Asthma is a common chronic inflammatory disease of the respiratory system that affects approximately 22 million people in US. It has been classified as a complex genetic condition that is determined by the interaction of numerous genes along with environmental factors.
Asthma can be characterized by hyper-reactivity of the airways and the propensity of airways to constrict in response to various stimuli. This leads to symptoms such as shortness of breath, chest tightening, coughing and wheezing. Triggers of asthma 'attacks' include common colds, exercise, allergens (irritants such as smoke, fumes and dust, along with pollutants).
Cytokine signaling contributes greatly to asthma and the associated airway obstruction. Cytokines such as IL-4 cause the secretion of mucus and the onset of allergic inflammatory responses including the development of T helper cells. There are also numerous structural changes that occur in asthmatic airways and collectively lead to 'remodeling'. These include deposition of matrix proteoglycan and collagen in the submucosa, epithelial mucus metaplasia and a proliferation of microvessels and nerves.
Treatment for asthma includes bronchodilator therapy or anti-inflammatory drugs, particularly corticosteroid inhalation. Corticosteroids act by blocking the immune reaction to an allergen, decreasing inflammation by inhibiting cells such as mast cells, eosinophils and basophils.
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A potent and specific LTD4 receptor antagonist with Ki of 0.22 nM; effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors; also is an inhibitor of multidrug resistance protein-1 (MRP1) mediated transportorally active.
Valategrast is a potent, α4β1 (VLA-4) and α4β7 dual antagonist.
Valategrast hydrochloride is a potent, α4β1 (VLA-4) and α4β7 dual antagonist.
Gemilukast (ONO-6950, ONO6950) is a potent, orally active, dual CysLT1 and CysLT2 antagonist with IC50 of 1.7 and 25 nM against human CysLT1 and human CysLT2, respectively; antagonized intracellular calcium signaling via human and guinea pig CysLT1 and CysLT2 receptors with IC50 values of 1.7 and 25 nM, respectively (human receptors) and 6.3 and 8.2 nM, respectively (guinea pig receptors); attenuated CysLT1-mediated bronchoconstriction and airway vascular hyperpermeability induced by LTD4 in normal guinea pigs (1 or 0.3 mg/kg, p.o.), strongly inhibited this asthmatic response to the level attained by combination therapy with montelukast and BayCysLT2RA.
A potent and reversible S-Nitrosoglutathione reductase (GSNOR) inhibitor with IC50 of 20 nM; reduces bronchoconstriction and pulmonary inflammation in a mouse model of asthma and demonstrates an acceptable safety profile.
AZD-7594 (AZ-13189620) is a potent, nonsteroidal, selective glucocorticoid receptor modulator (SGRM) with binding IC50 of 0.9 nM, shows no affinity for AR, PR, MR and ERα/β; demonstrates cell potentcy with IC50 of 55 nM (repression of AP-1 dependent transcription), inhibits LPS-stimulated TNF-α production in human PBMC with IC50 0.43 nM; potently inhibits lung edema in a rat model of allergic airway inflammation with inhaled EC50 of 130 uM/Kg.
CJ-13610 is a potent 5-Lipoxygenase (5-LO) inhibitor that suppresses 5-LO product formation with IC50 of 70 nM; demonstrates antihyperalgesic activity in inflammatory pain models including the acute carrageenan model and the chronic inflammatory model.
CDP-840 (CDP840;L-765527) is a potent and selective PDE4 inhibitor with IC50 of 4-45 nM for PDE 4 extracted from tissues or recombinant PDE 4 isoforms expressed in yeast; shows no effect for PDE-1, 2, 3, 5, and 7 (IC50>100 uM), exhibits no significant selectivity in inhibiting human recombinant isoenzymes PDE-4A, B, C or D and is equally active against the isoenzymes lacking UCR1 (PDE-4B2 and PDE-4D2); causes a dose-dependent reduction of IL-5-induced pleural eosinophilia in rats (ED50=0.03 mg/kg); prevents antigen-induced eosinophilia and bronchoconstriction; orally active.
ABT-080 is a potent FLAP inhibitor that inhibits ionophore-stimulated LTB(4) formation with with IC50 of 20 nM; selectively inhibits zymosan-stimulated mouse peritoneal macrophages producing LTC(4) with IC50 of 0.16 nM, 9000-fold selectivity over PGE(2) producing; demonstrates leukotriene inhibition with oral dosing in a rat pleural inflammation model.
A potent, orally available inhibitor of TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with IC50 of 1 nM; inhibits phosphorylation of ZAP70 at Tyr319 and of CD3ζ at Tyr142; inhibits TCR triggering-induced gene expression (1093 genes), including genes that are relevant for inflammatory T cell responses (cytokines IL-17A, IL-2, IL-6R and IL-18R1); attenuates the severity of skin inflammation in a psoriasis model as well as of lung inflammation in an asthma model.
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