Disease relevance of Nasonex

• Short-term lower leg growth rate in children with rhinitis treated with intranasal mometasone furoate and budesonide [1].
• METHODS: In this double-blind, randomized study patients with seasonal allergic rhinitis (SAR) 12 years of age or older received 200 microg mometasone furoate nasal spray (n = 80) or placebo spray (n = 41) once daily for 2 weeks [2].
• Role of mometasone furoate nasal spray as an adjunct treatment of acute sinusitis [3].
• MF also inhibited ICAM-1 messenger RNA induction by rhinovirus infection in a dose-dependent manner [4].
• The most common adverse events associated with mometasone furoate therapy were nasal irritation and/or burning, headache, epistaxis and pharyngitis [5].

High impact information on Nasonex

• Safety and efficacy of mometasone furoate aqueous nasal spray in children with allergic rhinitis: results of recent clinical trials [6].
• Dose-dependent effects of inhaled mometasone furoate on airway function and inflammation after allergen inhalation challenge [7].
• Inhaled mometasone furoate reduces oral prednisone requirements while improving respiratory function and health-related quality of life in patients with severe persistent asthma [8].
• Mometasone furoate antagonizes AMP-induced bronchoconstriction in patients with mild asthma [9].
• OBJECTIVE: The purpose of this study was to investigate the effect of systemic (hydrocortisone [HC], dexamethasone [DM]) and topical (mometasone furoate [MF]) corticosteroids on rhinovirus-induced ICAM-1 up-regulation [4].

Chemical compound and disease context of Nasonex

• Clinically, both mometasone furoate and fluticasone propionate appear to be well tolerated, to have quick onsets of action, and to be equivalent in efficacy in the treatment of seasonal allergic and perennial rhinitis [10].
• BACKGROUND: Mometasone furoate (Nasonex), in a new once-daily aqueous nasal spray formulation, has been shown to be as effective and well-tolerated as twice-daily beclomethasone dipropionate aqueous nasal spray in treating symptoms of seasonal allergic rhinitis and perennial rhinitis [11].
• We conducted a 6-week randomized, blinded study that compared mometasone furoate 0.1% cream, applied once daily, and hydrocortisone 1.0% cream, applied twice daily, in 48 children with moderate to severe atopic dermatitis [12].
• Mometasone furoate-salicylic acid ointment provides more effective treatment of moderate-to-severe psoriasis than does mometasone furoate ointment alone and is safe and well tolerated [13].
• The effects of mometasone furoate on experimental allergic rhinitis in rats were studied in comparison with that of fluticasone propionate [14].

Biological context of Nasonex

• BACKGROUND: Mometasone furoate (MF) aqueous nasal spray is a potent intranasal glucocorticoid with low systemic bioavailability [1].
• The objective measures of eosinophil, basophil, and neutrophil counts and mucociliary clearance were significantly better in mometasone furoate- than in placebo-treated patients [2].
• Human receptor kinetics, tissue binding affinity, and stability of mometasone furoate [15].
• RESULTS: At the end point, the mean increase in forced expiratory volume in 1 second relative to baseline for the mometasone furoate DPI group of 0.43 L (16.8%) was significantly greater than that for the placebo group of 0.16 L (6.0%) (P < .01) [16].
• Morning peak expiratory flow, forced vital capacity, and forced expiratory flow between 25% and 75% also significantly improved with mometasone furoate DPI treatment relative to placebo (P < .01) [16].

Anatomical context of Nasonex

• OBJECTIVE: The purpose of this study was to compare the systemic bioactivity of aqueous formulations of intranasal budesonide, mometasone furoate (MF), and triamcinolone acetonide (TAA) in terms of adrenal, bone, and white blood cell markers [17].
• Relative lack of systemic effects of mometasone furoate on Langerhans cells of mice after topical administration as compared with other glucocorticosteroids [18].
• The binding affinities of mometasone furoate (MF), its metabolites and related compounds for the glucocorticoid receptor of rat epidermis and dermis were measured [19].
• Interleukin (IL)-1 beta caused a significant increase in NF-kappa B-mediated granulocyte/macrophage colony stimulating factor (GM-CSF) release, which was inhibited by the glucocorticoid mometasone furoate (MF) (EC(50)=2 x 10(-11) M) [20].
• These results extend the profile of the anti-inflammatory activity of mometasone furoate to lung fibroblast functions involved in airway inflammation and remodeling [21].

Associations of Nasonex with other chemical compounds

• Overall, the newer corticosteroids, including mometasone furoate (MF), beclomethasone dipropionate, and budesonide have an improved risk-benefit ratio compared with older cortico-steroids and are now considered the drug of choice for pediatric allergic rhinitis [22].
• The rank order of potency of GC for inhibition of the expression of VCAM-1 in BEAS-2B cells was MF congruent with FP >> BUD > TAA > HC congruent with BDP [23].
• Similarly, within-treatment statistically significant improvements were produced by mometasone furoate but not by placebo sprays for levels of eosinophilic cationic protein, tryptase and albumin, NAR, and odor identification [2].
• Although progesterone, the natural ligand of the progesterone receptor (PR), has a hydrogen atom at the 17alpha position, other potent steroid agonists such as norethindrone and mometasone furoate have larger substituents at this position that are accommodated by the PR ligand binding pocket [24].
• When administered intranasally, mometasone furoate is reported to have comparable relative systemic bioavailability to that of fluticasone propionate (mean plasma area under the curve, 123 pmol x h/L vs 112 pmol x h/L, respectively) [25].

Gene context of Nasonex

• Within-treatment comparisons suggested that mometasone furoate reduced the antigen-induced late-phase response for IL-6, IL-8, and eosinophils compared with pretreatment [26].
• CONCLUSION: These results suggest that the clinical activity of mometasone furoate nasal spray in seasonal allergic rhinitis is likely due, in part, to a reduction in the levels of histamine in nasal secretions related to the early phase response, and reductions in IL-6, IL-8, and eosinophils during the late phase response [26].
• There were increased levels of steady-state mRNA for interleukin-4, interleukin-5, and to a lesser extent, gamma-interferon in the lungs of sensitized mice after ovalbumin challenge and pretreatment with mometasone furoate reduced the steady-state mRNA levels of these cytokines [27].
• A placebo- and active-controlled randomized trial of prophylactic treatment of seasonal allergic rhinitis with mometasone furoate aqueous nasal spray [28].
• METHODS: A randomised, double blind, crossover trial of placebo and mometasone furoate (800 microg/day), each given for 6 weeks with a 4 week washout period, was performed in subjects with COPD treated with bronchodilator therapy only [29].

Analytical, diagnostic and therapeutic context of Nasonex

• Recent randomised, double-blind, multicentre trials have assessed the efficacy of mometasone furoate delivered by dry powder inhaler over 12 weeks in adults and adolescents with mild to severe persistent asthma [30].
• STUDY OBJECTIVES: To investigate the potential for mometasone furoate (MF) to exert systemic effects following administration by dry powder inhaler (DPI) or metered-dose inhaler (MDI) [31].
• METHODS: Fourteen patients with perennial allergic rhinitis (PAR) were randomized to receive 2 weeks treatment with placebo (PL) or 200 microg intranasal mometasone furoate (MF) once daily in a randomized single-blind crossover study [32].
• Bioavailability and metabolism of mometasone furoate following administration by metered-dose and dry-powder inhalers in healthy human volunteers [33].
• The structure of an unusual rearrangement product obtained during the production of mometasone furoate (Sch 32088) was assigned on the basis of NMR and X-ray crystallography data [34].

References