Identification

Name
Mometasone
Accession Number
DB00764  (APRD00289)
Type
Small Molecule
Groups
Approved, 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
  • Mometasona
  • Mométasone
  • Mometasonum
External IDs
LAS-41002 / LAS41002
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Mometasone FuroateSpray, metered50 ug/1NasalApotex Corporation2016-03-22Not applicableUs
Mometasone FuroateSpray, metered50 ug/1NasalRemedy Repack2018-03-20Not applicableUs
Mometasone FuroateSpray, metered50 ug/1NasalGolden State Medical Supply2016-03-29Not applicableUs
MomexinCream1 mg/1gTopicalInnocutis Holdings, LLC2009-05-012011-12-20Us
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.

TargetActionsOrganism
AGlucocorticoid receptor
agonist
Human
UProgesterone receptor
agonist
Human
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.

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
DrugInteraction
(4R)-limoneneThe risk or severity of adverse effects can be increased when (4R)-limonene is combined with Mometasone.
1,10-PhenanthrolineThe risk or severity of adverse effects can be increased when Mometasone is combined with 1,10-Phenanthroline.
AceclofenacThe risk or severity of adverse effects can be increased when Aceclofenac is combined with Mometasone.
AcemetacinThe risk or severity of adverse effects can be increased when Acemetacin is combined with Mometasone.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Mometasone.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Mometasone.
AlclofenacThe risk or severity of adverse effects can be increased when Alclofenac is combined with Mometasone.
AlclometasoneThe risk or severity of adverse effects can be increased when Alclometasone is combined with Mometasone.
AldesleukinThe therapeutic efficacy of Aldesleukin can be decreased when used in combination with Mometasone.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Mometasone.
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
R03BA07 — MometasoneD07XC03 — MometasoneR01AD09 — MometasoneR03AK09 — Formoterol and mometasoneD07AC13 — 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
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentSpinal Cord Injuries (SCI)1
1CompletedNot AvailableHealthy Volunteers1
1CompletedTreatmentAllergic Rhinitis (AR)2
1CompletedTreatmentAsthma Bronchial1
1CompletedTreatmentAtopic Dermatitis (AD)1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentPsoriasis Vulgaris (Plaque Psoriasis)1
1, 2CompletedNot AvailableSeasonal Allergic Rhinitis (SAR)1
2CompletedTreatmentAcute Rhinosinusitis1
2CompletedTreatmentAirway Inflammation / Asthma Bronchial1
2CompletedTreatmentAsthma Bronchial7
2CompletedTreatmentChronic Rhinosinusitis1
2CompletedTreatmentPolyps, Nasal1
2CompletedTreatmentPsoriasis Vulgaris (Plaque Psoriasis)1
2CompletedTreatmentRhinitis, Allergic, Perennial1
2CompletedTreatmentSeasonal Allergic Rhinitis (SAR)2
2Enrolling by InvitationTreatmentOesophagitis, Eosinophilic1
2Enrolling by InvitationTreatmentPolyps, Nasal1
2RecruitingTreatmentSickle Cell Disorders1
2SuspendedTreatmentPsoriasis Vulgaris (Plaque Psoriasis)1
2WithdrawnTreatmentAsthma Bronchial1
3Active Not RecruitingTreatmentRhinitis, Allergic, Seasonal1
3CompletedNot AvailablePerennial Allergic Rhinitis (PAR)1
3CompletedSupportive CareCancer, Breast / Dermatologic Complications / Radiation Toxicity / Skin Reactions Secondary to Radiation Therapy1
3CompletedTreatmentAcute Rhinosinusitis1
3CompletedTreatmentAllergies / Conjunctivitis / Rhinitis / Rhinoconjunctivitis2
3CompletedTreatmentAsthma Bronchial7
3CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)2
3CompletedTreatmentChronic Rhinosinusitis / Nasal Polyposis1
3CompletedTreatmentOtitis Media With Effiusion1
3CompletedTreatmentPerennial Allergic Rhinitis (PAR)5
3CompletedTreatmentPerennial Allergic Rhinitis (PAR) / Rhinitis, Allergic, Perennial1
3CompletedTreatmentPolyps, Nasal2
3CompletedTreatmentRhinitis, Allergic, Perennial4
3CompletedTreatmentSeasonal Allergic Rhinitis (SAR)4
3Not Yet RecruitingTreatmentAllergic Rhinitis (AR)2
3Not Yet RecruitingTreatmentAllergies1
3RecruitingTreatmentMild Asthma1
3RecruitingTreatmentPolyps, Nasal1
3Unknown StatusNot AvailableItching / Nasal Obstruction / Sneezing1
3Unknown StatusTreatmentMild to Moderate Persistent Allergic Rhinitis1
3WithdrawnTreatmentObstructive Sleep Apnea (Mild, Moderate, Severe) as Per Polysomnography1
4Active Not RecruitingTreatmentSeasonal Allergic Rhinitis (SAR)1
4CompletedNot AvailableAtopic Dermatitis (AD)1
4CompletedOtherRhinitis, Allergic, Perennial and Seasonal1
4CompletedTreatmentAdenoidal Hypertrophy1
4CompletedTreatmentAdenoids1
4CompletedTreatmentAllergic Rhinitis (AR)2
4CompletedTreatmentAsthma Bronchial5
4CompletedTreatmentAsthma Bronchial / Rhinitis / Sinusitis1
4CompletedTreatmentObstructive Sleep Apnea (OSA) / Perennial Allergic Rhinitis (PAR) / Sleep Disorder1
4CompletedTreatmentPsoriasis1
4RecruitingHealth Services ResearchEarly Radiation Dermatitis1
4RecruitingTreatmentAsthma Bronchial / Sinusitis1
4RecruitingTreatmentChoanal Atresia1
4RecruitingTreatmentChronic Rhinosinusitis Without Nasal Polyps1
4TerminatedBasic SciencePolyps, Nasal1
4TerminatedTreatmentAdenoidectomy / Adenoids Hypertrophy / Nasal Obstruction1
4TerminatedTreatmentAsthma Bronchial2
4TerminatedTreatmentAsthma Bronchial / Rhinitis, Allergic, Seasonal1
4TerminatedTreatmentPerennial Allergic Rhinitis (PAR)1
4TerminatedTreatmentSeasonal Allergic Rhinitis (SAR)1
4Unknown StatusTreatmentAsthma Bronchial / Polyps, Nasal / Sinusitis1
4Unknown StatusTreatmentPhimosis1
4Unknown StatusTreatmentVitiligo1
4WithdrawnTreatmentEnuresis / Obstructive Sleep Apnea (OSA) / Sleep Disordered Breathing (SDB)1
Not AvailableCompletedNot AvailableAllergic Rhinitis (AR)1
Not AvailableCompletedNot AvailableRhinitis, Allergic, Perennial / Rhinitis, Allergic, Seasonal1
Not AvailableCompletedNot AvailableSeasonal Allergic Rhinitis (SAR)1
Not AvailableCompletedOtherAsthma Bronchial1
Not AvailableNot Yet RecruitingNot AvailableAsthma in Children1
Not AvailableRecruitingNot AvailableAsthma Bronchial1
Not AvailableSuspendedTreatmentAsthma Bronchial / Rhinitis1

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
FormRouteStrength
Spray, meteredNasal50 ug/1
CreamTopical1 mg/1g
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)
US5394868No1995-06-252012-06-25Us
CA2282360No2004-11-092018-03-16Canada
CA2091360No1997-04-082011-09-06Canada
US6127353Yes1998-04-032018-04-03Us
US6240918Yes1997-08-202017-08-20Us
US8173172Yes1998-09-172018-09-17Us
US6503537Yes1998-09-172018-09-17Us
US5829434Yes1996-05-032016-05-03Us
US6068832No1997-08-272017-08-27Us
US7067502No2000-05-212020-05-21Us
US7566705No2000-05-212020-05-21Us
US8109918No2004-03-122024-03-12Us
US7951131No2004-03-122024-03-12Us
US8025635No2007-06-122027-06-12Us
US9585681No2006-04-042026-04-04Us
US7951130No2004-03-122024-03-12Us
US7544192No2006-11-292026-11-29Us
US7951133No2004-03-122024-03-12Us
US7713255No2004-03-122024-03-12Us
US7662141No2004-03-122024-03-12Us
US8763222No2012-02-082032-02-08Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)218-220 °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)12.49ChemAxon
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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot 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

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 modula...
Gene Name
NR3C1
Uniprot ID
P04150
Uniprot Name
Glucocorticoid receptor
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]
Kind
Protein
Organism
Human
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
  1. 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

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 un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
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]
Kind
Protein
Organism
Human
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
  1. 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]
  2. 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 September 21, 2018 20:42