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Identification
NameMometasone
Accession NumberDB00764  (APRD00289)
TypeSmall Molecule
GroupsApproved, Vet Approved
Description

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
Thumb
Synonyms
(+)-Mometasone
Mometason
Mometason furoat-1-Wasser
Mometasona
Mométasone
Mométasone (furoate de)
Mometasone Furoate
Mometasone Furoate Hydrate
Mometasonfuroat
Mometasoni furoas
Mometasonum
External Identifiers
  • Sch 32088
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Asmanexinhalant220 ug/1respiratory (inhalation)Physicians Total Care, Inc.2006-03-09Not applicableUs
Asmanexinhalant110 ug/1respiratory (inhalation)Merck Sharp & Dohme Corp.2005-03-30Not applicableUs
Asmanexinhalant220 ug/1respiratory (inhalation)Merck Sharp & Dohme Corp.2005-03-30Not applicableUs
Asmanex HFAaerosol100 ug/1respiratory (inhalation)Merck Sharp & Dohme Corp.2014-04-25Not applicableUs
Asmanex HFAaerosol200 ug/1respiratory (inhalation)Merck Sharp & Dohme Corp.2014-04-25Not applicableUs
Asmanex Twisthalerpowder100 mcginhalationMerck Canada Inc2015-04-08Not applicableCanada
Asmanex Twisthalerpowder400 mcginhalationMerck Canada Inc2011-12-21Not applicableCanada
Asmanex Twisthalerpowder200 mcginhalationMerck Canada Inc2011-12-21Not applicableCanada
Elocom Creamcream0.1 %topicalMerck Canada Inc1991-12-31Not applicableCanada
Elocom Lotionlotion1 mgtopicalMerck Canada Inc1991-12-31Not applicableCanada
Elocom Ointmentointment0.1 %topicalMerck Canada Inc1991-12-31Not applicableCanada
Eloconointment1 mg/gtopicalMerck Sharp & Dohme Corp.1987-04-30Not applicableUs
Eloconcream1 mg/gtopicalMerck Sharp & Dohme Corp.1987-05-06Not applicableUs
Eloconcream1 mg/gtopicalPhysicians Total Care, Inc.1994-05-31Not applicableUs
Eloconcream1 mg/gtopicalA S Medication Solutions Llc1987-05-06Not applicableUs
Eloconlotion1 mg/mLtopicalMerck Sharp & Dohme Corp.1989-03-30Not applicableUs
Mometasone Furoate Monohydratespray, metered50 ug/1nasalSandoz Inc.2016-03-25Not applicableUs
Nasonexspray, metered50 ug/1nasalPhysicians Total Care, Inc.2000-05-12Not applicableUs
Nasonexspray, metered50 ug/1nasalMerck Sharp & Dohme Corp.1997-10-01Not applicableUs
Nasonexspray, metered50 ug/1nasalREMEDYREPACK INC.2013-06-13Not applicableUs
Nasonexspray, metered dose50 mcgnasalMerck Canada Inc1998-09-15Not applicableCanada
PMS-mometasonelotion.1 %topicalPharmascience IncNot applicableNot applicableCanada
PMS-mometasonecream.1 %topicalPharmascience IncNot applicableNot applicableCanada
PMS-mometasoneointment0.1 %topicalPharmascience Inc2003-11-25Not applicableCanada
PMS-mometasoneointment0.1 %topicalPharmascience Inc2005-11-03Not applicableCanada
Ratio-mometasoneointment0.1 %topicalTeva Canada Limited2003-11-04Not applicableCanada
Sandoz Mometasonespray, metered dose50 mcgnasalSandoz Canada IncorporatedNot applicableNot applicableCanada
Taro-mometasone Creamcream0.1 %topicalTaro Pharmaceuticals Inc2011-06-08Not applicableCanada
Taro-mometasone Lotionsolution0.1 %topicalTaro Pharmaceuticals Inc2009-12-01Not applicableCanada
Taro-mometasone Ointmentointment0.1 %topicalTaro Pharmaceuticals Inc2005-06-21Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-mometasonespray, metered dose50 mcgnasalApotex Inc2013-03-25Not applicableCanada
Mometasone Furoatecream1 mg/gtopicalTaro Pharmaceuticals U.S.A., Inc.2004-12-21Not applicableUs
Mometasone Furoatesolution1 mg/mLtopicalPhysicians Total Care, Inc.2006-03-30Not applicableUs
Mometasone Furoatecream1 mg/gtopicalE. Fougera & Co. a division of Fougera Pharmaceuticals Inc.2005-04-08Not applicableUs
Mometasone Furoatecream1 mg/gtopicalImpax Generics2007-04-18Not applicableUs
Mometasone Furoatecream1 mg/gtopicalHarris Pharmaceutical, Inc.2006-08-23Not applicableUs
Mometasone Furoatecream1 mg/gtopicalSTAT Rx USA LLC2006-08-23Not applicableUs
Mometasone Furoatelotion1 mg/mLtopicalGlenmark Pharmaceuticals Inc., Usa2010-08-09Not applicableUs
Mometasone Furoateointment1 mg/gtopicalTaro Pharmaceuticals U.S.A., Inc.2004-12-03Not applicableUs
Mometasone Furoatecream1 mg/gtopicalProficient Rx LP2008-05-28Not applicableUs
Mometasone Furoatesolution1 mg/mLtopicalG&W Laboratories, Inc.2014-03-04Not applicableUs
Mometasone Furoateointment1 mg/gtopicalGlenmark Pharmaceuticals Inc., Usa2008-05-28Not applicableUs
Mometasone Furoatesolution1 mg/mLtopicalTaro Pharmaceuticals U.S.A., Inc.2006-03-15Not applicableUs
Mometasone Furoatecream1 mg/gtopicalProficient Rx LP2004-12-21Not applicableUs
Mometasone Furoateointment1 mg/gtopicalG&W Laboratories, Inc.2014-03-04Not applicableUs
Mometasone Furoatespray, metered50 ug/1nasalGolden State Medical Supply, Inc.2016-03-29Not applicableUs
Mometasone Furoatecream1 mg/gtopicalPerrigo New York Inc.2004-12-21Not applicableUs
Mometasone Furoatecream1 mg/gtopicalGlenmark Pharmaceuticals Inc., Usa2008-05-28Not applicableUs
Mometasone Furoatecream1 mg/gtopicalClinical Solutions Wholesale2005-11-28Not applicableUs
Mometasone Furoatecream1 mg/gtopicalG&W Laboratories, Inc.2006-08-23Not applicableUs
Mometasone Furoatespray, metered50 ug/1nasalApotex Corp.2016-03-21Not applicableUs
Mometasone Furoatesolution1 mg/mLtopicalPerrigo New York Inc2008-12-11Not applicableUs
Mometasone Furoateointment1 mg/gtopicalDispensing Solutions, Inc.2006-10-18Not applicableUs
Mometasone Furoatesolution1 mg/mLtopicalE. Fougera & Co. a division of Fougera Pharmaceuticals Inc.2007-11-29Not applicableUs
Mometasone Furoateointment1 mg/gtopicalPerrigo New York Inc2008-07-18Not applicableUs
Mometasone Furoateointment1 mg/gtopicalPhysicians Total Care, Inc.2010-12-22Not applicableUs
Mometasone Furoateointment1 mg/gtopicalHarris Pharmaceutical, Inc.2006-10-18Not applicableUs
Mometasone Furoateointment1 mg/gtopicalRebel Distributors Corp2006-10-18Not applicableUs
Mometasone Furoateointment1 mg/gtopicalImpax Generics2003-11-14Not applicableUs
Mometasone Furoateointment1 mg/gtopicalREMEDYREPACK INC.2013-06-17Not applicableUs
Mometasone Furoateointment1 mg/gtopicalE. Fougera & Co. a division of Fougera Pharmaceuticals Inc.2005-03-28Not applicableUs
Mometasone Furoatelotion1 mg/gtopicalImpax Generics2007-11-21Not applicableUs
Mometasone Furoatecream1 mg/gtopicalPhysicians Total Care, Inc.2006-03-30Not applicableUs
Mometasone Furoatesolution1 mg/mLtopicalHarris Pharmaceutical, Inc.2014-03-04Not applicableUs
Mometasone Furoatecream1 mg/gtopicalRebel Distributors Corp2006-08-23Not applicableUs
Approved Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Mosasprayspray, metered dose50 mcgnasalSandoz Canada IncorporatedNot applicableNot applicableCanada
Nasal Allergy and Congestion Reliefspray, metered dose50 mcgnasalApotex IncNot applicableNot applicableCanada
Nasonex Allergy and Congestionspray, metered dose50 mcgnasalMerck Canada IncNot applicableNot applicableCanada
Unapproved/Other Products Not Available
International Brands
NameCompany
EcuralEssex pharma
ElocomMerck
ElometSchering-Plough
EziwinIntas
mometAidProgreś Laboratories
NovasoneSchering-Plough
Brand mixtures
NameLabellerIngredients
DuleraMerck Sharp & Dohme Corp.
ZenhaleMerck Canada Inc
Salts
Name/CASStructureProperties
Mometasone furoate monohydrate
ThumbNot applicableDBSALT001244
Categories
UNII8HR4QJ6DW8
CAS number105102-22-5
WeightAverage: 427.361
Monoisotopic: 426.136464798
Chemical FormulaC22H28Cl2O4
InChI KeyInChIKey=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,2S,10S,11S,13R,14R,15S,17S)-1-chloro-14-(2-chloroacetyl)-14,17-dihydroxy-2,13,15-trimethyltetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadeca-3,6-dien-5-one
SMILES
[H][C@@]12C[C@@H](C)[C@](O)(C(=O)CCl)[C@@]1(C)C[[email protected]](O)[C@@]1(Cl)[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassPregnane steroids
Direct ParentGluco/mineralocorticoids, progestogins and derivatives
Alternative Parents
Substituents
  • Progestogin-skeleton
  • 20-oxosteroid
  • 17-hydroxysteroid
  • 11-hydroxysteroid
  • 11-beta-hydroxysteroid
  • Oxosteroid
  • Hydroxysteroid
  • Halo-steroid
  • 9-halo-steroid
  • 3-oxosteroid
  • 3-oxo-delta-1,4-steroid
  • Delta-1,4-steroid
  • Tertiary alcohol
  • Cyclic alcohol
  • Alpha-hydroxy ketone
  • Cyclic ketone
  • Secondary alcohol
  • Ketone
  • Halohydrin
  • Chlorohydrin
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Alkyl halide
  • Alkyl chloride
  • Alcohol
  • Aliphatic homopolycyclic compound
Molecular FrameworkAliphatic homopolycyclic compounds
External Descriptors
Pharmacology
IndicationThe 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.
PharmacodynamicsMometasone 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 actionUnbound 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.
Related Articles
AbsorptionNasal spray is virtually undetectable in plasma
Volume of distributionNot Available
Protein binding98% 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.

SubstrateEnzymesProduct
Mometasone
Not Available
6-beta-hydroxy-mometasone furoateDetails
Route of eliminationNot Available
Half life5.8 hours
ClearanceNot Available
ToxicityThe 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.995
Blood Brain Barrier+0.9721
Caco-2 permeable+0.7845
P-glycoprotein substrateSubstrate0.7849
P-glycoprotein inhibitor INon-inhibitor0.7635
P-glycoprotein inhibitor IINon-inhibitor0.656
Renal organic cation transporterNon-inhibitor0.7753
CYP450 2C9 substrateNon-substrate0.852
CYP450 2D6 substrateNon-substrate0.9135
CYP450 3A4 substrateSubstrate0.8028
CYP450 1A2 substrateNon-inhibitor0.9383
CYP450 2C9 inhibitorNon-inhibitor0.8572
CYP450 2D6 inhibitorNon-inhibitor0.8429
CYP450 2C19 inhibitorNon-inhibitor0.8966
CYP450 3A4 inhibitorNon-inhibitor0.6761
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8898
Ames testNon AMES toxic0.8962
CarcinogenicityNon-carcinogens0.9393
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.9124 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9254
hERG inhibition (predictor II)Non-inhibitor0.6092
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
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
Dosage forms
FormRouteStrength
Inhalantrespiratory (inhalation)110 ug/1
Inhalantrespiratory (inhalation)220 ug/1
Aerosolrespiratory (inhalation)100 ug/1
Aerosolrespiratory (inhalation)200 ug/1
Powderinhalation100 mcg
Powderinhalation200 mcg
Powderinhalation400 mcg
Aerosolrespiratory (inhalation)
Creamtopical0.1 %
Lotiontopical1 mg
Ointmenttopical0.1 %
Creamtopical1 mg/g
Lotiontopical1 mg/mL
Ointmenttopical1 mg/g
Lotiontopical1 mg/g
Solutiontopical1 mg/mL
Spray, meterednasal50 ug/1
Spray, metered dosenasal50 mcg
Creamtopical.1 %
Lotiontopical.1 %
Solutiontopical0.1 %
Aerosol, metered doseinhalation
Prices
Unit descriptionCostUnit
Asmanex 120 Metered Doses 220 mcg/inh Aerosol 0.24 gm Inhaler230.27USD inhaler
Asmanex twisthaler 220 mcg #30131.47USD inhaler
Asmanex twisthaler 110 mcg #30121.76USD inhaler
Nasonex 50 mcg/act Suspension 50 mcg Nasal Spray116.82USD inhaler
Elocon 0.1% Lotion 60ml Bottle86.71USD bottle
Elocon 0.1% Cream 45 gm Tube79.13USD tube
Elocon 0.1% Ointment 45 gm Tube76.45USD tube
Mometasone Furoate 0.1% Solution 60ml Bottle64.99USD bottle
Mometasone Furoate 0.1% Cream 45 gm Tube50.96USD tube
Elocon 0.1% Lotion 30ml Bottle49.85USD bottle
Elocon 0.1% Ointment 15 gm Tube49.85USD tube
Elocon 0.1% Cream 15 gm Tube47.68USD tube
Mometasone Furoate 0.1% Ointment 45 gm Tube35.99USD tube
Mometasone Furoate 0.1% Solution 30ml Bottle32.99USD bottle
Mometasone Furoate 0.1% Cream 15 gm Tube29.99USD tube
Mometasone Furoate 0.1% Ointment 15 gm Tube19.19USD tube
Nasonex 50 mcg nasal spray6.37USD g
Elocon 0.1% cream2.69USD g
Mometasone furoate 0.1% cream1.42USD g
Elocom 0.1 % Cream0.7USD g
Elocom 0.1 % Ointment0.63USD g
Elocom 0.1 % Lotion0.47USD g
Pms-Mometasone 0.1 % Ointment0.35USD g
Ratio-Mometasone 0.1 % Ointment0.35USD g
Taro-Mometasone 0.1 % Ointment0.35USD g
Taro-Mometasone 0.1 % Lotion0.33USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2091360 No1997-04-082011-09-06Canada
CA2282360 No2004-11-092018-03-16Canada
US5394868 No1995-06-252012-06-25Us
US5829434 Yes1996-05-032016-05-03Us
US6068832 No1997-08-272017-08-27Us
US6127353 Yes1998-04-032018-04-03Us
US6240918 Yes1997-08-202017-08-20Us
US6503537 Yes1998-09-172018-09-17Us
US7067502 No2000-05-212020-05-21Us
US7566705 No2000-05-212020-05-21Us
US8173172 Yes1998-09-172018-09-17Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point218-220 °CNot Available
water solubilityPractically insoluble.Not Available
logP2.1Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00523 mg/mLALOGPS
logP2.81ALOGPS
logP3.5ChemAxon
logS-4.9ALOGPS
pKa (Strongest Acidic)12.48ChemAxon
pKa (Strongest Basic)-3.3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area74.6 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity110.29 m3·mol-1ChemAxon
Polarizability43.82 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot 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 ReferencesNot Available
External Links
ATC CodesR03BA07R03AK09R01AD09D07XC03D07AC13
AHFS Codes
  • 52:08.08
  • 84:06.00
PDB EntriesNot Available
FDA labelDownload (152 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AldesleukinMometasone may decrease the antineoplastic activities of Aldesleukin.
Amphotericin BMometasone may increase the hypokalemic activities of Amphotericin B.
CeritinibMometasone may increase the hyperglycemic activities of Ceritinib.
Corticorelin ovine triflutateThe therapeutic efficacy of Corticorelin can be decreased when used in combination with Mometasone.
DeferasiroxThe risk or severity of adverse effects can be increased when Mometasone is combined with Deferasirox.
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Mometasone.
LoxapineThe risk or severity of adverse effects can be increased when Mometasone is combined with Loxapine.
NelfinavirThe serum concentration of Mometasone can be increased when it is combined with Nelfinavir.
TorasemideMometasone may increase the hypokalemic activities of Torasemide.
TrichlormethiazideMometasone may increase the hypokalemic activities of Trichlormethiazide.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
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 modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Could act as a coactivator for STAT5-dependent transcription upon grow...
Gene Name:
NR3C1
Uniprot ID:
P04150
Molecular Weight:
85658.57 Da
References
  1. 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 ]
  2. 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 ]
  3. 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 ]
  4. 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 ]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. 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 ]
  2. 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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 24, 2016 03:05