Formoterol (Fumarate)

Formoterol

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GPCR/G Protein, Neuronal Signaling

Formoterol fumarate(Foradil) is a potent, selective and long-acting beta2-adrenoceptor agonist.
IC50 Value: 2.1 nM in pregnant C3H/HeN strain mice[5]
Target: beta2 receptor
Budesonide/formoterol in a single inhaler for both maintenance and reliever therapy is now an established therapeutic option for management of inadequately controlled asthma[4].
in vitro:. The long-acting beta(2)-agonist formoterol and the glucocorticoid dexamethasone significantly reduced HRV-induced ERK phosphorylation, Fra-1, and MMP-9 expression in BEAS-2B cells[3].
in vivo: compared the bronchodilatory effects of inhaled budesonide/formoterol (dose: 200 ug and 12 ug respectively) combination with budesonide (200 ug)/salbutamol (200 ug) administered by metered dose inhaler and spacer in children of 5-15 years with mild acute exacerbation of asthma [Modified Pulmonary Index Score (MPIS) between 6-8] in this double-blind, randomized controlled trial. The primary outcome was FEV1 (% predicted) in the two groups at 1, 5, 15, 30, 60 min after administration of the study drug[1]. Fifteen randomized, placebo-controlled clinical trials including COPD patients were evaluated: indacaterol 75 ug once daily (n = 2 studies), indacaterol 150 ug once daily (n = 5), indacaterol 300 ug once daily (n = 4), FOR/BUD 9/160 ug twice daily (n = 2), FOR/BUD 9/320 ug twice daily (n = 2), SAL/FP 50/500 ug twice daily (n = 4), and SAL/FP 50/250 ug twice daily (n = 1)[2].
Clinical trial: Effects of Mometasone Furoate/Formoterol Combination Versus Mometasone Furoate Alone in Persistent Asthmatics (Study P04073) . Phage3