Fluticasone Propionate

Fluticasone propionate is a synthetic corticosteroid and glucocorticoid receptor agonist.¹ It inhibits AP-1-mediated transcription in a transrepression assay using ChaGo-K-1 cells (IC₅₀ = 0.04 nM).¹ Fluticasone propionate selectively binds to the glucocorticoid receptor (IC₅₀ = 0.0009 µM) over the progesterone, mineralocorticoid, and androgen receptors (IC₅₀s = 0.021, 0.149, and >10 µM, respectively), as well as estrogen receptor α (ERα) and ERβ (IC₅₀s = >10 µM for both). It increases apoptosis of T cells isolated from human peripheral blood in a concentration-dependent manner and induces spontaneous apoptosis of primary human eosinophils (EC₅₀ = 3.7 nM).^2,3 Fluticasone propionate completely inhibits congestion in a guinea pig model of allergic rhinitis induced by ovalbumin when administered as a 0.5 mg/ml solution at 20 µl/nostril.⁴ It reduces ovalbumin-induced increases in IL-4 in nasal lavage fluid in the same model. Fluticasone propionate also potentiates voltage-dependent potassium channel 1 (K_v1) currents in an inside-out patch-clamp assay (EC₅₀ = 37 nM).⁵ Formulations containing fluticasone propionate have been used in the treatment of allergic and non-allergic rhinitis.

WARNING This product is not for human or veterinary use.

1. Hemmerling, M., Nilsson, S., Edman, K., et al. Selective nonsteroidal glucocorticoid receptor modulators for the inhaled treatment of pulmonary diseases. J. Med. Chem. 60(20), 8591-8605 (2017).

2. Pace, E., Gagliardo, R., Melis, M., et al. Synergistic effects of fluticasone propionate and salmeterol on in vitro T-cell activation and apoptosis in asthma. J. Allergy. Clin. Immunol. 114(5), 1216-1223 (2004).

3. Zhang, X., Moilanen, E., and Kankaanranta, H. Enhancement of human eosinophil apoptosis by fluticasone propionate, budesonide, and beclomethasone. Eur. J. Pharmacol. 406(3), 325-332 (2000).

4. Bahekar, P.C., Shah, J.H., Ayer, U.B., et al. Validation of guinea pig model of allergic rhinitis by oral and topical drugs. Int. Immunopharmacol. 8(11), 1540-1551 (2008).

5. Pan, Y., Levin, E.J., Quick, M., et al. Potentiation of the K_v1 family K⁺ channel by cortisone analogues. ACS Chem. Biol. 7(10), 1641-1646 (2012).