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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
Structure of Mometasone Furoate

SMILES

C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(Cl)[C@@H](O)C[C@]2(C)[C@@]1(OC(=O)C5=CC=CO5)C(=O)CCl

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

HIDE SMILES / InChI

Molecular Formula C27H30Cl2O6
Molecular Weight 521.429
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 8 / 8
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

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 TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
ELOCON
Preventing
ASMANEX

Cmax

ValueDoseCo-administeredAnalytePopulation
64.8 pg/mL
400 μg single, respiratory
MOMETASONE plasma
Homo sapiens
10.6 pg/mL
800 μg single, respiratory
MOMETASONE plasma
Homo sapiens
86.4 pg/mL
800 μg 1 times / day steady-state, respiratory
MOMETASONE plasma
Homo sapiens
183 pg/mL
320 μg 1 times / day steady-state, respiratory
MOMETASONE plasma
Homo sapiens
7.56 pg/mL
100 μg single, nasal
MOMETASONE plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
924 pg × h/mL
400 μg single, respiratory
MOMETASONE plasma
Homo sapiens
386 pg × h/mL
800 μg single, respiratory
MOMETASONE plasma
Homo sapiens
386 pg × h/mL
800 μg 1 times / day steady-state, respiratory
MOMETASONE plasma
Homo sapiens
1560 pg × h/mL
320 μg 1 times / day steady-state, respiratory
MOMETASONE plasma
Homo sapiens
92 pg × h/mL
100 μg single, nasal
MOMETASONE plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
13.2 h
400 μg single, respiratory
MOMETASONE plasma
Homo sapiens
18.9 h
800 μg single, respiratory
MOMETASONE plasma
Homo sapiens
19.24 h
100 μg single, nasal
MOMETASONE plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
1.5%
MOMETASONE plasma
Homo sapiens

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer



Drug as perpetrator​

Drug as victim

Sourcing

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
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
Mac-1 expression and human eosinophil migration were effectively downregulated by preincubation with Mometasone at 1, 10 and 100 nM
Substance Class Chemical
Record UNII
04201GDN4R
Record Status Validated (UNII)
Record Version