Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C27H30Cl2O6 |
Molecular Weight | 521.429 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12C[C@@H](C)[C@](OC(=O)C3=CC=CO3)(C(=O)CCl)[C@@]1(C)C[C@H](O)[C@@]4(Cl)[C@@]2([H])CCC5=CC(=O)C=C[C@]45C
InChI
InChIKey=WOFMFGQZHJDGCX-ZULDAHANSA-N
InChI=1S/C27H30Cl2O6/c1-15-11-19-18-7-6-16-12-17(30)8-9-24(16,2)26(18,29)21(31)13-25(19,3)27(15,22(32)14-28)35-23(33)20-5-4-10-34-20/h4-5,8-10,12,15,18-19,21,31H,6-7,11,13-14H2,1-3H3/t15-,18+,19+,21+,24+,25+,26+,27+/m1/s1
DescriptionSources: http://www.drugbank.ca/drugs/DB00764Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/019796s026lbl.pdf
Sources: http://www.drugbank.ca/drugs/DB00764
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/019796s026lbl.pdf
Mometasone is a medium-potency synthetic corticosteroid with antiinflammatory, antipruritic, and vasoconstrictive properties. Studies in asthmatic patients have demonstrated that mometasone provides a favorable ratio of topical to systemic activity due to its primary local effect along with the extensive hepatic metabolism and the lack of active metabolites. Though effective for the treatment of asthma, glucocorticoids do not affect asthma symptoms immediately. Maximum improvement in symptoms following inhaled administration of mometasone furoate may not be achieved for 1 to 2 weeks or longer after starting treatment. When glucocorticoids are discontinued, asthma stability may persist for several days or longer. Mometasone has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor which is approximately 12 times that of dexamethasone, 7 times that of triamcinolone acetonide, 5 times that of budesonide, and 1.5 times that of fluticasone. Mometasone inhaler is indicated for the maintenance treatment of asthma as prophylactic therapy. The nasal spray is indicated for the treatment of the nasal symptoms of seasonal allergic and perennial allergic rhinitis. ELOCON Lotion (Mometasone) is indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2034 Sources: http://www.drugbank.ca/drugs/DB00764 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | ELOCON Approved UseELOCON Lotion is a corticosteroid indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses in patients ≥12 years of age. Launch Date5.47171205E11 |
|||
Preventing | ASMANEX Approved UseASMANEX TWISTHALER is a corticosteroid indicated for:
• Maintenance treatment of asthma as prophylactic therapy in patients 4 years of age and older. Launch Date1.11205443E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
183 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26845343 |
320 μg 1 times / day steady-state, respiratory dose: 320 μg route of administration: Respiratory experiment type: STEADY-STATE co-administered: |
MOMETASONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
7.56 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29669668 |
100 μg single, nasal dose: 100 μg route of administration: Nasal experiment type: SINGLE co-administered: |
MOMETASONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1560 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26845343 |
320 μg 1 times / day steady-state, respiratory dose: 320 μg route of administration: Respiratory experiment type: STEADY-STATE co-administered: |
MOMETASONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
92 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29669668 |
100 μg single, nasal dose: 100 μg route of administration: Nasal experiment type: SINGLE co-administered: |
MOMETASONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
19.24 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29669668 |
100 μg single, nasal dose: 100 μg route of administration: Nasal experiment type: SINGLE co-administered: |
MOMETASONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.5% |
MOMETASONE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
0.1 % 1 times / day steady, topical Recommended Dose: 0.1 %, 1 times / day Route: topical Route: steady Dose: 0.1 %, 1 times / day Sources: |
unhealthy, 0.5 - 2 yeas n = 63 Health Status: unhealthy Condition: dermatoses Age Group: 0.5 - 2 yeas Sex: unknown Population Size: 63 Sources: |
Other AEs: Glucocorticoid decreased, Skin and subcutaneous conditions NEC... Other AEs: Glucocorticoid decreased (1 patient) Sources: Skin and subcutaneous conditions NEC (1 patient) Skin bacterial infection (1 patient) |
0.1 % 1 times / day steady, topical Recommended Dose: 0.1 %, 1 times / day Route: topical Route: steady Dose: 0.1 %, 1 times / day Sources: |
unhealthy, adult n = 812 Health Status: unhealthy Condition: dermatoses Age Group: adult Sex: unknown Population Size: 812 Sources: |
Other AEs: Pruritus, Skin atrophy... Other AEs: Pruritus (4.8%) Sources: Skin atrophy (4.8%) Tingling (4.8%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Glucocorticoid decreased | 1 patient | 0.1 % 1 times / day steady, topical Recommended Dose: 0.1 %, 1 times / day Route: topical Route: steady Dose: 0.1 %, 1 times / day Sources: |
unhealthy, 0.5 - 2 yeas n = 63 Health Status: unhealthy Condition: dermatoses Age Group: 0.5 - 2 yeas Sex: unknown Population Size: 63 Sources: |
Skin and subcutaneous conditions NEC | 1 patient | 0.1 % 1 times / day steady, topical Recommended Dose: 0.1 %, 1 times / day Route: topical Route: steady Dose: 0.1 %, 1 times / day Sources: |
unhealthy, 0.5 - 2 yeas n = 63 Health Status: unhealthy Condition: dermatoses Age Group: 0.5 - 2 yeas Sex: unknown Population Size: 63 Sources: |
Skin bacterial infection | 1 patient | 0.1 % 1 times / day steady, topical Recommended Dose: 0.1 %, 1 times / day Route: topical Route: steady Dose: 0.1 %, 1 times / day Sources: |
unhealthy, 0.5 - 2 yeas n = 63 Health Status: unhealthy Condition: dermatoses Age Group: 0.5 - 2 yeas Sex: unknown Population Size: 63 Sources: |
Pruritus | 4.8% | 0.1 % 1 times / day steady, topical Recommended Dose: 0.1 %, 1 times / day Route: topical Route: steady Dose: 0.1 %, 1 times / day Sources: |
unhealthy, adult n = 812 Health Status: unhealthy Condition: dermatoses Age Group: adult Sex: unknown Population Size: 812 Sources: |
Skin atrophy | 4.8% | 0.1 % 1 times / day steady, topical Recommended Dose: 0.1 %, 1 times / day Route: topical Route: steady Dose: 0.1 %, 1 times / day Sources: |
unhealthy, adult n = 812 Health Status: unhealthy Condition: dermatoses Age Group: adult Sex: unknown Population Size: 812 Sources: |
Tingling | 4.8% | 0.1 % 1 times / day steady, topical Recommended Dose: 0.1 %, 1 times / day Route: topical Route: steady Dose: 0.1 %, 1 times / day Sources: |
unhealthy, adult n = 812 Health Status: unhealthy Condition: dermatoses Age Group: adult Sex: unknown Population Size: 812 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/15601807/ Page: 6.0 |
yes [IC50 0.327 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
likely | ||||
likely | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205641Orig1s000ClinPharmR.pdf#page=22 Page: 22,23 |
yes | unlikely (co-administration study) Comment: ketoconazole 200 mg (as well as placebo) were given twice daily concomitantly on Days 4 to 9. Mometasone furoate plasma concentrations were <150 pcg/mL on Day 3 prior to coadministration of ketoconazole or placebo. Following concomitant administration of ketoconazole, 4 out of 12 subjects in the ketoconazole treatment group (n=12) had peak plasma concentrations of mometasone furoate >200 pcg/mL on Day 9 (211-324 pcg/mL) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205641Orig1s000ClinPharmR.pdf#page=22 Page: 22,23 |
PubMed
Title | Date | PubMed |
---|---|---|
Efficacy and safety of ketotifen eye drops as adjunctive therapy to mometasone nasal spray in subjects with seasonal allergic rhinoconjunctivitis. | 2003 |
|
Eosinophilic airway inflammation in COPD. | 2006 |
|
Cough and its importance in COPD. | 2006 |
|
The benefits of combined treatment with corticosteroids and long-acting beta agonists. | 2006 |
|
Pharmacological treatment of chronic obstructive pulmonary disease. | 2006 |
|
Future therapeutic treatment of COPD: struggle between oxidants and cytokines. | 2007 |
|
Exogenous Cushing syndrome with inhaled fluticasone in a child receiving lopinavir/ritonavir. | 2007 Jul |
|
Seborrhoeic dermatitis. | 2007 Jul 1 |
|
Human receptor kinetics and lung tissue retention of the enhanced-affinity glucocorticoid fluticasone furoate. | 2007 Jul 25 |
|
Onset of action of azelastine nasal spray compared with mometasone nasal spray and placebo in subjects with seasonal allergic rhinitis evaluated in an environmental exposure chamber. | 2007 Jul-Aug |
|
Montelukast in the management of allergic rhinitis. | 2007 Jun |
|
The role of mometasone furoate aqueous nasal spray in the treatment of adenoidal hypertrophy in the pediatric age group: preliminary results of a prospective, randomized study. | 2007 Jun |
|
Synergistic effect of formoterol and mometasone in a mouse model of allergic lung inflammation. | 2007 Sep |
|
Onset and duration of action of nasal sprays in seasonal allergic rhinitis patients: olopatadine hydrochloride versus mometasone furoate monohydrate. | 2007 Sep-Oct |
|
[Patient preference survey on the lack of taste and odor of Nasonex nasal spray. Which impact on compliance to treatment?]. | 2008 |
|
Airways inflammation and treatment during acute exacerbations of COPD. | 2008 |
|
Vancomycin-induced DRESS syndrome in a female patient. | 2008 |
|
New treatment options in allergic rhinitis: patient considerations and the role of ciclesonide. | 2008 Apr |
|
New approaches to managing asthma: a US perspective. | 2008 Apr |
|
Long-term follow-up of children undergoing topical intranasal steroid therapy for adenoidal hypertrophy. | 2008 Aug |
|
Effect of allergic rhinitis on the use and cost of health services by children with asthma. | 2008 Aug 30 |
|
Mometasone furoate in the management of asthma: a review. | 2008 Dec |
|
Foxp3+ T regulatory cells (Tregs) are increased in nasal polyps (NP) after treatment with intranasal steroid. | 2008 Dec |
|
A prospective clinical review of "multi model" approach for treating ear keloids. | 2008 Jan |
|
Relative oral corticosteroid-sparing effect of 7 inhaled corticosteroids in chronic asthma: a meta-analysis. | 2008 Jul |
|
Chronic hypokalemia due to excessive cola consumption: a case report. | 2008 Jul 14 |
|
Expression of chloride channel protein CLC-3 in patients with allergic rhinitis: effect of topical corticosteroid treatment. | 2008 Mar |
|
[The effect of desloratadine on quality of life of patients with seasonal allergic rhinitis]. | 2008 May |
|
Antibacterial activity of mometasone furoate. | 2008 May |
|
One-year treatment with mometasone furoate in chronic obstructive pulmonary disease. | 2008 Nov 13 |
|
Effectiveness of twice daily azelastine nasal spray in patients with seasonal allergic rhinitis. | 2008 Oct |
|
Effect of illicit direct to consumer advertising on use of etanercept, mometasone, and tegaserod in Canada: controlled longitudinal study. | 2008 Sep 2 |
|
Comparative adrenocortical suppression in dogs with otitis externa following topical otic administration of four different glucocorticoid-containing medications. | 2008 Summer |
|
Local cytokines and clinical symptoms in children with allergic rhinitis after different treatments. | 2009 |
|
Comparison of corticosteroid nasal sprays in relation to concomitant use and cost of other prescription medications to treat allergic rhinitis symptoms: retrospective cohort analysis of pharmacy claims data. | 2009 |
|
Bronchial diffusing capacity of nitric oxide is increased in patients with allergic rhinitis. | 2009 |
|
A double-blind randomised placebo-controlled trial of topical intranasal corticosteroids in 4- to 11-year-old children with persistent bilateral otitis media with effusion in primary care. | 2009 Aug |
|
Mometasone furoate: an inhaled glucocorticoid for the management of asthma in adults and children. | 2009 Aug |
|
Topical intranasal corticosteroids in 4-11 year old children with persistent bilateral otitis media with effusion in primary care: double blind randomised placebo controlled trial. | 2009 Dec 16 |
|
Using nasal steroids to treat nasal obstruction caused by adenoid hypertrophy: does it work? | 2009 Feb |
|
Inhaled corticosteroids for asthma: are they all the same? | 2009 Feb |
|
Inhaled corticosteroids for asthma: impact of practice level device switching on asthma control. | 2009 Jan 2 |
|
Use of mometasone furoate to prevent polyp relapse after endoscopic sinus surgery. | 2009 Mar |
|
Twelve years' experience with direct-to-consumer advertising of prescription drugs in Canada: a cautionary tale. | 2009 May 27 |
|
Effect of the inhaled corticosteroid mometasone on small airway patency in patients with asthma. | 2009 May-Jun |
|
Treatment of postviral olfactory loss with glucocorticoids, Ginkgo biloba, and mometasone nasal spray. | 2009 Oct |
|
Drugs associated with more suicidal ideations are also associated with more suicide attempts. | 2009 Oct 2 |
|
Alitretinoin--its use in intractable hand eczema and other potential indications. | 2009 Sep 21 |
|
Mapping analyses to estimate health utilities based on responses to the OM8-30 Otitis Media Questionnaire. | 2010 Feb |
|
Allergic contact dermatitis to inhalation corticosteroids. | 2010 Jan-Feb |
Patents
Sample Use Guides
In Vivo Use Guide
Curator's Comment: Can also be used as inhalation powder http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021067s013lbl.pdf
Apply a few drops to the affected skin areas once daily and
massage lightly until it disappears.
Route of Administration:
Topical
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15454120
Mac-1 expression and human eosinophil migration were effectively downregulated by preincubation with Mometasone at 1, 10 and 100 nM
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Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
691019
Created by
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NCI_THESAURUS |
C29505
Created by
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746171
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04201GDN4R
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SUB166214
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100000091860
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DTXSID4023333
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83919-23-7
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SUB03318MIG
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CHEMBL1161
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MOMETASONE FUROATE
Created by
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X-51
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m7597
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30145
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47564
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04201GDN4R
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441336
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C29268
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760077
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1832
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DB14512
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1445470
Created by
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
SUBSTANCE RECORD