Asthma Therapeutics: New Treatment Options And Emerging Drug Discovery Targets
LeadDiscovery
April 1, 2003 SKU: LD1330849
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It has proved to be very difficult to develop new classes of anti-asthma therapy, partly because existing drugs, especially inhaled corticosteroids and combination inhalers, are so effective. New classes of therapeutics are expected to allow for oral treatment which will further improve patient compliance and possibly offer improved efficacy to treatment resistant patients. This report evaluates over 30 major therapeutic targets currently under investigation offering an expert view of the potential and the limitations of each target. Such an evaluation is important to the success of drug discovery efforts since the asthma arena is characterized by targets that have initially offered promise but have failed to meet expectations in the clinic.
The only new class of drug developed in the last 30 years are anti-leukotrienes, which are far less effective than inhaled corticosteroids. New bronchodilators have been difficult to develop as new drugs are less effective than b2-agonists and have more side effects. Mediator antagonists have proved disappointing as so many mediators are involved in asthma.
A number of emerging targets are however especially promising including IL-13, TACE inhibitors, IL-10, dissociated steroids, PDE4, IgE and vaccine therapies. Proof of concept data and expert opinion on each of these targets is offered in this report. Over 30 other targets are also discussed even though they have yet to be adequately investigated. For each of these, available data is provided and the risks associated with these targets are analyzed in order to guide future research.
The report concludes with a listing of therapeutics on the market or in development. Profiles are provided for those in advanced development or those that have been launched; a strategic analysis is then provided underlining those targets perceived to be the most promising and how these targets should be exploited.
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- INTRODUCTION
- BACKGROUND INFORMATION
- The increasing prevalence of asthma
- The role of genetic factors in asthma
- The role of infective agents in asthma
- Asthma as an inflammatory disease
- Airway remodelling
- Airway hyperresponsiveness
- Anti-inflammatory mechanisms
- Transcription factors
- MODERN ASTHMA MANAGEMENT
- Asthma guidelines
- Inhaled corticosteroids
- Add-on therapies
- Anti-leukotrienes
- NEW BRONCHODILATORS
- ß2-Agonists.
- Drugs which increase cyclic AMP
- Drugs which increase cyclic GMP
- Selective anticholinergics
- K+ channel openers
- MEDIATOR ANTAGONISTS
- Leukotriene modifiers
- Prostaglandin inhibitors
- Endothelin antagonists
- Antioxidants
- Purine receptor modulators
- Nitric Oxide
- Tryptase inhibitors
- CYTOKINES AND CYTOKINE INHIBITORS
- Strategies for inhibiting cytokines
- Inhibition of Th2 cytokines
- Anti-IL-5
- Anti-IL-4
- Anti-IL-13
- Anti-IL-9
- Anti-IL-25
- Inhibition of proinflammatory cytokines
- Anti-inflammatory cytokines
- IL-10
- Interferons
- IL-12
- IL-18
- CHEMOKINE INHIBITORS
- CCR3 inhibitors
- inhibitors
- Other CCR inhibitors
- NEW ANTI-INFLAMMATORY DRUGS
- Novel corticosteroids
- Soft steroids
- Ciclesonide
- Dissociated corticosteroids
- Phosphodiesterase-4 inhibitors
- Transcription factor inhibitors
- NF-AT/calcineurin inhibitors
- GATA-3 inhibitors
- MAP kinase inhibitors
- p38 MAP kinase inhibitors
- JNK inhibitors
- Tyrosine kinase inhibitors
- Syk kinase inhibitors
- Lyn kinase inhibitors
- EGF receptor kinase
- Immunomodulators
- Th2 cell inhibitors
- Cell adhesion blockers
- SPECIFIC ANTI-ALLERGIC DRUGS
- Cromones
- Furosemide
- Co-stimulation inhibitors
- Anti-IgE
- PREVENTIVE STRATEGIES IN ASTHMA
- Specific allergen vaccination (immunotherapy)
- Peptide immunotherapy
- Vaccination
- CgP oligonucleotides
- GENE THERAPY
- Gene transfer
- Antisense oligonucleotides
- THE ASTHMA THERAPEUTICS MARKET
- ASTHMA THERAPEUTICS DEVELOPMENT
- Full listing of therapeutics on the market or in developement aranged by originating company, phase of development, pharmacology
- Therapeutic profiles of marketed products
- zileuton
- pseudoephedrine
- (R)-salbutamol
- bambuterol
- formoterol
- pirbuterol
- reproterol
- salbutamol
- salmeterol + fluticasone
- suplatast tosilate
- epinastine
- oxatomide
- amlexanox
- tranilast
- Broncostat
- Alergim PG
- TO-194
- pranlukast
- montelukast sodium
- zafirlukast
- cyclidrol
- letosteine
- flutropium bromide
- budilast
- aminophylline
- doxofylline
- theophylline
- triamcinolone
- beclometasone
- budesonide
- deflazacort
- fluticasone
- methylprednisolone
- budesonide
- beclometasone
- budesonide
- flunisolide
- mometasone
- budesonide + formoterol
- seratrodast
- Therapeutic profiles of products in advanced clinical development
- salbutamol
- formoterol
- omalizumab
- ciclesonide
- budesonide
- flunisolide
- israpafant
- (R,R)-formoterol
- ebastine
- roflumilast
- CONCLUSIONS & STRATEGIC ADVICE
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