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Identification
NameRimexolone
Accession NumberDB00896  (APRD01220)
TypeSmall Molecule
GroupsApproved
DescriptionRimexolone is a glucocorticoid steroid used to treat inflammation in the eye. It is marketed as a 1% eye drop solution under the trade name Vexol
Structure
Thumb
Synonyms
Rimexolon
External Identifiers
  • Org 6216
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
VexolSuspension / drops10 mg/mLOphthalmicAlcon Laboratories, Inc1995-09-15Not applicableUs
Vexol Ophthalmic Suspension - 1%Suspension1 %OphthalmicAlcon Canada Inc1997-01-222016-06-16Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIO7M2E4264D
CAS number49697-38-3
WeightAverage: 370.533
Monoisotopic: 370.250794955
Chemical FormulaC24H34O3
InChI KeyQTTRZHGPGKRAFB-OOKHYKNYSA-N
InChI
InChI=1S/C24H34O3/c1-6-20(27)24(5)14(2)11-18-17-8-7-15-12-16(25)9-10-22(15,3)21(17)19(26)13-23(18,24)4/h9-10,12,14,17-19,21,26H,6-8,11,13H2,1-5H3/t14-,17+,18+,19+,21-,22+,23+,24-/m1/s1
IUPAC Name
(1S,2R,10S,11S,13R,14S,15S,17S)-17-hydroxy-2,13,14,15-tetramethyl-14-propanoyltetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadeca-3,6-dien-5-one
SMILES
[H][C@@]12C[C@@H](C)[C@](C)(C(=O)CC)[C@@]1(C)C[[email protected]](O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
Pharmacology
IndicationFor the treatment of postoperative inflammation following ocular surgery and in the treatment of anterior uveitis.
Structured Indications
PharmacodynamicsRimexolone is a glucocorticoid corticosteroid for systemic use. Corticosteroids suppress the inflammatory response to a variety of inciting agents of a mechanical, chemical, or immunological nature. They inhibit edema, cellular infiltration, capillary dilatation, fibroblastic proliferation, deposition of collagen and scar formation associated with inflammation.
Mechanism of actionRimexolone is a glucocorticoid receptor agonist. The antiinflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition of arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. By binding to the glucocorticoid receptor, this drug ultimately leads to changes in genetic transcription involving the lipocortins and prostaglandins.
TargetKindPharmacological actionActionsOrganismUniProt ID
Glucocorticoid receptorProteinyes
agonist
HumanP04150 details
Related Articles
AbsorptionSystemically absorbed.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Undergoes extensive metabolism. Following intravenous administration of radiolabeled rimexolone in rats, more than 80% of the dose was excreted in the feces as rimexolone and metabolites. Metabolites have been shown to be either less active than rimexolone or inactive in human glucocorticoid receptor binding assays.

Route of eliminationFollowing IV administration of radio-labelled rimexolone to rats, greater than 80% of the dose is excreted via the feces as rimexolone and metabolites.
Half lifeThe serum half-life of rimexolone could not be reliably estimated due to the large number of samples below the quantitation limit of the assay (80 pg/mL). However, based on the time required to reach steady-state, the half-life appears to be short (1-2 hours).
ClearanceNot Available
ToxicitySymptoms of overdose include retinal toxicity, glaucoma, and subcapsular cataract.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe risk or severity of adverse effects can be increased when Rimexolone is combined with 1,10-Phenanthroline.Experimental
AceclofenacThe risk or severity of adverse effects can be increased when Aceclofenac is combined with Rimexolone.Approved
AcetovanilloneThe risk or severity of adverse effects can be increased when Acetovanillone is combined with Rimexolone.Investigational
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Rimexolone.Approved, Vet Approved
AdapaleneThe risk or severity of adverse effects can be increased when Adapalene is combined with Rimexolone.Approved
AldesleukinRimexolone may decrease the antineoplastic activities of Aldesleukin.Approved
ALT-110The risk or severity of adverse effects can be increased when Rimexolone is combined with ALT-110.Investigational
Aluminum hydroxideThe bioavailability of Rimexolone can be decreased when combined with Aluminum hydroxide.Approved
Aluminum phosphateThe bioavailability of Rimexolone can be decreased when combined with Aluminum phosphate.Approved
AmbenoniumThe risk or severity of adverse effects can be increased when Rimexolone is combined with Ambenonium.Approved
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Rimexolone.Approved
AmiodaroneThe serum concentration of Rimexolone can be increased when it is combined with Amiodarone.Approved, Investigational
Amphotericin BRimexolone may increase the hypokalemic activities of Amphotericin B.Approved, Investigational
AnisodamineThe risk or severity of adverse effects can be increased when Anisodamine is combined with Rimexolone.Investigational
AntipyrineThe risk or severity of adverse effects can be increased when Antipyrine is combined with Rimexolone.Approved
ApremilastThe risk or severity of adverse effects can be increased when Apremilast is combined with Rimexolone.Approved, Investigational
AprepitantThe serum concentration of Rimexolone can be increased when it is combined with Aprepitant.Approved, Investigational
AtazanavirThe serum concentration of Rimexolone can be increased when it is combined with Atazanavir.Approved, Investigational
Atracurium besylateAtracurium besylate may increase the adverse neuromuscular activities of Rimexolone.Approved
AzapropazoneThe risk or severity of adverse effects can be increased when Azapropazone is combined with Rimexolone.Withdrawn
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Rimexolone.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Rimexolone.Approved, Investigational
BazedoxifeneThe serum concentration of Rimexolone can be increased when it is combined with Bazedoxifene.Approved, Investigational
BendroflumethiazideRimexolone may increase the hypokalemic activities of Bendroflumethiazide.Approved
BenoxaprofenThe risk or severity of adverse effects can be increased when Benoxaprofen is combined with Rimexolone.Withdrawn
Benzoic AcidThe therapeutic efficacy of Benzoic Acid can be decreased when used in combination with Rimexolone.Approved
Betulinic AcidThe risk or severity of adverse effects can be increased when Betulinic Acid is combined with Rimexolone.Investigational
Bismuth SubcitrateThe bioavailability of Rimexolone can be decreased when combined with Bismuth Subcitrate.Approved
BoceprevirThe serum concentration of Rimexolone can be increased when it is combined with Boceprevir.Approved
BromfenacThe risk or severity of adverse effects can be increased when Bromfenac is combined with Rimexolone.Approved
BucillamineThe risk or severity of adverse effects can be increased when Bucillamine is combined with Rimexolone.Investigational
BumetanideRimexolone may increase the hypokalemic activities of Bumetanide.Approved
CalcitriolThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Rimexolone.Approved, Nutraceutical
Calcium carbonateThe bioavailability of Rimexolone can be decreased when combined with Calcium carbonate.Approved
CarbamazepineThe serum concentration of Rimexolone can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarprofenThe risk or severity of adverse effects can be increased when Carprofen is combined with Rimexolone.Approved, Vet Approved, Withdrawn
CastanospermineThe risk or severity of adverse effects can be increased when Castanospermine is combined with Rimexolone.Experimental
CDX-110The risk or severity of adverse effects can be increased when Rimexolone is combined with CDX-110.Investigational
CelecoxibThe risk or severity of adverse effects can be increased when Celecoxib is combined with Rimexolone.Approved, Investigational
CeritinibRimexolone may increase the hyperglycemic activities of Ceritinib.Approved
ChloroquineThe risk or severity of adverse effects can be increased when Chloroquine is combined with Rimexolone.Approved, Vet Approved
ChlorothiazideRimexolone may increase the hypokalemic activities of Chlorothiazide.Approved, Vet Approved
ChlorotrianiseneThe serum concentration of Rimexolone can be increased when it is combined with Chlorotrianisene.Withdrawn
ChlorthalidoneRimexolone may increase the hypokalemic activities of Chlorthalidone.Approved
CholestyramineCholestyramine can cause a decrease in the absorption of Rimexolone resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
CinoxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Cinoxacin.Approved, Withdrawn
CiprofloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Ciprofloxacin.Approved, Investigational
ClarithromycinThe serum concentration of Rimexolone can be increased when it is combined with Clarithromycin.Approved
ClonixinThe risk or severity of adverse effects can be increased when Clonixin is combined with Rimexolone.Approved
CobicistatThe serum concentration of Rimexolone can be increased when it is combined with Cobicistat.Approved
ColesevelamColesevelam can cause a decrease in the absorption of Rimexolone resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
ColestipolColestipol can cause a decrease in the absorption of Rimexolone resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Conjugated Equine EstrogensThe serum concentration of Rimexolone can be increased when it is combined with Conjugated Equine Estrogens.Approved
Corticorelin ovine triflutateThe therapeutic efficacy of Corticorelin ovine triflutate can be decreased when used in combination with Rimexolone.Approved
CoumaphosThe risk or severity of adverse effects can be increased when Rimexolone is combined with Coumaphos.Vet Approved
CurcuminThe risk or severity of adverse effects can be increased when Curcumin is combined with Rimexolone.Investigational
D-LimoneneThe risk or severity of adverse effects can be increased when D-Limonene is combined with Rimexolone.Investigational
DarunavirThe serum concentration of Rimexolone can be increased when it is combined with Darunavir.Approved
DecamethoniumThe risk or severity of adverse effects can be increased when Rimexolone is combined with Decamethonium.Approved
DeferasiroxThe risk or severity of adverse effects can be increased when Rimexolone is combined with Deferasirox.Approved, Investigational
DemecariumThe risk or severity of adverse effects can be increased when Rimexolone is combined with Demecarium.Approved
dersalazineThe risk or severity of adverse effects can be increased when dersalazine is combined with Rimexolone.Investigational
DichlorvosThe risk or severity of adverse effects can be increased when Rimexolone is combined with Dichlorvos.Vet Approved
DiclofenacThe risk or severity of adverse effects can be increased when Diclofenac is combined with Rimexolone.Approved, Vet Approved
DienestrolThe serum concentration of Rimexolone can be increased when it is combined with Dienestrol.Approved
DiethylstilbestrolThe serum concentration of Rimexolone can be increased when it is combined with Diethylstilbestrol.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Rimexolone.Approved
DihydrotestosteroneRimexolone may increase the fluid retaining activities of Dihydrotestosterone.Illicit
DonepezilThe risk or severity of adverse effects can be increased when Rimexolone is combined with Donepezil.Approved
DroxicamThe risk or severity of adverse effects can be increased when Droxicam is combined with Rimexolone.Approved
DuvelisibThe risk or severity of adverse effects can be increased when Duvelisib is combined with Rimexolone.Investigational
E6201The risk or severity of adverse effects can be increased when E6201 is combined with Rimexolone.Investigational
EbselenThe risk or severity of adverse effects can be increased when Ebselen is combined with Rimexolone.Investigational
EchothiophateThe risk or severity of adverse effects can be increased when Rimexolone is combined with Echothiophate.Approved
EdrophoniumThe risk or severity of adverse effects can be increased when Rimexolone is combined with Edrophonium.Approved
EnoxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Enoxacin.Approved
EnzalutamideThe serum concentration of Rimexolone can be decreased when it is combined with Enzalutamide.Approved
EpirizoleThe risk or severity of adverse effects can be increased when Epirizole is combined with Rimexolone.Approved
EstradiolThe serum concentration of Rimexolone can be increased when it is combined with Estradiol.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Rimexolone can be increased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Rimexolone can be increased when it is combined with Estrone.Approved
Etacrynic acidRimexolone may increase the hypokalemic activities of Etacrynic acid.Approved
EtanerceptThe risk or severity of adverse effects can be increased when Etanercept is combined with Rimexolone.Approved, Investigational
Ethinyl EstradiolThe serum concentration of Rimexolone can be increased when it is combined with Ethinyl Estradiol.Approved
EtodolacThe risk or severity of adverse effects can be increased when Etodolac is combined with Rimexolone.Approved, Investigational, Vet Approved
EtofenamateThe risk or severity of adverse effects can be increased when Etofenamate is combined with Rimexolone.Approved
EtoricoxibThe risk or severity of adverse effects can be increased when Etoricoxib is combined with Rimexolone.Approved, Investigational
Evening primrose oilThe risk or severity of adverse effects can be increased when Evening primrose oil is combined with Rimexolone.Approved
exisulindThe risk or severity of adverse effects can be increased when exisulind is combined with Rimexolone.Investigational
FenbufenThe risk or severity of adverse effects can be increased when Fenbufen is combined with Rimexolone.Approved
FenoprofenThe risk or severity of adverse effects can be increased when Fenoprofen is combined with Rimexolone.Approved
FenthionThe risk or severity of adverse effects can be increased when Rimexolone is combined with Fenthion.Vet Approved
FleroxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Fleroxacin.Approved
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Rimexolone.Approved, Withdrawn
FlumequineThe risk or severity of adverse effects can be increased when Rimexolone is combined with Flumequine.Withdrawn
FlunixinThe risk or severity of adverse effects can be increased when Flunixin is combined with Rimexolone.Vet Approved
FluoxymesteroneRimexolone may increase the fluid retaining activities of Fluoxymesterone.Approved, Illicit
FlurbiprofenThe risk or severity of adverse effects can be increased when Flurbiprofen is combined with Rimexolone.Approved, Investigational
FosaprepitantThe serum concentration of Rimexolone can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Rimexolone can be decreased when it is combined with Fosphenytoin.Approved
FurosemideRimexolone may increase the hypokalemic activities of Furosemide.Approved, Vet Approved
G17DTThe risk or severity of adverse effects can be increased when Rimexolone is combined with G17DT.Investigational
GalantamineThe risk or severity of adverse effects can be increased when Rimexolone is combined with Galantamine.Approved
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Rimexolone is combined with Gallamine Triethiodide.Approved
GarenoxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Garenoxacin.Investigational
GatifloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Gatifloxacin.Approved, Investigational
GemifloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Gemifloxacin.Approved, Investigational
GenisteinThe serum concentration of Rimexolone can be increased when it is combined with Genistein.Investigational
GI-5005The risk or severity of adverse effects can be increased when Rimexolone is combined with GI-5005.Investigational
Ginkgo bilobaThe risk or severity of adverse effects can be increased when Rimexolone is combined with Ginkgo biloba.Approved, Nutraceutical
Glycerol PhenylbutyrateThe therapeutic efficacy of Glycerol Phenylbutyrate can be decreased when used in combination with Rimexolone.Approved
GrepafloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Grepafloxacin.Withdrawn
HexestrolThe serum concentration of Rimexolone can be increased when it is combined with Hexestrol.Withdrawn
HigenamineThe risk or severity of adverse effects can be increased when Higenamine is combined with Rimexolone.Investigational
HMPL-004The risk or severity of adverse effects can be increased when HMPL-004 is combined with Rimexolone.Investigational
Huperzine AThe risk or severity of adverse effects can be increased when Rimexolone is combined with Huperzine A.Investigational
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Rimexolone.Approved, Investigational
HydrochlorothiazideRimexolone may increase the hypokalemic activities of Hydrochlorothiazide.Approved, Vet Approved
HydroflumethiazideRimexolone may increase the hypokalemic activities of Hydroflumethiazide.Approved
IbuprofenThe risk or severity of adverse effects can be increased when Ibuprofen is combined with Rimexolone.Approved
IbuproxamThe risk or severity of adverse effects can be increased when Ibuproxam is combined with Rimexolone.Withdrawn
IcatibantThe risk or severity of adverse effects can be increased when Icatibant is combined with Rimexolone.Approved
IdelalisibThe serum concentration of Rimexolone can be increased when it is combined with Idelalisib.Approved
IndacaterolIndacaterol may increase the hypokalemic activities of Rimexolone.Approved
IndapamideRimexolone may increase the hypokalemic activities of Indapamide.Approved
IndinavirThe serum concentration of Rimexolone can be increased when it is combined with Indinavir.Approved
IndomethacinThe risk or severity of adverse effects can be increased when Indomethacin is combined with Rimexolone.Approved, Investigational
IndoprofenThe risk or severity of adverse effects can be increased when Indoprofen is combined with Rimexolone.Withdrawn
INGN 201The risk or severity of adverse effects can be increased when Rimexolone is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Rimexolone is combined with INGN 225.Investigational
IsoflurophateThe risk or severity of adverse effects can be increased when Rimexolone is combined with Isoflurophate.Approved, Withdrawn
IsoniazidThe serum concentration of Isoniazid can be decreased when it is combined with Rimexolone.Approved
IsoxicamThe risk or severity of adverse effects can be increased when Isoxicam is combined with Rimexolone.Withdrawn
ItraconazoleThe serum concentration of Rimexolone can be increased when it is combined with Itraconazole.Approved, Investigational
KebuzoneThe risk or severity of adverse effects can be increased when Kebuzone is combined with Rimexolone.Experimental
KetoconazoleThe serum concentration of Rimexolone can be increased when it is combined with Ketoconazole.Approved, Investigational
KetoprofenThe risk or severity of adverse effects can be increased when Ketoprofen is combined with Rimexolone.Approved, Vet Approved
KetorolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Rimexolone.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Leflunomide is combined with Rimexolone.Approved, Investigational
LevofloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Levofloxacin.Approved, Investigational
LisofyllineThe risk or severity of adverse effects can be increased when Lisofylline is combined with Rimexolone.Investigational
LomefloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Lomefloxacin.Approved
LopinavirThe serum concentration of Rimexolone can be increased when it is combined with Lopinavir.Approved
LornoxicamThe risk or severity of adverse effects can be increased when Lornoxicam is combined with Rimexolone.Approved
LoxoprofenThe risk or severity of adverse effects can be increased when Loxoprofen is combined with Rimexolone.Approved
LumacaftorThe serum concentration of Rimexolone can be decreased when it is combined with Lumacaftor.Approved
LumiracoxibThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Rimexolone.Approved, Investigational
MagaldrateThe bioavailability of Rimexolone can be decreased when combined with Magaldrate.Withdrawn
Magnesium carbonateThe bioavailability of Rimexolone can be decreased when combined with Magnesium carbonate.Approved
Magnesium hydroxideThe bioavailability of Rimexolone can be decreased when combined with Magnesium hydroxide.Approved
Magnesium oxideThe bioavailability of Rimexolone can be decreased when combined with Magnesium oxide.Approved
Magnesium salicylateThe risk or severity of adverse effects can be increased when Magnesium salicylate is combined with Rimexolone.Approved
Magnesium TrisilicateThe bioavailability of Rimexolone can be decreased when combined with Magnesium Trisilicate.Approved
MalathionThe risk or severity of adverse effects can be increased when Rimexolone is combined with Malathion.Approved, Investigational
MasoprocolThe risk or severity of adverse effects can be increased when Masoprocol is combined with Rimexolone.Approved
Meclofenamic acidThe risk or severity of adverse effects can be increased when Meclofenamic acid is combined with Rimexolone.Approved, Vet Approved
Mefenamic acidThe risk or severity of adverse effects can be increased when Mefenamic acid is combined with Rimexolone.Approved
MefloquineThe risk or severity of adverse effects can be increased when Rimexolone is combined with Mefloquine.Approved
MeloxicamThe risk or severity of adverse effects can be increased when Meloxicam is combined with Rimexolone.Approved, Vet Approved
MemantineThe risk or severity of adverse effects can be increased when Rimexolone is combined with Memantine.Approved, Investigational
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Rimexolone.Approved
MestranolThe serum concentration of Rimexolone can be increased when it is combined with Mestranol.Approved
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Rimexolone.Withdrawn
MethallenestrilThe serum concentration of Rimexolone can be increased when it is combined with Methallenestril.Experimental
Methanesulfonyl FluorideThe risk or severity of adverse effects can be increased when Rimexolone is combined with Methanesulfonyl Fluoride.Investigational
MethyclothiazideRimexolone may increase the hypokalemic activities of Methyclothiazide.Approved
MethyltestosteroneRimexolone may increase the fluid retaining activities of Methyltestosterone.Approved
MetolazoneRimexolone may increase the hypokalemic activities of Metolazone.Approved
MifepristoneThe therapeutic efficacy of Rimexolone can be decreased when used in combination with Mifepristone.Approved, Investigational
MinaprineThe risk or severity of adverse effects can be increased when Rimexolone is combined with Minaprine.Approved
MitotaneThe serum concentration of Rimexolone can be decreased when it is combined with Mitotane.Approved
MivacuriumMivacurium may increase the adverse neuromuscular activities of Rimexolone.Approved
MizoribineThe risk or severity of adverse effects can be increased when Mizoribine is combined with Rimexolone.Investigational
MoxifloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Moxifloxacin.Approved, Investigational
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Rimexolone.Approved, Investigational
Mycophenolic acidThe risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Rimexolone.Approved
NabumetoneThe risk or severity of adverse effects can be increased when Nabumetone is combined with Rimexolone.Approved
NafamostatThe risk or severity of adverse effects can be increased when Nafamostat is combined with Rimexolone.Investigational
NaftifineThe risk or severity of adverse effects can be increased when Naftifine is combined with Rimexolone.Approved
Nalidixic AcidThe risk or severity of adverse effects can be increased when Rimexolone is combined with Nalidixic Acid.Approved
NaproxenThe risk or severity of adverse effects can be increased when Naproxen is combined with Rimexolone.Approved, Vet Approved
NCX 4016The risk or severity of adverse effects can be increased when NCX 4016 is combined with Rimexolone.Investigational
NefazodoneThe serum concentration of Rimexolone can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Rimexolone can be increased when it is combined with Nelfinavir.Approved
NemonoxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Nemonoxacin.Investigational
NeostigmineThe risk or severity of adverse effects can be increased when Rimexolone is combined with Neostigmine.Approved, Vet Approved
NepafenacThe risk or severity of adverse effects can be increased when Nepafenac is combined with Rimexolone.Approved
NevirapineThe serum concentration of Rimexolone can be decreased when it is combined with Nevirapine.Approved
NicorandilThe risk or severity of adverse effects can be increased when Rimexolone is combined with Nicorandil.Approved
Niflumic AcidThe risk or severity of adverse effects can be increased when Niflumic Acid is combined with Rimexolone.Approved
NimesulideThe risk or severity of adverse effects can be increased when Nimesulide is combined with Rimexolone.Approved, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Nitroaspirin is combined with Rimexolone.Investigational
NorfloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Norfloxacin.Approved
OfloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Ofloxacin.Approved
OlopatadineThe risk or severity of adverse effects can be increased when Olopatadine is combined with Rimexolone.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Rimexolone.Approved
OrgoteinThe risk or severity of adverse effects can be increased when Orgotein is combined with Rimexolone.Vet Approved
OxandroloneRimexolone may increase the fluid retaining activities of Oxandrolone.Approved, Investigational
OxaprozinThe risk or severity of adverse effects can be increased when Oxaprozin is combined with Rimexolone.Approved
OxymetholoneRimexolone may increase the fluid retaining activities of Oxymetholone.Approved, Illicit
OxyphenbutazoneThe risk or severity of adverse effects can be increased when Oxyphenbutazone is combined with Rimexolone.Withdrawn
ParecoxibThe risk or severity of adverse effects can be increased when Parecoxib is combined with Rimexolone.Approved
PazufloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Pazufloxacin.Investigational
PefloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Pefloxacin.Approved
PentobarbitalThe serum concentration of Rimexolone can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PhenobarbitalThe serum concentration of Rimexolone can be decreased when it is combined with Phenobarbital.Approved
Phenylacetic acidThe therapeutic efficacy of Phenylacetic acid can be decreased when used in combination with Rimexolone.Approved
PhenylbutazoneThe risk or severity of adverse effects can be increased when Phenylbutazone is combined with Rimexolone.Approved, Vet Approved
PhenytoinThe serum concentration of Rimexolone can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PhysostigmineThe risk or severity of adverse effects can be increased when Rimexolone is combined with Physostigmine.Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Rimexolone.Approved, Investigational
PiretanideRimexolone may increase the hypokalemic activities of Piretanide.Experimental
PirfenidoneThe risk or severity of adverse effects can be increased when Pirfenidone is combined with Rimexolone.Investigational
PiroxicamThe risk or severity of adverse effects can be increased when Piroxicam is combined with Rimexolone.Approved, Investigational
Polyestradiol phosphateThe serum concentration of Rimexolone can be increased when it is combined with Polyestradiol phosphate.Approved
PolythiazideRimexolone may increase the hypokalemic activities of Polythiazide.Approved
PosaconazoleThe serum concentration of Rimexolone can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe serum concentration of Rimexolone can be decreased when it is combined with Primidone.Approved, Vet Approved
PromestrieneThe serum concentration of Rimexolone can be increased when it is combined with Promestriene.Investigational
PropacetamolThe risk or severity of adverse effects can be increased when Propacetamol is combined with Rimexolone.Approved
PrulifloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Prulifloxacin.Investigational
PTC299The risk or severity of adverse effects can be increased when PTC299 is combined with Rimexolone.Investigational
PyridostigmineThe risk or severity of adverse effects can be increased when Rimexolone is combined with Pyridostigmine.Approved
QuinestrolThe serum concentration of Rimexolone can be increased when it is combined with Quinestrol.Approved
QuinethazoneRimexolone may increase the hypokalemic activities of Quinethazone.Approved
Rabies vaccineThe risk or severity of adverse effects can be increased when Rimexolone is combined with Rabies vaccine.Approved
RapacuroniumRapacuronium may increase the adverse neuromuscular activities of Rimexolone.Withdrawn
ResveratrolThe risk or severity of adverse effects can be increased when Resveratrol is combined with Rimexolone.Experimental, Investigational
RifabutinThe serum concentration of Rimexolone can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Rimexolone can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Rimexolone can be decreased when it is combined with Rifapentine.Approved
RitonavirThe serum concentration of Rimexolone can be increased when it is combined with Ritonavir.Approved, Investigational
RivastigmineThe risk or severity of adverse effects can be increased when Rimexolone is combined with Rivastigmine.Approved, Investigational
RofecoxibThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Rimexolone.Investigational, Withdrawn
RosoxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Rosoxacin.Approved
S EquolThe serum concentration of Rimexolone can be increased when it is combined with S Equol.Investigational
SalicylamideThe risk or severity of adverse effects can be increased when Salicylamide is combined with Rimexolone.Approved
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Rimexolone.Approved, Vet Approved
SalsalateThe risk or severity of adverse effects can be increased when Salsalate is combined with Rimexolone.Approved
SaquinavirThe serum concentration of Rimexolone can be increased when it is combined with Saquinavir.Approved, Investigational
SecoisolariciresinolThe serum concentration of Rimexolone can be increased when it is combined with Secoisolariciresinol.Investigational
SeratrodastThe risk or severity of adverse effects can be increased when Seratrodast is combined with Rimexolone.Approved, Investigational
Sodium phenylbutyrateThe therapeutic efficacy of Sodium phenylbutyrate can be decreased when used in combination with Rimexolone.Approved
SparfloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Sparfloxacin.Approved
SRP 299The risk or severity of adverse effects can be increased when Rimexolone is combined with SRP 299.Investigational
SRT501The risk or severity of adverse effects can be increased when SRT501 is combined with Rimexolone.Investigational
St. John's WortThe serum concentration of Rimexolone can be decreased when it is combined with St. John's Wort.Nutraceutical
StanozololRimexolone may increase the fluid retaining activities of Stanozolol.Approved, Vet Approved
SulfasalazineThe risk or severity of adverse effects can be increased when Sulfasalazine is combined with Rimexolone.Approved
SulindacThe risk or severity of adverse effects can be increased when Sulindac is combined with Rimexolone.Approved
SuprofenThe risk or severity of adverse effects can be increased when Suprofen is combined with Rimexolone.Approved, Withdrawn
Synthetic Conjugated Estrogens, AThe serum concentration of Rimexolone can be increased when it is combined with Synthetic Conjugated Estrogens, A.Approved
Synthetic Conjugated Estrogens, BThe serum concentration of Rimexolone can be increased when it is combined with Synthetic Conjugated Estrogens, B.Approved
TacrineThe risk or severity of adverse effects can be increased when Rimexolone is combined with Tacrine.Withdrawn
TelaprevirThe serum concentration of Telaprevir can be decreased when it is combined with Rimexolone.Approved
TelithromycinThe serum concentration of Rimexolone can be increased when it is combined with Telithromycin.Approved
TemafloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Temafloxacin.Withdrawn
TenoxicamThe risk or severity of adverse effects can be increased when Tenoxicam is combined with Rimexolone.Approved
TepoxalinThe risk or severity of adverse effects can be increased when Tepoxalin is combined with Rimexolone.Vet Approved
TeriflunomideThe risk or severity of adverse effects can be increased when Teriflunomide is combined with Rimexolone.Approved
TestosteroneRimexolone may increase the fluid retaining activities of Testosterone.Approved, Investigational
TG4010The risk or severity of adverse effects can be increased when Rimexolone is combined with TG4010.Investigational
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Tiaprofenic acid is combined with Rimexolone.Approved
TiboloneThe serum concentration of Rimexolone can be increased when it is combined with Tibolone.Approved
TinoridineThe risk or severity of adverse effects can be increased when Tinoridine is combined with Rimexolone.Investigational
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Tolfenamic Acid is combined with Rimexolone.Approved
TolmetinThe risk or severity of adverse effects can be increased when Tolmetin is combined with Rimexolone.Approved
TorasemideRimexolone may increase the hypokalemic activities of Torasemide.Approved
TranilastThe risk or severity of adverse effects can be increased when Tranilast is combined with Rimexolone.Approved, Investigational
TrichlorfonThe risk or severity of adverse effects can be increased when Rimexolone is combined with Trichlorfon.Vet Approved
TrichlormethiazideRimexolone may increase the hypokalemic activities of Trichlormethiazide.Approved, Vet Approved
Trisalicylate-cholineThe risk or severity of adverse effects can be increased when Trisalicylate-choline is combined with Rimexolone.Approved
TrovafloxacinThe risk or severity of adverse effects can be increased when Rimexolone is combined with Trovafloxacin.Approved, Withdrawn
TubocurarineThe risk or severity of adverse effects can be increased when Rimexolone is combined with Tubocurarine.Approved
ValdecoxibThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Rimexolone.Investigational, Withdrawn
VoriconazoleThe serum concentration of Rimexolone can be increased when it is combined with Voriconazole.Approved, Investigational
WarfarinRimexolone may increase the anticoagulant activities of Warfarin.Approved
ZaltoprofenThe risk or severity of adverse effects can be increased when Zaltoprofen is combined with Rimexolone.Approved
ZeranolThe serum concentration of Rimexolone can be increased when it is combined with Zeranol.Vet Approved
ZileutonThe risk or severity of adverse effects can be increased when Zileuton is combined with Rimexolone.Approved, Investigational, Withdrawn
ZomepiracThe risk or severity of adverse effects can be increased when Zomepirac is combined with Rimexolone.Withdrawn
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesH02AB12S01BA13
AHFS Codes
  • 52:08.08
PDB EntriesNot Available
FDA labelDownload (108 KB)
MSDSDownload (248 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9796
Caco-2 permeable+0.7879
P-glycoprotein substrateSubstrate0.7261
P-glycoprotein inhibitor IInhibitor0.616
P-glycoprotein inhibitor IIInhibitor0.5126
Renal organic cation transporterNon-inhibitor0.8022
CYP450 2C9 substrateNon-substrate0.8142
CYP450 2D6 substrateNon-substrate0.9195
CYP450 3A4 substrateSubstrate0.7631
CYP450 1A2 substrateNon-inhibitor0.9521
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.6544
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7217
Ames testNon AMES toxic0.9396
CarcinogenicityNon-carcinogens0.9243
BiodegradationNot ready biodegradable0.9906
Rat acute toxicity2.1317 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8573
hERG inhibition (predictor II)Non-inhibitor0.7387
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Alcon laboratories inc
Packagers
Dosage forms
FormRouteStrength
Suspension / dropsOphthalmic10 mg/mL
SuspensionOphthalmic1 %
Prices
Unit descriptionCostUnit
Vexol 1% Suspension 10ml Bottle74.08USD bottle
Vexol 1% Suspension 5ml Bottle48.29USD bottle
Vexol 1% eye drops7.14USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityInsolubleNot Available
logP4.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0121 mg/mLALOGPS
logP3.64ALOGPS
logP4.38ChemAxon
logS-4.5ALOGPS
pKa (Strongest Acidic)18.76ChemAxon
pKa (Strongest Basic)-0.21ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area54.37 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity109.07 m3·mol-1ChemAxon
Polarizability42.91 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as 20-oxosteroids. These are steroid derivatives carrying a C=O group at the 20-position of the steroid skeleton.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassOxosteroids
Direct Parent20-oxosteroids
Alternative Parents
Substituents
  • 20-oxosteroid
  • Androgen-skeleton
  • Androstane-skeleton
  • 3-oxo-delta-1,4-steroid
  • 3-oxosteroid
  • Hydroxysteroid
  • 11-beta-hydroxysteroid
  • 11-hydroxysteroid
  • Delta-1,4-steroid
  • Cyclic alcohol
  • Ketone
  • Secondary alcohol
  • Cyclic ketone
  • Organooxygen compound
  • Alcohol
  • Carbonyl group
  • Organic oxide
  • Hydrocarbon derivative
  • Organic oxygen compound
  • Aliphatic homopolycyclic compound
Molecular FrameworkAliphatic homopolycyclic compounds
External DescriptorsNot 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. Hochhaus G, Moellmann HW: Binding affinities of rimexolone (ORG 6216), flunisolide and their putative metabolites for the glucocorticoid receptor of human synovial tissue. Agents Actions. 1990 Jun;30(3-4):377-80. [PubMed:2386110 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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
Molecular Weight:
45140.49 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23