Fluticasone Furoate

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 µg/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.

WARNING This product is not for human or veterinary use.

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 disease. Am. 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-vivo. PLoS One 9(4):e93754, (2014).