti-Cancer Agents in Medicinal Chemistry Targeting the Voltage-Dependent K+ Channels Kv1.3 and Kv1.5 as Tumor Biomarkers for Cancer Detection and Prevention
Current Medicinal Chemistry Pharmacological Aspects of the Enzastaurin-Pemetrexed Combination in Non-Small Cell Lung Cancer (NSCLC)
Current Drug Targets