A synthetic glucocorticoid
Fluticasone furoate is a synthetic glucocorticoid.1 It is selective for the glucocorticoid receptor over the mineralocorticoid, progesterone, and androgen receptors in reporter assays (EC50s = 0.03, 23.4, 0.9, and >10,000 nM, respectively), as well as estrogen receptor α (ERα) and ERβ in scintillation proximity assays (EC50s = >10,000 nM for both). Fluticasone furoate reduces LPS-induced increases in TNF-α production in human peripheral blood mononuclear cells (PBMCs) with an EC50 value of 0.12 nM. It decreases S. aureus enterotoxin-induced increases in IFN-γ, IL-2, IL-5, IL-17, and TNF-α levels in patient-derived nasal polyp tissue when used at a concentration of 100 nM.2 Intrathecal administration of fluticasone furoate (30 ?g/animal) reduces ovalbumin-induced increases in bronchoalveolar lavage fluid (BALF) eosinophil infiltration in a rat model of allergic inflammation.1 Formulations containing fluticasone furoate have been used in the treatment of seasonal allergies.
1.Salter, M., Biggadike, K., Matthews, J.L., et al.Pharmacological properties of the enhanced-affinity glucocorticoid fluticasone furoate in vitro and in an in vivo model of respiratory inflammatory diseaseAm. J. Physiol. Lung Cell Mol. Physiol.293(3)L660-L667(2007) 2.Zhang, N., Van Crombruggen, K., Holtappels, G., et al.Suppression of cytokine release by fluticasone furoate vs. mometasone furoate in human nasal tissue ex-vivoPLoS One9(4):e93754(2014)
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