Fluorometholone
Identification
- Summary
Fluorometholone is an ophthalmic corticosteroid used for the relief of inflammation located in both the palpebral and bulbar conjunctiva, the cornea, and the anterior segment of the globe of the eye.
- Brand Names
- FML, FML Forte Liquifilm, FML-S, Flarex, Fluor-OP
- Generic Name
- Fluorometholone
- DrugBank Accession Number
- DB00324
- Background
A glucocorticoid employed, usually as eye drops, in the treatment of allergic and inflammatory conditions of the eye. It has also been used topically in the treatment of various skin disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p732)
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 376.4617
Monoisotopic: 376.204987621 - Chemical Formula
- C22H29FO4
- Synonyms
- (1R,2S,8S,10S,11S,14R,15S,17S)-14-acetyl-1-fluoro-14,17-dihydroxy-2,8,15-trimethyltetracyclo[8.7.0.02,7.011,15]heptadeca-3,6-dien-5-one
- 9-Fluoro-11beta,17-dihydroxy-6alpha-methylpregna-1,4-diene-3,20-dione
- Fluorometholon
- Fluorométholone
- Fluorometholone
- Fluorometholonum
- Fluorometolona
- External IDs
- NSC 33001
- U 17323
Pharmacology
- Indication
For the ophthalmic treatment of corticosteroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Anterior chamber inflammation Combination Product in combination with: Tetryzoline (DB06764) •••••••••••• ••••••••• •••••••• • ••••• Adjunct therapy in treatment of Bacterial eye infection ••• ••••• Used in combination to treat Conjunctivitis allergic Combination Product in combination with: Tetryzoline (DB06764) •••••••••••• ••••••••• •••••••• • ••••• Used in combination to treat Corneal inflammation Combination Product in combination with: Tetryzoline (DB06764) •••••••••••• ••••••••• •••••••• • ••••• Treatment of Eye inflammation •••••••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Corticosteroids such as fluorometholone inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation.
- Mechanism of action
There is no generally accepted explanation for the mechanism of action of ocular corticosteroids. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. Their primary target is the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes.
Target Actions Organism AGlucocorticoid receptor agonistHumans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Side effects may include acute anterior uveitis and perforation of the globe. Keratitis, conjunctivitis, corneal ulcers, mydriasis, conjunctival hyperemia, loss of accommodation and ptosis have occasionally been reported following local use of corticosteroids. LD50 = 234 mg/kg (rats)
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Fluorometholone can be increased when it is combined with Abametapir. Abatacept The risk or severity of adverse effects can be increased when Fluorometholone is combined with Abatacept. Acarbose The risk or severity of hyperglycemia can be increased when Fluorometholone is combined with Acarbose. Aceclofenac The risk or severity of gastrointestinal irritation can be increased when Fluorometholone is combined with Aceclofenac. Acemetacin The risk or severity of gastrointestinal irritation can be increased when Fluorometholone is combined with Acemetacin. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Fluorometholone acetate 9I50C3I3OK 3801-06-7 YRFXGQHBPBMFHW-SBTZIJSASA-N - International/Other Brands
- Efflumidex (Allergan) / Fluaton (Allergan) / Flumetholon (Ferron) / Flurolon (Allergan) / FML Liquifilm (Allergan) / Foxone (Winston) / Fucin (Mey See) / Fuluson (Dae Wo) / Fumelon (Han Lim) / Humetoron (Kuk Je) / Oxylone
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Flarex Suspension 0.1 % w/v Ophthalmic Novartis 1987-12-31 Not applicable Canada Flarex Suspension / drops 1 mg/1mL Ophthalmic ALCON LABORATORIES, INC. 1992-02-06 Not applicable US Flarex Suspension / drops 1 mg/1mL Ophthalmic Eyevance Pharmaceuticals 2019-03-05 Not applicable US Fluor-Op Suspension 0.1 mL/100mL Ophthalmic Novartis Ophthalmics 2006-05-11 Not applicable US FML Suspension / drops 1 mg/1mL Ophthalmic Allergan, Inc. 1972-02-01 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Fluorometholone Solution / drops 1 mg/1mL Ophthalmic REMEDYREPACK INC. 2019-03-01 2020-06-01 US Fluorometholone Solution / drops 1 mg/1mL Ophthalmic Pacific Pharma, Inc. 1997-10-31 Not applicable US Fluorometholone Ophthalmic Suspension Suspension / drops 1 mg/1mL Ophthalmic Amneal Pharmaceuticals NY LLC 2023-01-09 Not applicable US Fluorometholone Ophthalmic Suspension Suspension / drops 1 mg/1mL Ophthalmic Amneal Pharmaceuticals NY LLC 2023-01-09 Not applicable US PMS-fluorometholone Suspension 0.1 % Ophthalmic Pharmascience Inc 2001-07-16 2016-10-28 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image EFEMOLINE 5 ML DAMLA Fluorometholone (1 mg/ml) + Tetrahydrozoline hydrochloride (0.25 mg/ml) Solution / drops Ophthalmic THEA PHARMA İLAÇ TİC.LTD. ŞTİ. 2011-11-18 Not applicable Turkey FLU-SURE T® SUSPENSIÓN OFTÁLMICA Fluorometholone (1 mg) + Tetrahydrozoline hydrochloride (0.25 mg) Suspension Ophthalmic ARBOFARMA S.A.S. 2012-10-03 Not applicable Colombia FML-neo Oph Sus Fluorometholone (0.1 %) + Neomycin sulfate (0.5 %) Suspension Ophthalmic Allergan 1977-12-31 2011-08-04 Canada FML-S Fluorometholone (1.0 mg/1mL) + Sulfacetamide sodium (100 mg/1mL) Suspension Ophthalmic Allergan 2007-02-20 Not applicable US Tobraflex Fluorometholone acetate (1 mg/1mL) + Tobramycin (3 mg/1mL) Suspension Ophthalmic Alcon, Inc. 1989-07-21 1989-07-21 US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image FLUOROPOS GOZ DAMLASI 1MG/ML 5ML Fluorometholone (1 mg/ml) Solution / drops Ophthalmic BİEM İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 2020-12-09 Turkey
Categories
- ATC Codes
- D07XB04 — Fluorometholone
- D07XB — Corticosteroids, moderately potent, other combinations
- D07X — CORTICOSTEROIDS, OTHER COMBINATIONS
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- D07AB — Corticosteroids, moderately potent (group II)
- D07A — CORTICOSTEROIDS, PLAIN
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- S01BA — Corticosteroids, plain
- S01B — ANTIINFLAMMATORY AGENTS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- S01BB — Corticosteroids and mydriatics in combination
- S01B — ANTIINFLAMMATORY AGENTS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- C05AA — Corticosteroids
- C05A — AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE
- C05 — VASOPROTECTIVES
- C — CARDIOVASCULAR SYSTEM
- D07CB — Corticosteroids, moderately potent, combinations with antibiotics
- D07C — CORTICOSTEROIDS, COMBINATIONS WITH ANTIBIOTICS
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- S01CB — Corticosteroids/antiinfectives/mydriatics in combination
- S01C — ANTIINFLAMMATORY AGENTS AND ANTIINFECTIVES IN COMBINATION
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- S01CA — Corticosteroids and antiinfectives in combination
- S01C — ANTIINFLAMMATORY AGENTS AND ANTIINFECTIVES IN COMBINATION
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- Drug Categories
- Adrenal Cortex Hormones
- Agents for Treatment of Hemorrhoids and Anal Fissures for Topical Use
- Anti-Acne Preparations
- Anti-Acne Preparations for Topical Use
- Anti-Allergic Agents
- Anti-Inflammatory Agents
- Corticosteroid Hormone Receptor Agonists
- Corticosteroids
- Corticosteroids, Dermatological Preparations
- Corticosteroids, Moderately Potent (Group II)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Inducers
- Cytochrome P-450 CYP3A5 Inducers (strength unknown)
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Substrates
- Dermatologicals
- Fused-Ring Compounds
- Glucocorticoids
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hyperglycemia-Associated Agents
- Immunosuppressive Agents
- Ophthalmologicals
- Pregnadienediols
- Pregnadienes
- Pregnanes
- Sensory Organs
- Steroids
- Steroids, Fluorinated
- Thyroxine-binding globulin inhibitors
- Vasoprotectives
- Chemical TaxonomyProvided by Classyfire
- 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 / Secondary alcohols / Fluorohydrins show 6 more
- Substituents
- 11-beta-hydroxysteroid / 11-hydroxysteroid / 17-hydroxysteroid / 20-oxosteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / 9-halo-steroid / Alcohol / Aliphatic homopolycyclic compound / Alkyl fluoride show 21 more
- Molecular Framework
- Aliphatic homopolycyclic compounds
- External Descriptors
- 11beta-hydroxy steroid, 17alpha-hydroxy steroid, glucocorticoid, 20-oxo steroid, fluorinated steroid, 3-oxo-Delta(1),Delta(4)-steroid (CHEBI:31625)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- SV0CSG527L
- CAS number
- 426-13-1
- InChI Key
- FAOZLTXFLGPHNG-KNAQIMQKSA-N
- InChI
- InChI=1S/C22H29FO4/c1-12-9-17-15-6-8-21(27,13(2)24)20(15,4)11-18(26)22(17,23)19(3)7-5-14(25)10-16(12)19/h5,7,10,12,15,17-18,26-27H,6,8-9,11H2,1-4H3/t12-,15-,17-,18-,19-,20-,21-,22-/m0/s1
- IUPAC Name
- (1R,3aS,3bS,5S,9aS,9bR,10S,11aS)-1-acetyl-9b-fluoro-1,10-dihydroxy-5,9a,11a-trimethyl-1H,2H,3H,3aH,3bH,4H,5H,7H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-7-one
- SMILES
- [H][C@@]12CC[C@](O)(C(C)=O)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])C[C@H](C)C2=CC(=O)C=C[C@]12C
References
- Synthesis Reference
Fried, J.; U.S. Patent 2,852,51 September 16,1958; assigned to Olin Mathieson Chemical Corporation. Lincoln, F.H. Jr., Schneider, W.P. and Spero, G.B.; US. Patent 2,867,637; January 6, 1959; assigned to The Upjohn Company . Lincoln, F.H. Jr., Schneider, W.P. and Spero, G.B.; U.S. Patent 2,867,638; January 6, 1959; assigned to The Upjohn Company. Magerlein, B.J., Kagan, F. and Schlagel, C.A.; U.S. Patent 3,038,914; June 12, 1962; assigned to The Upjohn Company.
- General References
- FDA Approved Drug Products: FML (fluorometholone) ophthalmic suspension [Link]
- External Links
- Human Metabolome Database
- HMDB0014469
- KEGG Drug
- D01367
- PubChem Compound
- 9878
- PubChem Substance
- 46505984
- ChemSpider
- 9494
- BindingDB
- 50103631
- 4491
- ChEBI
- 31625
- ChEMBL
- CHEMBL1200600
- ZINC
- ZINC000118912517
- Therapeutic Targets Database
- DAP001047
- PharmGKB
- PA164781355
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Fluorometholone
- FDA label
- Download (64.7 KB)
- MSDS
- Download (72 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Adenoviral Keratoconjunctivitis 1 4 Completed Treatment Intraocular Pressure (IOP) 1 4 Not Yet Recruiting Treatment Fuchs' Endothelial Dystrophy / Intraocular Pressure (IOP) / Pseudophakic Bullous Keratopathy 1 4 Not Yet Recruiting Treatment Steroid Ophthalmic Insert 1 4 Unknown Status Health Services Research Dry Eye Syndrome (DES) / Inflammation / Microvessels 1
Pharmacoeconomics
- Manufacturers
- Pharmacia and upjohn co
- Allergan pharmaceutical
- Novartis pharmaceuticals corp
- Alcon laboratories inc
- Packagers
- Alcon Laboratories
- Allergan Inc.
- A-S Medication Solutions LLC
- Bausch & Lomb Inc.
- Dispensing Solutions
- Novartis AG
- OMJ Pharmaceuticals
- Pacific Pharma Lp
- Pharma Pac LLC
- Pharmedix
- Physicians Total Care Inc.
- Dosage Forms
Form Route Strength Suspension Conjunctival; Ophthalmic 1 mg Solution / drops Ophthalmic Solution / drops Ophthalmic 0.1 % Suspension Ophthalmic 0.1 % w/v Suspension Ophthalmic 1 mg Ointment Ophthalmic Ointment Ophthalmic 0.1 % Solution / drops Ophthalmic 0.2 % Suspension Conjunctival; Ophthalmic 100000 mg Suspension Ophthalmic 1.000 mg Suspension Ophthalmic; Topical 1 mg Suspension Ophthalmic; Topical 100000 mg Suspension Ophthalmic 0.1 mL/100mL Solution / drops Ophthalmic 1 mg/1mL Solution / drops Ophthalmic 1 mg/ml Ointment Ophthalmic 1 mg/1g Suspension Ophthalmic 0.1 % Suspension / drops Ophthalmic 1 mg/1mL Suspension / drops Ophthalmic 2.5 mg/1mL Suspension Ophthalmic 0.25 % Solution Ophthalmic 1 mg/ml Suspension / drops Conjunctival 0.1 % w/v Suspension Ophthalmic Suspension / drops Ophthalmic 0.1 % Suspension Conjunctival; Ophthalmic Suspension Conjunctival; Intraocular; Ophthalmic Solution / drops Ophthalmic Suspension / drops Conjunctival Liquid Ophthalmic 1 mg/1ml - Prices
Unit description Cost Unit FML Liquifilm 0.1% Suspension 15ml Bottle 82.16USD bottle FML Forte 0.25% Suspension 15ml Bottle 60.98USD bottle FML Liquifilm 0.1% Suspension 10ml Bottle 60.17USD bottle Flarex 0.1% Suspension 10ml Bottle 50.7USD bottle FML Forte 0.25% Suspension 10ml Bottle 48.58USD bottle Flarex 0.1% Suspension 5ml Bottle 42.82USD bottle FML Liquifilm 0.1% Suspension 5ml Bottle 41.65USD bottle FML-S Liquifilm 0.1-10% Suspension 10ml Bottle 35.99USD bottle Fluor-Op 0.1% Suspension 15ml Bottle 30.99USD bottle FML Forte 0.25% Suspension 5ml Bottle 30.07USD bottle Fluor-Op 0.1% Suspension 10ml Bottle 25.99USD bottle Fluor-Op 0.1% Suspension 5ml Bottle 17.99USD bottle Flarex 0.1% eye drops 8.11USD ml Fml liquifilm 0.1% eye drop 6.27USD ml Fml forte 0.25% eye drops 5.09USD ml Fluorometholone 0.1% drops 3.25USD ml Fml Forte 0.25 % Suspension 2.96USD ml Flarex 0.1 % Suspension 1.96USD ml Pms-Fluorometholone 0.1 % Suspension 1.73USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 292-303 Fried, J.; U.S. Patent 2,852,51 September 16,1958; assigned to Olin Mathieson Chemical Corporation. Lincoln, F.H. Jr., Schneider, W.P. and Spero, G.B.; US. Patent 2,867,637; January 6, 1959; assigned to The Upjohn Company . Lincoln, F.H. Jr., Schneider, W.P. and Spero, G.B.; U.S. Patent 2,867,638; January 6, 1959; assigned to The Upjohn Company. Magerlein, B.J., Kagan, F. and Schlagel, C.A.; U.S. Patent 3,038,914; June 12, 1962; assigned to The Upjohn Company. water solubility 30 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992) logP 2.00 HANSCH,C ET AL. (1995) logS -4.1 ADME Research, USCD - Predicted Properties
Property Value Source Water Solubility 0.0166 mg/mL ALOGPS logP 2.34 ALOGPS logP 2.42 Chemaxon logS -4.4 ALOGPS pKa (Strongest Acidic) 12.65 Chemaxon pKa (Strongest Basic) -3.4 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 1 Chemaxon Refractivity 100.87 m3·mol-1 Chemaxon Polarizability 39.94 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 + 0.9956 Blood Brain Barrier + 0.9716 Caco-2 permeable + 0.8169 P-glycoprotein substrate Substrate 0.7834 P-glycoprotein inhibitor I Non-inhibitor 0.6791 P-glycoprotein inhibitor II Non-inhibitor 0.8382 Renal organic cation transporter Non-inhibitor 0.8397 CYP450 2C9 substrate Non-substrate 0.8762 CYP450 2D6 substrate Non-substrate 0.907 CYP450 3A4 substrate Substrate 0.7663 CYP450 1A2 substrate Non-inhibitor 0.9149 CYP450 2C9 inhibitor Non-inhibitor 0.8345 CYP450 2D6 inhibitor Non-inhibitor 0.9232 CYP450 2C19 inhibitor Non-inhibitor 0.9285 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9452 Ames test Non AMES toxic 0.9025 Carcinogenicity Non-carcinogens 0.9404 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.3393 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9694 hERG inhibition (predictor II) Non-inhibitor 0.5956
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 193.454293 predictedDarkChem Lite v0.1.0 [M-H]- 178.7936128 predictedDarkChem Lite v0.1.0 [M-H]- 190.0317 predictedDeepCCS 1.0 (2019) [M+H]+ 195.074593 predictedDarkChem Lite v0.1.0 [M+H]+ 186.1119747 predictedDarkChem Lite v0.1.0 [M+H]+ 191.92708 predictedDeepCCS 1.0 (2019) [M+Na]+ 194.054393 predictedDarkChem Lite v0.1.0 [M+Na]+ 185.2282366 predictedDarkChem Lite v0.1.0 [M+Na]+ 197.5807 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- 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
- Samudre SS, Lattanzio FA Jr, Williams PB, Sheppard JD Jr: Comparison of topical steroids for acute anterior uveitis. J Ocul Pharmacol Ther. 2004 Dec;20(6):533-47. [Article]
- Grossman R, Yehuda R, Golier J, McEwen B, Harvey P, Maria NS: Cognitive effects of intravenous hydrocortisone in subjects with PTSD and healthy control subjects. Ann N Y Acad Sci. 2006 Jul;1071:410-21. [Article]
- Rautanen A, Eriksson JG, Kere J, Andersson S, Osmond C, Tienari P, Sairanen H, Barker DJ, Phillips DI, Forsen T, Kajantie E: Associations of body size at birth with late-life cortisol concentrations and glucose tolerance are modified by haplotypes of the glucocorticoid receptor gene. J Clin Endocrinol Metab. 2006 Nov;91(11):4544-51. Epub 2006 Aug 8. [Article]
- Hammer F, Stewart PM: Cortisol metabolism in hypertension. Best Pract Res Clin Endocrinol Metab. 2006 Sep;20(3):337-53. [Article]
- Shaw JR, Gabor K, Hand E, Lankowski A, Durant L, Thibodeau R, Stanton CR, Barnaby R, Coutermarsh B, Karlson KH, Sato JD, Hamilton JW, Stanton BA: Role of glucocorticoid receptor in acclimation of killifish (Fundulus heteroclitus) to seawater and effects of arsenic. Am J Physiol Regul Integr Comp Physiol. 2007 Feb;292(2):R1052-60. Epub 2006 Oct 12. [Article]
- Sher L: Combined dexamethasone suppression-corticotropin-releasing hormone stimulation test in studies of depression, alcoholism, and suicidal behavior. ScientificWorldJournal. 2006 Oct 31;6:1398-404. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Oxygen binding
- 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
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Dvorak Z, Pavek P: Regulation of drug-metabolizing cytochrome P450 enzymes by glucocorticoids. Drug Metab Rev. 2010 Nov;42(4):621-35. doi: 10.3109/03602532.2010.484462. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- 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
- El-Sankary W, Bombail V, Gibson GG, Plant N: Glucocorticoid-mediated induction of CYP3A4 is decreased by disruption of a protein: DNA interaction distinct from the pregnane X receptor response element. Drug Metab Dispos. 2002 Sep;30(9):1029-34. [Article]
- Dvorak Z, Pavek P: Regulation of drug-metabolizing cytochrome P450 enzymes by glucocorticoids. Drug Metab Rev. 2010 Nov;42(4):621-35. doi: 10.3109/03602532.2010.484462. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Steroid binding
- Specific Function
- Major transport protein for glucocorticoids and progestins in the blood of almost all vertebrate species.
- Gene Name
- SERPINA6
- Uniprot ID
- P08185
- Uniprot Name
- Corticosteroid-binding globulin
- Molecular Weight
- 45140.49 Da
References
- Moisan MP, Castanon N: Emerging Role of Corticosteroid-Binding Globulin in Glucocorticoid-Driven Metabolic Disorders. Front Endocrinol (Lausanne). 2016 Dec 19;7:160. doi: 10.3389/fendo.2016.00160. eCollection 2016. [Article]
- Gardill BR, Vogl MR, Lin HY, Hammond GL, Muller YA: Corticosteroid-binding globulin: structure-function implications from species differences. PLoS One. 2012;7(12):e52759. doi: 10.1371/journal.pone.0052759. Epub 2012 Dec 26. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55