Mometasone is a medium-potency synthetic corticosteroid with anti-inflammatory, 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. The anti-inflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

Structure

Similar Structures

Synonyms

(+)-Mometasone
Mometason
Mometasona
Mométasone
Mometasone
Mometasonum

External IDs

LAS-41002 / LAS41002

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Unlock Additional Data
Mometasone Furoate	Spray, metered	50 ug/1	Nasal	Golden State Medical Supply, Inc.	2016-03-29	Not applicable
Mometasone Furoate	Spray, metered	50 ug/1	Nasal	Apotex Corporation	2016-03-22	Not applicable
Mometasone Furoate	Spray, metered	50 ug/1	Nasal	Remedy Repack	2018-03-20	Not applicable
Momexin	Cream	1 mg/1g	Topical	Innocutis Holdings, LLC	2009-05-01	2011-12-20

Additional Data Available

Application Number

A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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Product Code

A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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International/Other Brands

Ecural (Essex pharma) / Elocom (Merck) / Elomet (Schering-Plough) / Eziwin (Intas) / mometAid (Progreś Laboratories) / Novasone (Schering-Plough)

Categories

UNII

8HR4QJ6DW8

CAS number

105102-22-5

Weight

Average: 427.361
Monoisotopic: 426.136464798

Chemical Formula

C₂₂H₂₈Cl₂O₄

InChI Key

QLIIKPVHVRXHRI-CXSFZGCWSA-N

InChI

InChI=1S/C22H28Cl2O4/c1-12-8-16-15-5-4-13-9-14(25)6-7-19(13,2)21(15,24)17(26)10-20(16,3)22(12,28)18(27)11-23/h6-7,9,12,15-17,26,28H,4-5,8,10-11H2,1-3H3/t12-,15+,16+,17+,19+,20+,21+,22+/m1/s1

IUPAC Name

(1R,2R,3aS,3bS,9aS,9bR,10S,11aS)-9b-chloro-1-(2-chloroacetyl)-1,10-dihydroxy-2,9a,11a-trimethyl-1H,2H,3H,3aH,3bH,4H,5H,7H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-7-one

SMILES

[H][C@@]12C[C@@H](C)[C@](O)(C(=O)CCl)[C@@]1(C)C[C@H](O)[C@@]1(Cl)[C@@]2([H])CCC2=CC(=O)C=C[C@]12C

Pharmacology

Indication

The 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.

Associated Conditions

Pharmacodynamics

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. The clinical significance of these findings is unknown.

Mechanism of action

Unbound corticosteroids cross cell membranes and bind with high affinity to specific cytoplasmic receptors. Inflammation is decreased by diminishing the release of leukocytic acid hydrolases, prevention of macrophage accumulation at inflamed sites, interference with leukocyte adhesion to the capillary wall, reduction of capillary membrane permeability, reduction of complement components, inhibition of histamine and kinin release, and interference with the formation of scar tissue. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A₂ inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. Mometasone furoate 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.

Target	Actions	Organism
AGlucocorticoid receptor	agonist	Humans
UProgesterone receptor	agonist	Humans

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Additional Data Available

Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available

Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available

Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

Nasal spray is virtually undetectable in plasma

Volume of distribution

Not Available

Protein binding

98% to 99% (in a concentration range of 5 to 500 ng/mL).

Metabolism

Hepatic. Extensive metabolism to multiple metabolites. There are no major metabolites detectable in plasma. Upon in vitro incubation, one of the minor metabolites formed is 6ß-hydroxy-mometasone furoate. In human liver microsomes, the formation of the metabolite is regulated by cytochrome P-450 3A4.

Mometasone
6-beta-hydroxy-mometasone furoate

Route of elimination

Not Available

Half life

5.8 hours

Clearance

Not Available

Toxicity

The potential for acute toxic effects following overdose with the mometasone inhaler is low. However, habitual overuse of the product can cause symptoms of steroid overload, including menstrual irregularities, acne, obesity, and muscle weakness. Single oral doses up to 8000 µg have been studied on human volunteers with no adverse events reported.

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

Drug	Interaction
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(R)-warfarin	The therapeutic efficacy of (R)-warfarin can be increased when used in combination with Mometasone.
(S)-Warfarin	The therapeutic efficacy of (S)-Warfarin can be increased when used in combination with Mometasone.
1-Testosterone	The risk or severity of edema formation can be increased when 1-Testosterone is combined with Mometasone.
16-Bromoepiandrosterone	The risk or severity of edema formation can be increased when 16-Bromoepiandrosterone is combined with Mometasone.
19-norandrostenedione	The risk or severity of edema formation can be increased when 19-norandrostenedione is combined with Mometasone.
1alpha-Hydroxyvitamin D5	The therapeutic efficacy of 1alpha-Hydroxyvitamin D5 can be decreased when used in combination with Mometasone.
2-Methoxyethanol	The risk or severity of adverse effects can be increased when Mometasone is combined with 2-Methoxyethanol.
2,4-thiazolidinedione	The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Mometasone.
3,5-diiodothyropropionic acid	The therapeutic efficacy of 3,5-diiodothyropropionic acid can be decreased when used in combination with Mometasone.
4-hydroxycoumarin	The metabolism of 4-hydroxycoumarin can be decreased when combined with Mometasone.

Additional Data Available

Extended Description

Extended description of the mechanism of action and particular properties of each drug interaction.

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Severity

A severity rating for each drug interaction, from minor to major.

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Evidence Level

A rating for the strength of the evidence supporting each drug interaction.

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Action

Evidence Level

An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions

Not Available

References

Synthesis Reference

Pui-Ho Yuen, Charles Eckhart, Teresa Etlinger, Nancy Levine, "Mometasone furoate monohydrate, process for making same and pharmaceutical compositions." U.S. Patent US6127353, issued April, 1988.

US6127353

General References

Not Available

External Links

Human Metabolome Database: HMDB0014902
KEGG Drug: D08227
KEGG Compound: C07816
PubChem Compound: 441335
PubChem Substance: 46505288
ChemSpider: 390090
ChEBI: 6970
ChEMBL: CHEMBL1201404
Therapeutic Targets Database: DAP001042
PharmGKB: PA450541
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
PDRhealth: PDRhealth Drug Page
Wikipedia: Mometasone

ATC Codes

R03AK09 — Formoterol and mometasone

AHFS Codes

68:04.00 — Adrenals
84:06.00 — Anti-inflammatory Agents
52:08.08 — Corticosteroids

FDA label

Download (152 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
1	Active Not Recruiting	Treatment	Spinal Cord Injuries (SCI)	1
1	Completed	Not Available	Healthy Volunteers	1
1	Completed	Treatment	Allergic Rhinitis (AR)	2
1	Completed	Treatment	Asthma Bronchial	1
1	Completed	Treatment	Atopic Dermatitis (AD)	1
1	Completed	Treatment	Healthy Volunteers	2
1	Completed	Treatment	Psoriasis Vulgaris (Plaque Psoriasis)	1
1, 2	Completed	Not Available	Seasonal Allergic Rhinitis (SAR)	1
2	Completed	Treatment	Acute Rhinosinusitis	1
2	Completed	Treatment	Airway Inflammation / Asthma Bronchial	1
2	Completed	Treatment	Asthma Bronchial	7
2	Completed	Treatment	Chronic Rhinosinusitis	1
2	Completed	Treatment	Polyps, Nasal	1
2	Completed	Treatment	Psoriasis Vulgaris (Plaque Psoriasis)	1
2	Completed	Treatment	Rhinitis, Allergic, Perennial	1
2	Completed	Treatment	Seasonal Allergic Rhinitis (SAR)	2
2	Completed	Treatment	Sickle Cell Disorders	1
2	Enrolling by Invitation	Treatment	Polyps, Nasal	1
2	Recruiting	Treatment	Sickle Cell Disorders	1
2	Suspended	Treatment	Psoriasis Vulgaris (Plaque Psoriasis)	1
2	Terminated	Treatment	Oesophagitis, Eosinophilic	1
2	Withdrawn	Treatment	Asthma Bronchial	1
3	Active Not Recruiting	Treatment	Polyps, Nasal	1
3	Completed	Not Available	Perennial Allergic Rhinitis (PAR)	1
3	Completed	Supportive Care	Cancer, Breast / Dermatologic Complications / Radiation Toxicity / Skin Reactions Secondary to Radiation Therapy	1
3	Completed	Treatment	Acute Rhinosinusitis	1
3	Completed	Treatment	Allergies / Conjunctivitis / Rhinitis / Rhinoconjunctivitis	2
3	Completed	Treatment	Asthma Bronchial	6
3	Completed	Treatment	Chronic Obstructive Pulmonary Disease (COPD)	2
3	Completed	Treatment	Chronic Rhinosinusitis / Nasal Polyposis	1
3	Completed	Treatment	Otitis Media With Effiusion	1
3	Completed	Treatment	Perennial Allergic Rhinitis (PAR)	5
3	Completed	Treatment	Perennial Allergic Rhinitis (PAR) / Rhinitis, Allergic, Perennial	1
3	Completed	Treatment	Polyps, Nasal	2
3	Completed	Treatment	Rhinitis, Allergic, Perennial	4
3	Completed	Treatment	Rhinitis, Allergic, Seasonal	1
3	Completed	Treatment	Seasonal Allergic Rhinitis (SAR)	4
3	Not Yet Recruiting	Treatment	Allergic Rhinitis (AR)	2
3	Not Yet Recruiting	Treatment	Allergies	1
3	Recruiting	Treatment	Mild Asthma	1
3	Unknown Status	Not Available	Itching / Nasal Obstruction / Sneezing	1
3	Unknown Status	Treatment	Mild to Moderate Persistent Allergic Rhinitis	1
3	Withdrawn	Treatment	Obstructive Sleep Apnea (Mild, Moderate, Severe) as Per Polysomnography	1
4	Active Not Recruiting	Treatment	Seasonal Allergic Rhinitis (SAR)	1
4	Completed	Not Available	Atopic Dermatitis (AD)	1
4	Completed	Other	Rhinitis, Allergic, Perennial and Seasonal	1
4	Completed	Treatment	Adenoidal Hypertrophy	1
4	Completed	Treatment	Adenoids	1
4	Completed	Treatment	Allergic Rhinitis (AR)	2
4	Completed	Treatment	Asthma Bronchial	5
4	Completed	Treatment	Asthma Bronchial / Rhinitis / Sinusitis	1
4	Completed	Treatment	Obstructive Sleep Apnea (OSA) / Perennial Allergic Rhinitis (PAR) / Sleep Disorder	1
4	Completed	Treatment	Psoriasis	1
4	Recruiting	Health Services Research	Early Radiation Dermatitis	1
4	Recruiting	Treatment	Asthma Bronchial / Sinusitis	1
4	Recruiting	Treatment	Choanal Atresia	1
4	Recruiting	Treatment	Chronic Rhinosinusitis Without Nasal Polyps	1
4	Terminated	Basic Science	Polyps, Nasal	1
4	Terminated	Treatment	Adenoidectomy / Adenoids Hypertrophy / Nasal Obstruction	1
4	Terminated	Treatment	Asthma Bronchial	2
4	Terminated	Treatment	Asthma Bronchial / Rhinitis, Allergic, Seasonal	1
4	Terminated	Treatment	Perennial Allergic Rhinitis (PAR)	1
4	Terminated	Treatment	Seasonal Allergic Rhinitis (SAR)	1
4	Unknown Status	Treatment	Asthma Bronchial / Polyps, Nasal / Sinusitis	1
4	Unknown Status	Treatment	Phimosis	1
4	Unknown Status	Treatment	Vitiligo	1
4	Withdrawn	Treatment	Enuresis / Obstructive Sleep Apnea (OSA) / Sleep Disordered Breathing (SDB)	1
Not Available	Completed	Not Available	Allergic Rhinitis (AR)	1
Not Available	Completed	Not Available	Rhinitis, Allergic, Perennial / Rhinitis, Allergic, Seasonal	1
Not Available	Completed	Not Available	Seasonal Allergic Rhinitis (SAR)	1
Not Available	Completed	Other	Asthma Bronchial	1
Not Available	Recruiting	Not Available	Asthma Bronchial	1
Not Available	Recruiting	Not Available	Asthma in Children	1
Not Available	Suspended	Treatment	Asthma Bronchial / Rhinitis	1

Pharmacoeconomics

Manufacturers

Schering corp sub schering plough corp
Altana inc
G and w laboratories inc
Glenmark generics inc usa
Taro pharmaceuticals usa inc
Tolmar inc
Nycomed us inc
Perrigo co
Perrigo new york inc
Schering corp
Schering plough healthcare products inc
Schering-Plough

Packagers

A-S Medication Solutions LLC
Dispensing Solutions
Diversified Healthcare Services Inc.
Dixie Chem Tec Inc.
E. Fougera and Co.
G & W Labs
Glenmark Generics Ltd.
Harris Pharmaceutical Inc.
JSJ Pharmaceuticals Inc.
Lake Erie Medical and Surgical Supply
Nycomed Inc.
Perrigo Co.
Pharmedix
Physicians Total Care Inc.
Sandoz
Schering Corp.
Schering-Plough Inc.
Taro Pharmaceuticals USA
Tolmar Inc.

Dosage forms

Form	Route	Strength
Spray, metered	Nasal	50 ug/1
Cream	Topical	1 mg/1g

Prices

Unit description	Cost	Unit
Asmanex 120 Metered Doses 220 mcg/inh Aerosol 0.24 gm Inhaler	230.27USD	inhaler
Asmanex twisthaler 220 mcg #30	131.47USD	inhaler
Asmanex twisthaler 110 mcg #30	121.76USD	inhaler
Nasonex 50 mcg/act Suspension 50 mcg Nasal Spray	116.82USD	inhaler
Elocon 0.1% Lotion 60ml Bottle	86.71USD	bottle
Elocon 0.1% Cream 45 gm Tube	79.13USD	tube
Elocon 0.1% Ointment 45 gm Tube	76.45USD	tube
Mometasone Furoate 0.1% Solution 60ml Bottle	64.99USD	bottle
Mometasone Furoate 0.1% Cream 45 gm Tube	50.96USD	tube
Elocon 0.1% Lotion 30ml Bottle	49.85USD	bottle
Elocon 0.1% Ointment 15 gm Tube	49.85USD	tube
Elocon 0.1% Cream 15 gm Tube	47.68USD	tube
Mometasone Furoate 0.1% Ointment 45 gm Tube	35.99USD	tube
Mometasone Furoate 0.1% Solution 30ml Bottle	32.99USD	bottle
Mometasone Furoate 0.1% Cream 15 gm Tube	29.99USD	tube
Mometasone Furoate 0.1% Ointment 15 gm Tube	19.19USD	tube
Nasonex 50 mcg nasal spray	6.37USD	g
Elocon 0.1% cream	2.69USD	g
Mometasone furoate 0.1% cream	1.42USD	g
Elocom 0.1 % Cream	0.7USD	g
Elocom 0.1 % Ointment	0.63USD	g
Elocom 0.1 % Lotion	0.47USD	g
Pms-Mometasone 0.1 % Ointment	0.35USD	g
Ratio-Mometasone 0.1 % Ointment	0.35USD	g
Taro-Mometasone 0.1 % Ointment	0.35USD	g
Taro-Mometasone 0.1 % Lotion	0.33USD	g

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
Unlock Additional Data
US5394868	No	1995-03-07	2012-06-25
CA2282360	No	2004-11-09	2018-03-16
CA2091360	No	1997-04-08	2011-09-06
US6127353	Yes	2000-10-03	2018-04-03
US6240918	Yes	2001-06-05	2017-08-20
US8173172	Yes	2012-05-08	2018-09-17
US6503537	Yes	2003-01-07	2018-09-17
US5829434	Yes	1998-11-03	2016-05-03
US6068832	No	2000-05-30	2017-08-27
US7067502	No	2006-06-27	2020-05-21
US7566705	No	2009-07-28	2020-05-21
US8109918	No	2012-02-07	2024-03-12
US7951131	No	2011-05-31	2024-03-12
US8025635	No	2011-09-27	2027-06-12
US9585681	No	2017-03-07	2026-04-04
US7951130	No	2011-05-31	2024-03-12
US7544192	No	2009-06-09	2026-11-29
US7951133	No	2011-05-31	2024-03-12
US7713255	No	2010-05-11	2024-03-12
US7662141	No	2010-02-16	2024-03-12
US8763222	No	2014-07-01	2032-02-08

Additional Data Available

Filed On

The date on which a patent was filed with the relevant government.

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Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	218-220 °C	Not Available
water solubility	Practically insoluble.	Not Available
logP	2.1	Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.00523 mg/mL	ALOGPS
logP	2.81	ALOGPS
logP	3.5	ChemAxon
logS	-4.9	ALOGPS
pKa (Strongest Acidic)	12.49	ChemAxon
pKa (Strongest Basic)	-3.3	ChemAxon
Physiological Charge	0	ChemAxon
Hydrogen Acceptor Count	4	ChemAxon
Hydrogen Donor Count	2	ChemAxon
Polar Surface Area	74.6 Å²	ChemAxon
Rotatable Bond Count	2	ChemAxon
Refractivity	110.29 m³·mol^-1	ChemAxon
Polarizability	43.82 Å³	ChemAxon
Number of Rings	4	ChemAxon
Bioavailability	1	ChemAxon
Rule of Five	Yes	ChemAxon
Ghose Filter	Yes	ChemAxon
Veber's Rule	No	ChemAxon
MDDR-like Rule	No	ChemAxon

Predicted ADMET features

Property	Value	Probability
Human Intestinal Absorption	+	0.995
Blood Brain Barrier	+	0.9721
Caco-2 permeable	+	0.7845
P-glycoprotein substrate	Substrate	0.7849
P-glycoprotein inhibitor I	Non-inhibitor	0.7635
P-glycoprotein inhibitor II	Non-inhibitor	0.656
Renal organic cation transporter	Non-inhibitor	0.7753
CYP450 2C9 substrate	Non-substrate	0.852
CYP450 2D6 substrate	Non-substrate	0.9135
CYP450 3A4 substrate	Substrate	0.8028
CYP450 1A2 substrate	Non-inhibitor	0.9383
CYP450 2C9 inhibitor	Non-inhibitor	0.8572
CYP450 2D6 inhibitor	Non-inhibitor	0.8429
CYP450 2C19 inhibitor	Non-inhibitor	0.8966
CYP450 3A4 inhibitor	Non-inhibitor	0.6761
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.8898
Ames test	Non AMES toxic	0.8962
Carcinogenicity	Non-carcinogens	0.9393
Biodegradation	Not ready biodegradable	1.0
Rat acute toxicity	1.9124 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.9254
hERG inhibition (predictor II)	Non-inhibitor	0.6092

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	Not Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available

Taxonomy

Description: This compound belongs to the class of organic compounds known as gluco/mineralocorticoids, progestogins and derivatives. These are steroids with a structure based on a hydroxylated prostane moiety.
Kingdom: Organic compounds
Super Class: Lipids and lipid-like molecules
Class: Steroids and steroid derivatives
Sub Class: Pregnane steroids
Direct Parent: Gluco/mineralocorticoids, progestogins and derivatives
Alternative Parents: 20-oxosteroids / 11-beta-hydroxysteroids / 17-hydroxysteroids / Halogenated steroids / 3-oxo delta-1,4-steroids / Delta-1,4-steroids / Tertiary alcohols / Alpha-hydroxy ketones / Alpha-chloroketones / Secondary alcohols
show 7 more
Substituents: Progestogin-skeleton / 20-oxosteroid / Hydroxysteroid / Halo-steroid / 9-halo-steroid / Oxosteroid / 11-beta-hydroxysteroid / 11-hydroxysteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid
show 23 more
Molecular Framework: Aliphatic homopolycyclic compounds
External Descriptors: 11beta-hydroxy steroid, 17alpha-hydroxy steroid, 20-oxo steroid, 3-oxo-Delta(1),Delta(4)-steroid, chlorinated steroid (CHEBI:6970)

Targets

Details1. Glucocorticoid receptor

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Agonist

General Function: Zinc ion binding
Specific Function: Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modula...
Gene Name: NR3C1
Uniprot ID: P04150
Uniprot Name: Glucocorticoid receptor
Molecular Weight: 85658.57 Da

References

Isogai M, Shimizu H, Esumi Y, Terasawa T, Okada T, Sugeno K: Binding affinities of mometasone furoate and related compounds including its metabolites for the glucocorticoid receptor of rat skin tissue. J Steroid Biochem Mol Biol. 1993 Feb;44(2):141-5. [PubMed:8439518]
Lumry WR: A review of the preclinical and clinical data of newer intranasal steroids used in the treatment of allergic rhinitis. J Allergy Clin Immunol. 1999 Oct;104(4 Pt 1):S150-8. [PubMed:10518812]
Smith CL, Kreutner W: In vitro glucocorticoid receptor binding and transcriptional activation by topically active glucocorticoids. Arzneimittelforschung. 1998 Sep;48(9):956-60. [PubMed:9793625]
Zhang X, Moilanen E, Adcock IM, Lindsay MA, Kankaanranta H: Divergent effect of mometasone on human eosinophil and neutrophil apoptosis. Life Sci. 2002 Aug 16;71(13):1523-34. [PubMed:12127907]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Details2. Progesterone receptor

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Agonist

General Function: Zinc ion binding
Specific Function: The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor ...
Gene Name: PGR
Uniprot ID: P06401
Uniprot Name: Progesterone receptor
Molecular Weight: 98979.96 Da

References

Madauss KP, Deng SJ, Austin RJ, Lambert MH, McLay I, Pritchard J, Short SA, Stewart EL, Uings IJ, Williams SP: Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes. J Med Chem. 2004 Jun 17;47(13):3381-7. [PubMed:15189034]

Enzymes

Details1. Cytochrome P450 2C8

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Steroid hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name: CYP2C8
Uniprot ID: P10632
Uniprot Name: Cytochrome P450 2C8
Molecular Weight: 55824.275 Da

References

Walsky RL, Gaman EA, Obach RS: Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78. [PubMed:15601807]
Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Details2. Cytochrome P450 3A4

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate

General Function: Vitamin d3 25-hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name: CYP3A4
Uniprot ID: P08684
Uniprot Name: Cytochrome P450 3A4
Molecular Weight: 57342.67 Da

References

Berger WE, Milgrom H, Chervinsky P, Noonan M, Weinstein SF, Lutsky BN, Staudinger H: Effects of treatment with mometasone furoate dry powder inhaler in children with persistent asthma. Ann Allergy Asthma Immunol. 2006 Nov;97(5):672-80. doi: 10.1016/S1081-1206(10)61099-X. [PubMed:17165278]
Sharpe M, Jarvis B: Inhaled mometasone furoate: a review of its use in adults and adolescents with persistent asthma. Drugs. 2001;61(9):1325-50. [PubMed:11511026]

Drug created on June 13, 2005 07:24 / Updated on April 25, 2019 16:16

Mometasone

Identification

Structure for Mometasone (DB00764)

Pharmacology

Interactions

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Taxonomy

Targets

References

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Enzymes

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References