Abstract
The discovery of the two isoenzymes COX-1 and COX-2 and the knowledge of their function, localisation and regulation has initiated the development of COX-2 selective inhibitors (coxibs). Inducible COX-2 at the peripheral site of inflammation has been detected in the early 1990s, the involvement of recently detected spinal COX-2 has led to new insights into mechanisms of pain and may explain analgesic and antipyretic properties of COX-2 selective inhibitors. The coxibs rofecoxib and celecoxib have been introduced into therapy and seem to offer some advantages over the classical non-selective NSAIDs. The search for new COX-2 inhibitors is going on, the development of etoricoxib and lumiracoxib is a step ahead concerning efficacy, tolerability and safety. Until today COX-2 selective inhibitors have found their place in therapy of arthritis, osteoarthritis, dysmenorrhea and acute pain. A new paradigm in pain therapy seems to justify their use in perioperative settings in a preemptive or multimodal therapeutical strategy. In the future COX-2 selective inhibitors as opioid sparing agents could become an important tool in pain therapy. Even a therapeutical benefit of COX-2 selective inhibitors in the treatment of Alzheimers Disease or in the prevention or treatment of colorectal or prostate cancer is presently intensely investigated. Recently some authors reported on COX-3, a splicing variant of COX-1. If COX-3 really represents the target for acetaminophen must be called into question.
Keywords: cox-1, cox-2, mechanism of pain, spinal cord cox-2, preemptive and multimodal analgesia, lox, coxinhibitors, cox-2 inhibitors in alzheimers disease and cancer
Current Medicinal Chemistry
Title: Novel Insights and Therapeutical Applications in the Field of Inhibitors of COX-2
Volume: 11 Issue: 24
Author(s): W. Kiefer and G. Dannhardt
Affiliation:
Keywords: cox-1, cox-2, mechanism of pain, spinal cord cox-2, preemptive and multimodal analgesia, lox, coxinhibitors, cox-2 inhibitors in alzheimers disease and cancer
Abstract: The discovery of the two isoenzymes COX-1 and COX-2 and the knowledge of their function, localisation and regulation has initiated the development of COX-2 selective inhibitors (coxibs). Inducible COX-2 at the peripheral site of inflammation has been detected in the early 1990s, the involvement of recently detected spinal COX-2 has led to new insights into mechanisms of pain and may explain analgesic and antipyretic properties of COX-2 selective inhibitors. The coxibs rofecoxib and celecoxib have been introduced into therapy and seem to offer some advantages over the classical non-selective NSAIDs. The search for new COX-2 inhibitors is going on, the development of etoricoxib and lumiracoxib is a step ahead concerning efficacy, tolerability and safety. Until today COX-2 selective inhibitors have found their place in therapy of arthritis, osteoarthritis, dysmenorrhea and acute pain. A new paradigm in pain therapy seems to justify their use in perioperative settings in a preemptive or multimodal therapeutical strategy. In the future COX-2 selective inhibitors as opioid sparing agents could become an important tool in pain therapy. Even a therapeutical benefit of COX-2 selective inhibitors in the treatment of Alzheimers Disease or in the prevention or treatment of colorectal or prostate cancer is presently intensely investigated. Recently some authors reported on COX-3, a splicing variant of COX-1. If COX-3 really represents the target for acetaminophen must be called into question.
Export Options
About this article
Cite this article as:
Kiefer W. and Dannhardt G., Novel Insights and Therapeutical Applications in the Field of Inhibitors of COX-2, Current Medicinal Chemistry 2004; 11 (24) . https://dx.doi.org/10.2174/0929867043363668
DOI https://dx.doi.org/10.2174/0929867043363668 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...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
-
Inflammation and Cancer: When NF-κB Amalgamates the Perilous Partnership
Current Cancer Drug Targets Therapeutic Targeting of Cancers with Loss of PTEN Function
Current Drug Targets Indolin-2-one Derivatives: Theoretical Studies Aimed at Finding More Potent Aurora B Kinase Inhibitors
Letters in Drug Design & Discovery Mechanisms of ERK1/2 Regulation by Seven-Transmembrane-Domain Receptors
Current Pharmaceutical Design Diagnostic Methods in the Detection of Prostate Cancer: Prospective Observational Study
Current Medical Imaging Potential Adverse Effects Associated with Inhibition of p38α/β MAP Kinases
Current Topics in Medicinal Chemistry Is Type D Personality Here to Stay? Emerging Evidence Across Cardiovascular Disease Patient Groups
Current Cardiology Reviews Imaging Cellular Receptors in Breast Cancers: An Overview
Current Pharmaceutical Biotechnology The Linkage Between Inflammation and Immune Tolerance: Interfering with Inflammation in Cancer
Current Cancer Drug Targets Metabolic Control of Glia-Mediated Neuroinflammation
Current Alzheimer Research Synthesis, Cytotoxicity, Antioxidant and Antimicrobial Activity of Indole Based Novel Small Molecules
Letters in Drug Design & Discovery Glycine Transporter-1: A New Potential Therapeutic Target for Schizophrenia
Current Pharmaceutical Design LAT1 Targeted Delivery of Methionine Based Imaging Probe Derived from M(III) Metal Ions for Early Diagnosis of Proliferating Tumours using Molecular Imaging Modalities
Current Cancer Drug Targets β3-Adrenoceptor Control of Lower Genitourinary Tract Organs and Function in Male: An Overview
Current Drug Targets Subject Index to Volume 4
Current Gene Therapy Natural Products and their (Semi-)Synthetic Forms in the Treatment of Migraine: History and Current Status
Current Medicinal Chemistry Diabetes, Cancer and Treatment – A Mini-Review
Current Drug Safety Advancements within Modern Machine Learning Methodology: Impacts and Prospects in Biomarker Discovery
Current Medicinal Chemistry Co-delivery Strategies Based on Multifunctional Nanocarriers for Cancer Therapy
Current Drug Metabolism Preclinical Evaluation of a Monoclonal Antibody (3C6) Specific for Prostate-Specific Membrane Antigen
Current Radiopharmaceuticals