Drug Evaluation

Efficacy and safety of mometasone furoate nasal

spray in allergic rhinitis, acute rhinosinusitis and
nasal polyposis
Seasonal and perennial allergic rhinitis, acute rhinosinusitis and nasal polyposis are common inflammatory
conditions of the airway that markedly impair patient health and quality of life. Treatment guidelines for
each of these conditions recommend intranasal corticosteroids, which help to alleviate symptoms by reducing
inflammation. One of the most extensively studied intranasal corticosteroids for these conditions is
mometasone furoate nasal spray (MFNS). In more than 20 clinical trials, MFNS has been shown to reduce
both objective and subjective signs of inflammation and promotes rapid resolution of nasal, sinus and ocular
symptoms in adults, adolescents and children. MFNS is well-tolerated and local adverse events are generally
mild and self-limiting, usually resolving without discontinuation of therapy. The low systemic bioavailability
(<0.1%) and high first-pass metabolism of MFNS also reduce its risk for systemic adverse events.

KEYWORDS: allergic rhinitis n congestion n intranasal corticosteroids n mometasone Catherine B Small1 &
furoate n nasal allergies n nasal polyposis n rhinosinusitis Ariel Teper2

Author for correspondence:
Seasonal and perennial allergic rhinitis, acute perennial allergic rhinitis, acute rhinosinusitis Division of Infectious Diseases,
rhinosinusitis and nasal polyposis are inflam- and nasal polyposis. Department of Medicine,
matory conditions of the nose and/or sinuses New York Medical College,
that produce bothersome symptoms and mark- Allergic rhinitis Westchester Medical Center,
edly affect patients quality of life [13] . These Allergic rhinitis affects approximately 13% Munger Pavilion, Room 245,
diseases frequently coexist, suggesting that each of the American population and 1729% of Valhalla, NY 10595, USA
may be a manifestation of an inflammatory pro- the European population, with the prevalence Tel.: +1 914 493 8865
cess within the continuous airway [35] . Clinical varying widely in different regions [5,28,29,201] . Fax: +1 914 594 4530
treatment guidelines for each of these condi- It is the most prevalent chronic allergic disease [email protected]
tions conclude that research evidence supports among children [202] , affecting approximately 2
Schering-Plough Research
treatment with an intranasal corticosteroid [59] . 40% by the age of 6 years [30] . Allergic rhinitis Institute, 2000 Galloping Hill
One of the most extensively investigated is generally classified as either seasonal or peren- Road, Kenilworth, NJ 07033,
intranasal corticosteroids for inflammatory nial [5,8,9] , and, as per the Allergic Rhinitis and USA
diseases of the nose and sinuses is mometa- its Impact on Asthma guidelines, it is now fur-
sone furoate nasal spray (MFNS). Mometasone ther subdivided into intermittent or persistent
furoate is a potent 17-heterocyclic cortico- disease [5,9] . Seasonal allergic rhinitis is an IgE-
steroid formulated in an aqueous suspension mediated response to outdoor seasonal allergens
for intranasal use with a metered-dose, manual such as molds or pollen [5,10] . Perennial allergic
pump nasal spray (FIGURE 1) [10] . In vitro testing rhinitis comprises a number of conditions that
has shown that mometasone furoate has a high result from either continuous or intermittent
binding affinity for the glucocorticoid recep- exposure to allergens, most commonly indoor
tor and is a potent stimulator of glucocorticoid allergens such as dust mites, molds, insects (cock-
receptor-mediated gene expression [11] . Owing roaches) and animal dander [5,9] . Both seasonal
to its anti-inflammatory properties, MFNS has and perennial allergic rhinitis are characterized
been proven to be effective for the prophylaxis by extensive infiltration of the nasal mucosa
and treatment of seasonal allergic rhinitis [1216] , by inflammatory cells, such as eosinophils and
the treatment of perennial allergic rhinitis [1719] , basophils, as well as the release of inflammatory
as an adjunct to antibiotics in the treatment of mediators such as histamine, prostaglandins and
acute bacterial rhinosinusitis [20,21] or as mono- leukotrienes from mast cells [31] .
therapy in uncomplicated cases of acute rhi- Patients with allergic rhinitis typically report
nosinusitis [22,23] , and the treatment of nasal nasal itching, sneezing, rhinorrhea, postnasal
polyposis [2427] . drainage and nasal congestion [2] . Ocular symp-
The purpose of this review is to summarize toms which may also be present include itching,
the efficacy and safety of MFNS for seasonal and burning, tearing and redness of the sclera and

10.2217/THY.09.6 2009 Future Medicine Ltd Therapy (2009) 6(3), 393406 ISSN 1475-0708 393
Drug Evaluation Small & Teper

CH2Cl
n Treatment of allergic rhinitis
O Since intranasal corticosteroids are considered
C O
CH3 to be the most effective medications available
O C O
HO for the treatment of allergic rhinitis, as stated
CH3 in the guidelines, they are recommended as
CH3
first-line therapy, especially in patients with
Cl moderate-to-severe, persistent symptoms and
impaired quality of life; nasal congestion
O
and/or blockage; or continuing symptoms
despite treatment with histamine H1-receptor
Figure 1. Mometasone furoate.
antagonists (FIGURE 2) [9,33,202] .
Mometasone furoate nasal spray is one of
ocular mucosa [9,12] . Although allergic rhinitis is the most intensively studied intranasal cortico-
often considered a minor condition [32,33] , it can steroids for allergic rhinitis. More than 20 clini-
substantially impair the ability of patients to func- cal trials involving more than 6000 adults, ado-
tion at work [34] , in social situations [737,201,202] or lescents and children have assessed its efficacy
at school [38,39] . These patients also have a lower and safety [1215,17,4350] . Ten of these were ran-
quality of life and a greater degree of depression domized, double-blind, placebo-controlled trials
than those without allergic rhinitis [3740] . The evaluating the use of MFNS to treat the nasal
losses in workplace productivity attributed to the symptoms of seasonal and perennial allergic
disease in the USA, where most of the available rhinitis (TABLE 1) [1219,51,52] .
data have been collected, are estimated to be
between US$2.4 and US$4.6 billion annually n Seasonal allergic rhinitis
[41] ; in addition, direct and indirect expenditures To evaluate the clinical efficacy and optimum
associated with the treatment of allergic rhinitis therapeutic dose of MFNS, Bronsky et al. con-
in the USA are approximately US$1.5 billion and ducted a multicenter, double-blind, dose-rang-
US$2 billion, respectively, per year [40] . Costs of ing study involving 480 adults (18 years) with
treating allergic rhinitis are also reported to be moderate seasonal allergic rhinitis [13] . Subjects
high in other countries [42] . were randomly assigned to treatment with one
of four daily doses of MFNS (50, 100, 200 or
800 g) or placebo for 28 days. Treatment effi-
cacy was determined using a seven-point scale
Patient requires additional to assess severity of nasal (discharge, rhinorrhea,
long-term allergic rhinitis control stuffiness/congestion, sneezing or itching) and
Second-generation antihistamine non-nasal (eye itching, tearing, and redness and
and/or intranasal steroid plus itching of ears or palate) symptoms. Within
leukotriene receptor antagonist
and/or topical or oral decongestants
3 days of treatment, subjects in the 50, 200 and
800 g daily MFNS groups reported a signifi-
Additional symptom relief
necessary cant (p < 0.05) reduction of symptoms. By day 7,
all four doses were found to be significantly more
Second-generation antihistamine
plus intranasal steroid and/or effective than placebo (p 0.05). Since the two
topical or or oral decongestants lower doses provided less consistent relief, the
investigators concluded that 200 g daily was
Additional symptom relief
necessary py the appropriate MFNS dose for alleviating the
th era
no symptoms of seasonal allergic rhinitis.
Second-generation antihistamine mu A series of additional trials extended these
or intranasal steroid and/or im
ific
topical or oral decongestants ec findings across a broad range of subjects. In the
Sp
double-blind, randomized, placebo-controlled
Diagnosis of
allergic rhinitis trial of 121 adolescents (12 years) and adults
carried out by Meltzer et al., MFNS 200 g daily
was associated with a significant reduction in
mean total morning nasal symptom scores (con-
gestion, rhinorrhea, itching and sneezing) com-
Figure 2. Stepwise approach to treatment for allergic rhinitis.
pared with placebo (p = 0.02) after 1 week [16] .
Adapted with permission from [33] . At week 2, significant improvement was noted
in the active treatment group (p = 0.029). In

394 Therapy (2009) 6(3) future science group

 Mometasone furoate nasal spray Drug Evaluation
Table 1. Summary of clinical studies of mometasone furoate nasal spray for the treatment of nasal symptoms
associated with SAR and PAR.
Author/year Subjects Age Treatment Effect on symptoms Ref.
(n) (years) (duration)

SAR studies
Hebert et al. (1996) 501 18 MFNS 100 g q.d. MFNS (both doses) and BDP more effective [15]
MFNS 200 g q.d. than placebo (p 0.01)
BDP 200 g b.i.d.
Placebo
4 weeks
Graft et al. (1996) 349 12 MFNS 200 g q.d. MFNS and BDP initiated 4 weeks before [14]
BDP 168 g b.i.d. ragweed season decreased minimal symptom
Placebo days versus placebo (p < 0.01)
8 weeks
Bronsky et al. (1997) 480 1865 MFNS 50 g q.d. MFNS 200 g q.d. and 800 g q.d. consistently [13]
MFNS 100 g q.d. more effective than placebo (p < 0.05)
MFNS 200 g q.d.
MFNS 800 g q.d.
Placebo
28 days
Meltzer et al. (1998) 121 12 MFNS 200 g q.d. MFNS improved total nasal symptom score [16]
placebo versus placebo (p = 0.024)
2 weeks
Meltzer et al. (1999) 679 611 MFNS 25 g q.d. MFNS 100 g q.d. (p = 0.03) and 200 g q.d. [51]
MFNS 100 g q.d. (p = 0.04) and BDP 84 g q.d. (p < 0.01) more
MFNS 200 g q.d. effective than placebo
BDP 84 g b.i.d.
Placebo
4 weeks
Berkowitz et al. (1999) 239 1260 MFNS 200 g q.d. MFNS improved total nasal symptom score in [12]
Placebo 7 h versus placebo (p < 0.01)
1 day
Gawchick et al. (2003) 245 12 MFNS 200 g q.d. MFNS improved total nasal symptom score [52]
Placebo versus placebo (p 0.017)
14 days
PAR studies
Drouin et al. (1996) 427 12 MFNS 200 g q.d. MFNS and BDP improved total nasal symptom [17]
BDP 200 g b.i.d. score versus placebo (p 0.01)
Placebo
12 weeks
Mandl et al. (1997) 474 12 MFNS 200 g q.d. MFNS and FP improved total nasal symptom [18]
FP 200 g q.d. score versus placebo (p < 0.01)
Placebo
12 weeks
Bende et al. (2002) 438 18 MFNS 200 g q.d. MFNS and BDP improved total nasal symptom [19]
BDP 128 g q.d. score versus placebo (p < 0.002)
BDP 256 g q.d.
Placebo
4 weeks
BDP: Beclomethasone dipropionate nasal spray; b.i.d.: Twice daily; FP: Fluticasone propionate nasal spray; MFNS: Mometasone furoate nasal spray;
PAR: Perennial allergic rhinitis; q.d.: Daily; SAR: Seasonal allergic rhinitis.

addition, MFNS was associated with a signifi- as young as 6 years old [51] . This multicenter,
cant improvement in nasal cytology, includ- double-blind, placebo-controlled, dose-ranging
ing a reduction in the numbers of eosinophils, study enrolled 679 children between 6 and
basophils and neutrophils. 11 years of age who received MFNS in doses
Meltzer et al. also confirmed that, when given of 25, 100 or 200 g daily or beclomethasone
in appropriate dosages, MFNS can alleviate the dipropionate (BDP) nasal spray 84 g twice-
symptoms of seasonal allergic rhinitis in children daily for up to 4 weeks. According to physician

future science group www.futuremedicine.com 395

Drug Evaluation Small & Teper

evaluation of total nasal symptom scores at day significantly alleviates the symptoms of peren-
8, all three dosages of MFNS and the twice-daily nial allergic rhinitis [1719] . In the first study,
dosage of BDP nasal spray afforded significantly Drouin followed 427 subjects of 12 years or
greater relief than placebo (p 0.02). At 4 weeks, older with a documented allergy to at least one
both the 100 g (p = 0.03) and 200 g (p = 0.04) perennial allergen for 12 weeks [17] . At 15 days,
daily doses of MFNS were significantly more those receiving MFNS 200 g daily and BDP
effective than the 25 g daily dose. However, nasal spray 200 g twice-daily experienced sig-
MFNS 200 g daily provided no significant nificantly (p < 0.01) greater improvement in total
advantage over the 100 g daily dose, leading nasal symptoms (congestion, rhinorrhea, sneez-
the investigators to conclude that MFNS 100 g ing and itching) than the placebo group, which
daily is the most appropriate therapeutic regimen persisted throughout the study period [17] .
for children with seasonal allergic rhinitis [51] . Two additional studies concluded that MFNS
The efficacy of MFNS in the prophylaxis 200 g daily significantly reduces the nasal
of seasonal allergic rhinitis was established by symptoms of perennial allergic rhinitis (conges-
Grafts study of 349 subjects, 12 years or older tion, rhinorrhea, sneezing and itching), increases
with a moderate-to-severe allergy to ragweed the number of symptom-free days, and improves
pollen [14] . Four weeks before the predicted nasal patency as measured by peak nasal inspira-
start of ragweed season, subjects were randomly tory flow [18,19] . Mandl et al. found significant
assigned to receive MFNS 200 g daily, BDP and equivalent efficacy with MFNS 200 g
nasal spray 168 g twice-daily, or placebo for once-daily and fluticasone propionate nasal spray
8 weeks. Subjects receiving MFNS reported a sig- (FPNS) 200 g once-daily (p < 0.01 for both) in
nificantly higher proportion of minimal symp- reducing the total nasal symptom score in both
tom days compared with placebo (p < 0.01). The the morning and evening [18] . In the study by
MFNS group had a median duration of 27 days Bende et al., significant improvement in nasal
before experiencing a non-minimal symptom symptoms occurred within 4 h of the first MFNS
day (defined as a day when the total nasal 200 g dose (p = 0.014) [19] . At 10 days, peak
symptom score was 3 on a 12-point scale), nasal inspiratory flow improved significantly in
compared with a median duration of 10.5 days the MFNS group compared with the placebo
in the placebo group [14] . group (p < 0.01), although BDP nasal spray
Two additional retrospective analyses of data 256 g daily had a greater improvement than
pooled from four randomized, double-blind stud- MFNS in this study compared with placebo.
ies comparing MFNS 200 g daily (n = 494) with
placebo (n = 497) confirmed the efficacy of MFNS n Sensory perceptions of intranasal
in reducing the ocular symptoms of redness, tear- corticosteroids & compliance in
ing and itching commonly associated with sea- allergic rhinitis
sonal allergic rhinitis [53,54] . During a 2-week Despite the discomfort and impairment associ-
study period, MFNS significantly reduced total ated with allergic rhinitis, only 20% of patients
ocular and individual symptom scores compared are compliant with treatment [56] . One factor
with placebo (p < 0.05) [53] . Subjects with moder- contributing to the high rate of noncompliance
ate-to-severe symptoms experienced a significantly may be sensory perception [57,58] , since patients
greater reduction in total ocular symptoms than prefer agents that do not have any taste or scent
those taking placebo (p < 0.05). [58] . In a multicenter, randomized, double-blind,
The mechanism of action of intranasal crossover study, 100 subjects with allergic rhini-
corticosteroids in relieving ocular allergy symp- tis were randomized to an alcohol- and scent-free
toms is not well understood. It has recently been formulation of MFNS, 200 g daily, followed by
shown that a nasalocular reflex follows nasal 200 g daily of FPNS 30 min later, or vice versa
challenge with antigen and probably contributes [56] . Significantly more subjects preferred MFNS
to the ocular symptoms associated with allergic to FPNS (p < 0.05), and fewer subjects reported
rhinitis. In addition to reducing inflammation, scent or odor (immediately and 2 min after
intranasal corticosteroids may reduce ocular drug administration; p < 0.001), taste (imme-
allergy symptoms by attenuating this reflex diately after drug administration; p = 0.002),
mechanism [55] . and aftertaste (2 min after drug administra-
tion; p = 0.007) with MFNS than with FPNS.
n Perennial allergic rhinitis In addition, 47% reported that they would be
Three multicenter, randomized, double-blind, more likely to comply with a MFNS regimen
placebo-controlled trials confirmed that MFNS than with a FPNS regimen (p = 0.03) [56] .

396 Therapy (2009) 6(3) future science group

 Mometasone furoate nasal spray Drug Evaluation
Acute rhinosinusitis anti-inf lammatory properties. By reducing
Rhinosinusitis is an inflammatory process that inflammation, intranasal corticosteroids foster
involves the mucosa of the nose and one or more drainage and increased aeration of the sinuses
sinuses [3,8] . It is classified as acute (symptom [3,5,6,8] . The use of intranasal corticosteroids as
duration <4 weeks), subacute (symptom dura- adjuncts to antibiotic therapy for acute bacte-
tion 48 weeks), chronic (symptom duration rial rhinosinusitis is considered appropriate for
>8 weeks), or recurrent (3 episodes of acute patients who do not respond to initial treatment,
sinusitis per year) [3,8,59,60] . The European posi- have concomitant nasal polyposis, or are experi-
tion paper on rhinosinusitis and nasal polyps encing marked mucosal edema [3,8,64] . Treatment
also classifies acute rhinosinusitis as mild, mod- of acute bacterial rhinosinusitis with antibiotics
erate or severe, based on the total severity visual and intranasal corticosteroids also hastens clear-
analogue scale score [3] . ance of bacteria, decreases the frequency and
The etiology of rhinosinusitis may be viral, severity of disease recurrence [6] and reduces the
bacterial or allergic [4,8] . Acute rhinosinusitis is duration of infection [43,67,68] .
usually caused by a viral infection that, in some Many recent studies support the benefits of
cases, may be complicated by a secondary bacte- intranasal corticosteroids as adjuncts to anti-
rial infection [4,8,61,62] . Symptoms of acute rhino- microbial therapy in acute bacterial rhino-
sinusitis resolve without the use of antibiotics in sinusitis, and three randomized, multicenter,
most patients [59,63] . One study reports that only placebo-controlled studies have demonstrated
38% of adults presenting with symptoms of acute that MFNS alleviates the course of acute bacte-
rhinosinusitis may actually have bacterial rhino- rial rhinosinusitis (TABLE 2) [2023] . In one study,
sinusitis [63] . Perennial allergic rhinitis may also be Meltzer et al. compared a 21-day regimen of
a predisposing factor to acute rhinosinusitis, since amoxicillin/clavulanate with or without MFNS
allergic rhinitis contributes to rhinosinusitis in up in 407 subjects, 12 years or older with acute rhi-
to 30% of patients with acute maxillary rhinosi- nosinusitis confirmed by CT scan of the para-
nusitis and up to 80% of patients with chronic nasal sinuses [20] . The addition of MFNS to the
rhinosinusitis [4] . American and European guide- antibiotic significantly (p < 0.01) reduced mean
lines for the diagnosis and treatment of acute total symptom scores and individual symptom
rhinosinusitis provide algorithms to improve scores, including congestion and facial pain,
treatment outcomes (FIGURES 3 & 4) [3,8,9,62,64] . during days 115 (p 0.01), and headache
The main clinical characteristics of acute (p < 0.01), congestion (p < 0.01) and purulent
rhinosinusitis include nasal congestion, facial rhinorrhea (p 0.05) during days 1621.
pain and/or pressure, rhinorrhea, postnasal In a similar study by Nayak et al. in 2002,
drainage, headache and cough. The four signs 967 subjects 12 years or older with moderate-
and symptoms most predictive of acute bacterial to-severe acute rhinosinusitis confirmed by CT
rhinosinusitis include purulent nasal discharge, scan received amoxicillin/clavulanate for 21 days
maxillary tooth or facial pain (especially uni- with MFNS 200 g twice-daily, MFNS 400 g
lateral), unilateral maxillary tenderness and twice-daily, or placebo [21] . Addition of either the
worsening of symptoms after initial improve- 200 g (p = 0.014) or 400 g (p = 0.017) regi-
ment [3,62,65] . Computed tomography is currently men of MFNS produced a significantly greater
the preferred radiographic modality to confirm improvement in the total symptom score than
acute rhinosinusitis [8] . placebo. MFNS also reduced nasal stuffiness/
Annual crude prevalence rates of acute rhinosi- congestion (200 g, p = 0.01; 400 g, p = 0.025),
nusitis in the USA range from 14 to 16% of adults facial pain (200 g, p = nonsignificant [NS];
[203] . Definitive prevalence rates are lacking owing 400 g, p = 0.008), postnasal drip (200 g,
to inconsistencies in the definition of acute rhino- p = 0.038; 400 g, p = NS), and rhinorrhea
sinusitis, and because not all patients with the (200 g, p = NS; 400 g, p = 0.045).
disease seek professional care [61] . Still, the eco- Since intranasal corticosteroids are an effec-
nomic burden of this disease is high; total annual tive adjunctive therapy for acute bacterial rhino-
costs related to acute rhinosinusitis as either a pri- sinusitis, they may have potential as mono-
mary or secondary diagnosis were estimated to therapy for acute uncomplicated rhinosinusitis
be US$5.93 billion in one American study [66] . [69] . A third study, by Meltzer et al. in 2005,
investigated the use of MFNS as monotherapy in
n Treatment of acute rhinosinusitis 981 subjects 12 years or older with acute uncom-
The rationale for the use of intranasal cortico- plicated rhinosinusitis lasting for 7 days or more
steroids in acute rhinosinusitis resides in their but 28 days or less; those with acute bacterial

future science group www.futuremedicine.com 397

Drug Evaluation Small & Teper

Signs and symptoms of

mild symptoms of acute rhinosinusitis lasting
viral rhinosinusitis less than 5 days receive treatment, such as anal-
(common cold or gesics or decongestants, aimed at symptomatic
influenzal illness) relief, while patients with moderate symptoms
persisting or increasing in severity after 5 days
should receive intranasal corticosteroids [3] . In
patients with severe acute rhinosinusitis, anti-
biotic therapy and intranasal corticosteroids are
Symptoms are no better
recommended (FIGURE 4) [3] . Current American
Symptoms for <7 days
and no recent antibiotic? or worse after 710 days? treatment guidelines are similar [8] . Infection
Likely viral Suspect bacterial infection with resistant pathogens should be considered
in severe cases if symptoms do not improve after
35 days of antibiotic treatment [8,62,69] .

Nasal polyposis
Symptomatic treatment Antibiotic Nasal polyposis is estimated to affect approxi-
mately 2.74% of the population [3,9,70] . Its preva-
lence increases to 715% in patients with asthma
and to 3696% in patients with aspirin sensitiv-
ity [3] . Symptoms include nasal obstruction, con-
No resolution of symptoms gestion, purulent nasal discharge and postnasal
No resolution or worsening within 35 days or symptoms
of symptoms? return within 2 weeks after
drip [71] . More than 75% of patients also have an
Suspect bacterial infection initial antibiotic? impaired sense of smell [72] . These symptoms have
Suspect resistant a marked impact on quality of life, interfering
pathogens with physical, social and normal daily activities.
The symptoms can also cause sleep disorders and
headaches, as well as impair patients moods and
their psychological well-being [73] .
Nasal polyposis is characterized by an eosi-
nophil-dominated inflammation of unknown
No resolution or worsening Use antibiotic with different cause and is often associated with asthma, aspi-
of signs and symptoms coverage for pathogens rin sensitivity or cystic fibrosis [9,71] . One possible
not covered with first
Sinus CT and ENT consult mechanism for the development of nasal polypo-
course of therapy
with sinus aspirate and sis involves bacterial colonization of the nasal cav-
sinus lavage ity, causing the synthesis and release of enterotox-
Antibiotic
ins that act as superantigens to stimulate the local
immune system [74] . A hallmark of bilateral nasal
polyposis, which is observed in approximately
90% of adults with the condition, is a mixed cel-
Figure 3. Algorithm for differentiating viral and bacterial acute
rhinosinusitis. lular infiltrate with predominant eosinophilia [75] .
CT: Computed tomography; ENT: Ear, nose and throat. Increased levels of inflammatory mediators, such
Adapted with permission from [62] . as interleukin-5 [76] , eotaxin [77] and eosinophilic
cationic protein [78] are also present.
rhinosinusitis were excluded [23] . This study
compared MFNS 200 g once- or twice-daily n Treatment of nasal polyposis
for 15 days with amoxicillin alone or placebo Treatment objectives for nasal polyposis include
alone. MFNS 200 g twice-daily was superior to reducing or eliminating polyps, opening the nasal
both placebo alone (p < 0.001) and amoxicillin airway, improving or restoring sense of smell
monotherapy (p = 0.002) in improving symptom and preventing recurrence. Surgical removal
scores. In another study, MFNS monotherapy of polyps, with or without medical therapy, for
was also shown to provide a significantly greater more severe cases and medical therapy for mild-
improvement in patients health-related quality to-moderate cases are the usual treatment regi-
of life [22] . mens [79] . Although endoscopic surgery has been
Fokkens et al., on behalf of the European shown to be effective for reducing polyp size and
Academy of A llergolog y and Clinical temporarily improving nasal blockage [8082] , one
Immunology, recommends that adults with randomized, controlled study in 2001 reported

398 Therapy (2009) 6(3) future science group

 Mometasone furoate nasal spray Drug Evaluation

Sudden onset of two or more symptoms, one of which should At any point immediate
be either nasal blockage/obstruction/congestion or nasal referral/hospitalization if any
discharge: of the following occur:
anterior/post nasal drip; 3
Periorbital edema
facial pain/pressure; 3
"*($
$'e
reduction or loss of smell; 3
',le vision
Examination: anterior rhinoscopy 3
(+!$%'($ "a
X-ray/CT not recommended 3
,
-"*,$
,"+0
3
vere unilateral or
bilateral frontal headache
3
rontal swelling
Symptoms less than 5 days Symptoms persisting or 3
" &*
'
%&"& "+"*
')
or improving thereafter increasing after 5 days focal neurologic signs

Common cold Moderate Severe*

Antibiotics
Symptomatic relief Topical steroids
Topical steroids

No improvement after No effect in 48 h

Effect in 48 h
14 days of treatment

Consider referral Continue treatment er to specialist

to specialist for 714 days

Figure 4. Treatment scheme for primary care for adults with acute rhinosinusitis.
*
Fever of greater than 38C and/or severe pain.
Adapted with permission from [3] .

that medical treatment alone with oral or topical Mometasone furoate nasal spray is the first
corticosteroids appeared to be sufficient to treat intranasal corticosteroid to be approved by the
most of the symptoms of nasal polyposis [81] . USA FDA for the medical treatment of nasal
Another study by Benitez and colleagues found polyposis [24] . Results of the first large-scale clin-
that subjects with severe nasal polyposis had a ical studies of MFNS for nasal polyposis were
significant improvement in their symptoms with published in 2005 and 2006. Three 4-month,
a short course of oral corticosteroids followed by multicenter, randomized, placebo-controlled
intranasal corticosteroids [83] . In addition, the clinical trials enrolled 354, 310 and 298 patients,
postsurgical recurrence rate for nasal polyposis respectively [2426] , to evaluate the efficacy and
after 2 years is reported to be as high as 60% in safety of 200 g daily and 200 g twice-daily
some studies [8486] . At this time, the benefits dosing of MFNS. The twice-daily regimen of
of surgery over medical therapy have not been MFNS was chosen to help overcome the possible
established [81,82] . obstruction of drug distribution by polyps. In
Treatment with intranasal corticosteroids all three studies, subjects receiving either dos-
reduces the eosinophil-associated inflammation age of MFNS experienced significantly greater
of polyposis, thereby helping to control symptoms improvement than those receiving placebo in the
and reduce polyp size [9,2425,81,87] . Fokkens et al. reduction of the size and extent of endoscopi-
and the European Academy of Allergology and cally verified bilateral nasal polyps, as well as in
Clinical Immunology, as well as other authors, congestion/obstruction, loss of sense of smell,
concluded that intranasal corticosteroids are anterior rhinorrhea and postnasal drip (FIGURE 5)
generally effective for improving symptoms and [2426] . A statistically significant improvement
decreasing polyp size, although little improvement with both doses of MFNS was observed within
in sense of smell was reported [3,8890] . the first month of treatment and continued

future science group www.futuremedicine.com 399

Drug Evaluation Small & Teper

Table 2. Summary of clinical studies of MFNS for the treatment of acute rhinosinusitis.
Author/year Subjects (n) Age (years) Treatment Effect on symptoms Ref.
(duration)
Meltzer et al. 407 12 ACP 875 mg b.i.d. ACP + MFNS significantly better than [20]
(2000) + ACP + placebo (p 0.01)
MFNS 400 g b.i.d.
or
placebo
21 days
Nayak et al. (2002) 967 12 ACP 875 mg b.i.d. ACP + MFNS (both doses) significantly [21]
+ better than ACP + placebo (p 0.017)
MFNS 200 g b.i.d.
or
MFNS 400 g b.i.d.
or
placebo
21 days
Meltzer et al. 981 12 Amoxicillin 500 mg t.i.d. MFNS 200 g b.i.d. significantly better [23]
(2005) 10 days than placebo (p < 0.001) or amoxicillin
or (p = 0.002);
MFNS 200 g q.d. MFNS 200 g q.d. significantly better
15 days than placebo (p = 0.018)
or
MFNS 200 g b.i.d.
15 days
or
placebo
ACP: Amoxicillin/clavulanate potassium; b.i.d.: Twice daily; MFNS: Mometasone furoate nasal spray; q.d.: Daily; t.i.d.: Three-times daily.

up to the study end points at 4 months [2426] . effect on hyposmia or anosmia [81] , supporting
The twice-daily dosing regimen of MFNS was the importance of medical therapy in treating
superior to the once-daily dosing formulation this symptom [24] .
for improving the symptoms of congestion and For many patients, loss of sense of smell is
obstruction (p = 0.039) [2426] . one of the most disturbing symptoms of nasal
In one study, the overall change in bilateral polyposis [95] , and its return is therefore an
polyp grade score with MFNS represented a important therapeutic goal. However, change
clinically significant reduction of approximately in sense of smell may be more subjective than
30% relative to baseline [24] . Since reducing other symptoms, which may account for the
polyp size is thought to be a slow process, this observed placebo effect in many studies [27] .
degree of improvement in 4 months is notewor- Importantly, the improvement in sense of smell
thy. Incremental improvements in polyp grade seen with MFNS therapy corresponds to the
continued throughout the course of the study, increased improvement in polyp grade scores
suggesting that treatment with MFNS should be over time [24,26,27] .
maintained to achieve a full response. Response A recent ana lysis of the onset of symptomatic
to MFNS did not vary with the size of the effect of MFNS 200 g twice-daily revealed a
polyps. In addition, 57% of patients receiving rapid improvement in most symptoms of nasal
MFNS 200 g twice-daily were considered to polyposis from within 24 h after the first dose to
be improved based on its effect on polyp grade within 5 days of initiating therapy [27] . Subjects
and congestion/obstruction score, compared receiving this dose of MFNS experienced sta-
with 43% of patients receiving MFNS 200 g tistically significant (p < 0.05) improvement
daily and 34% of patients receiving placebo [24] . compared with placebo at day 2 for anterior
The significant improvement in loss of rhinorrhea, day 3 for nasal congestion, day 5
sense of smell associated with MFNS contrasts for postnasal drip and day 13 for sense of smell.
with previous studies regarding endoscopic Peak nasal inspiratory flow also improved sig-
surgery or other intranasal corticosteroids, in nificantly at day 2 (p = 0.031) [27] . The rapid
which sense of smell did not improve [84,9194] . onset of action of MFNS in nasal polyposis
Comparisons between medical and surgical may be due to the high topical potency of the
treatment indicate that surgery has very little drug in inhibiting the synthesis and release of

400 Therapy (2009) 6(3) future science group

 Mometasone furoate nasal spray Drug Evaluation

MFNS 200 g MFNS 200 g

q.d. AM b.i.d. Placebo
0

-0.2
(LS mean bilateral polyp grade score)

-0.4

-0.5
-0.6
Change from baseline

-0.8

-1 -0.96

*
-1.2 -1.15 *p < 0.05 vs placebo
** **p < 0.001 vs placebo
-1.4

MFNS 200 g b.i.d.

MFNS 200 g q.d. AM
Placebo

-1.2 **
-1.10
**
-1.01
Change from baseline (LS mean
congestion/obstruction score)

-1.0 **
-0.83

-0.8 -0.86
**
-0.61 -0.78 **
-0.6 -0.68 * -0.50
**
-0.4 -0.47 -0.48
**
-0.2 -0.32
-0.24
0
1 2 3 4

Time (month)
*p < 0.01 vs placebo
**p < 0.001 vs placebo

p < 0.05 vs MFNS 200 g q.d. AM

Figure 5. Change from baseline in bilateral polyp grade score (A) and congestion/
obstruction score (B) following 4 weeks of treatment with MFNS.
b.i.d.: Twice daily; LS: Least squares; MFNS: Mometasone furoate nasal spray; q.d.: Once daily.
Adapted with permission from [24] .

proinflammatory cytokines such as IL-1, IL-5, A pronounced placebo effect occurred in this
IL-6 and TNF [13,27,96] . Similar to the previous study, particularly for the end points of nasal
studies, the treatment effect of MFNS for all congestion/obstruction and sense of smell, and
symptoms persisted for at least 4 months [24,26,27] increased over time [27] . Such an effect, observed
and increased with the duration of therapy [27] . in many studies of nasal polyposis [24,26,27] , may
This improvement in symptom scores corre- be attributable to the inactive components of
sponds to the increased improvement in polyp MFNS. Thus, the use of placebo groups remains
grade scores over time. important for future trials of nasal polyposis [26,27] .

future science group www.futuremedicine.com 401

Drug Evaluation Small & Teper

Table 3. Bioavailability of intranasal corticosteroids. due to suppressed cortisol levels, formation of

cataracts and osteoporosis [101,102] . However,
Intranasal corticosteroid Bioavailability (%)
use of intranasal corticosteroids has not been
Flunisolide 49 associated with serious side effects.
Beclomethasone dipropionate 44 One indication of an agents potential for sys-
Budesonide 34 temic adverse events is its bioavailability, which
Fluticasone propionate 0.42 depends partly on its absorption across the
Mometasone furoate 0.46 highly vascular nasal mucosa [103] . The degree of
Fluticasone furoate 0.50 systemic absorption depends on its lipophilicity.
Data taken from [100,102,103,105]. Thus, intranasal corticosteroids with lower sys-
temic bioavailability, such as MFNS, fluticasone
Mometasone furoate may thus offer patients furoate and fluticasone propionate, are highly
with nasal polyposis a therapeutic option that lipophilic, whereas those with higher bioavail-
can reduce or delay the need for surgery by effec- ability, such as flunisolide, beclomethasone
tively relieving the symptoms of this disease [24] . dipropionate and budesonide, are less lipophilic
Once-daily dosing of MFNS appears to be as [103,104] . Systemic bioavailability is also partly
effective as twice-daily dosing across this popu- determined by the degree of first-pass hepatic
lation as a whole, except for nasal congestion metabolism, which is generally favorable with
and obstruction. Individual subject response intranasal corticosteroids [101] . When used at
should determine the optimal dosing regimen recommended doses, MFNS has a systemic con-
[24] . Further studies are necessary to determine centration of less than 0.5%, which is equal to
the lasting effect of MFNS on the continued res- or lower than that reported for other intranasal
olution of nasal symptoms associated with nasal corticosteroids (TABLE 3) [100,102105] .
polyposis, since maximal reduction in polyp size Studies of the systemic safety of MFNS reveal
may take several months to achieve [24,27,89] . no effect on hypothalamicpituitaryadrenal
(HPA)-axis function in adults, as assessed by
Safety of MFNS the measurement of cortisol levels. In a placebo-
n Local adverse events controlled, randomized, parallel-group study
In clinical studies involving both adults and chil- of 24 adult volunteers, eight received MFNS,
dren, the incidence of adverse events is generally administered at single doses of 1, 2 and 4 mg;
similar in patients receiving MFNS in doses rang- none experienced clinical symptoms of HPA-
ing from 50 to 800 g daily, and is comparable to axis suppression [48] . Effects on the plasma cor-
those receiving placebo. Local adverse events in tical concentration curve, urinary free cortisol,
patients from all age groups are mild in intensity and 8 am plasma cortisol were similar to placebo
and self-limiting, and resolve without discontinu- at all doses of MFNS. These findings reveal that
ation of therapy [1219,51,52,97] . The most common even when given in doses up to 20-times the
local adverse events include epistaxis (ranging projected clinical dose, MFNS does not affect
from blood-tinged mucus to bleeding) and head- cortisol secretion. In another study involving
ache [1215,1719,51,52,98] . A multicenter, open-label, 27 adults with perennial allergic rhinitis, ran-
12-month study of changes in nasal histopathol- domized to MFNS 200 g daily or triamcino-
ogy reported that MFNS did not lead to changes lone acetonide 220 g daily for 3 weeks, there
in epithelial thickness or focal metaplasia, sug- were no differences between the two drugs in
gesting that long-term treatment is not associated values obtained at baseline and at 3 weeks in
with nasal atrophy [99] . systemic bioactivity markers, including plasma
and urine cortisol levels [106] . In a third study of
n Systemic safety MFNS in nasal polyposis, no significant differ-
The possible routes of systemic exposure with ences in 24-h urinary free cortisol were found
intranasal corticosteroids include absorption over the treatment period among the MFNS
of the locally deposited dose through the nasal 200 g twice-daily, MFNS 200 g daily or
mucosa or absorption of a potentially swallowed placebo groups [24] .
dose through the gastrointestinal tract [100] . Suppressed cortisol levels impair the normal
Some clinicians are reluctant to prescribe intra- response to stress and can retard growth rate in
nasal corticosteroids, particularly for pediatric children [107] . However, studies of MFNS in chil-
patients, owing to concerns regarding possible dren have not demonstrated that it produces any
systemic effects, including impairment of the relevant absorption. In a randomized, evaluator-
normal response to stress, growth retardation masked, placebo-controlled study of 96 children

402 Therapy (2009) 6(3) future science group

 Mometasone furoate nasal spray Drug Evaluation
aged 312 years with allergic rhinitis, MFNS The safety profile of MFNS is well-established.
doses of up to 200 g daily for as many as Local adverse events tend to be mild-to-moderate
14 days were well-tolerated and did not result and resolve without discontinuation of treatment.
in clinically relevant exposure [48] . In addition, No systemic adverse events have been reported in
no significant differences were observed between adults or children. In summary, extensive clinical
mean plasma cortisol and 24-h urinary free cor- testing has demonstrated that MFNS is a safe and
tisol concentrations between children receiving effective therapeutic option for the prophylaxis
MFNS or placebo. Other studies with MFNS and treatment of seasonal allergic rhinitis and
in children as young as 3 years did not report the treatment of perennial allergic rhinitis, acute
any signs of suppression of HPA-axis function rhinosinusitis and nasal polyposis.
[51,107] . For example, a 52-week study of 98 chil-
dren aged between 3 and 9 years with perennial Future perspective
allergic rhinitis who were randomized to MFNS Current clinical investigations with MFNS are
100 g daily or placebo found that children in providing substantial evidence regarding its
the MFNS group had no suppression of growth efficacy in reducing the ocular symptoms of
compared with those in the placebo group [108] . allergic rhinitis. Numerous clinical studies have
found that MFNS is not associated with ocular-
Conclusion related adverse events, such as the development
Extensive clinical evidence has confirmed that of glaucoma or subcapsular cataracts. They also
MFNS is a highly effective treatment for com- indicate that MFNS could be a primary treat-
mon inflammatory disorders of the upper respira- ment for both the nasal and ocular symptoms of
tory tract. Multiple clinical studies have consis- allergic rhinitis, possibly eliminating the need
tently revealed that MFNS rapidly alleviates the for patients to use separate medications for the
symptoms of seasonal allergic rhinitis, perennial two symptoms. In addition, MFNS has dem-
allergic rhinitis and nasal polyposis. MFNS is onstrated an improved quality of life in patients
also important in the treatment of acute rhino- with allergic rhinitis by increasing their quality
sinusitis, as monotherapy in uncomplicated cases, of sleep and workplace productivity.
or as an adjunct to antibiotics in documented Mometasone furoate nasal spray has been
cases of acute bacterial rhinosinusitis. recommended as an adjunct to antibiotics for

Executive summary
Mometasone furoate is a potent 17-heterocyclic corticosteroid formulated in an aqueous suspension for intranasal application with a
metered-dose, manual pump nasal spray.
Mometasone furoate nasal spray (MFNS) is safe and effective for the treatment and prophylaxis of seasonal allergic rhinitis and the
treatment of perennial allergic rhinitis, nasal polyposis, and as an adjunct to antibiotics for acute bacterial rhinosinusitis, as well as
monotherapy for acute uncomplicated rhinosinusitis.
Allergic rhinitis
When administered to patients with seasonal or perennial allergic rhinitis, MFNS reduces nasal congestion, rhinorrhea, nasal itching,
sneezing and postnasal drainage, as well as the ocular symptoms of itching, redness and tearing.
Acute rhinosinusitis
The rationale for using intranasal corticosteroids in acute rhinosinusitis resides in their anti-inflammatory properties.
The administration of MFNS together with an antibiotic significantly reduces the symptoms of acute bacterial rhinosinusitis, including
purulent rhinorrhea, nasal congestion, postnasal drip, headache, facial pain and cough.
MFNS has been found to be an effective monotherapy in cases of uncomplicated acute rhinosinusitis that are usually secondary to a viral
infection; its use could decrease the overuse of antibiotics in this disease.
Nasal polyposis
Nasal polyps are benign growths that develop in the nose and sinuses, causing obstruction and interfering with breathing. They often
lead to impairment or loss of sense of smell.
MFNS has been shown to reduce nasal polyp size, but a longer duration of therapy than that used for acute rhinosinusitis may be
required.
MFNS 200 g twice-daily significantly improves nasal congestion/obstruction, rhinorrhea, postnasal drip and sense of smell in nasal
polyposis.
It has a rapid onset and provides lasting relief of most of the major symptoms of nasal polyposis within 25 days of initiating therapy.
Local adverse events associated with MFNS in patients from all age groups are mild in intensity, self-limiting and usually resolve without
discontinuation of therapy.

future science group www.futuremedicine.com 403

Drug Evaluation Small & Teper

acute bacterial rhinosinusitis. By using MFNS determine if MFNS prophylaxis is necessary to

in acute rhinosinusitis, inappropriate antibiotic prevent the recurrence of nasal polyposis.
use will be decreased, leading to lower costs and,
most importantly, reduced bacterial resistance Financial & competing interests disclosure
to antibiotics. MFNS has also been shown to Dr Teper is an employee of Schering Plough and owns com-
reduce nasal polyp size and improve the trou- pany stocks. The authors have no other relevant affiliations
bling associated symptoms of nasal congestion/ or financial involvement with any organization or entity
obstruction and loss of sense of smell. It has a with a financial interest in or financial conflict with the
rapid onset of action and provides lasting relief, subject matter or materials discussed in the manuscript
thereby reducing or delaying the need for nasal apart from those disclosed. No writing assistance was
polyp surgery. Future studies are needed to utilized in the production of this manuscript.

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