This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification
NameTibolone
Accession NumberDB09070
TypeSmall Molecule
GroupsApproved
Description

Tibolone is a synthetic steroid hormone drug, which is fairly non-selective in its binding profile, acting as an agonist mainly at estrogen receptors, with a preference for ER alpha.

Structure
Thumb
Synonyms
17-hydroxy-7alpha-methyl-19-nor-17alpha-pregn-5(10)-en-20-yn-3-one
tibolona
tibolonum
External IDs ORG OD 14
Product Ingredients Not Available
ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
Categories
UNIIFF9X0205V2
CAS number5630-53-5
WeightAverage: 312.453
Monoisotopic: 312.208930142
Chemical FormulaC21H28O2
InChI KeyWZDGZWOAQTVYBX-XOINTXKNSA-N
InChI
InChI=1S/C21H28O2/c1-4-21(23)10-8-18-19-13(2)11-14-12-15(22)5-6-16(14)17(19)7-9-20(18,21)3/h1,13,17-19,23H,5-12H2,2-3H3/t13-,17-,18+,19-,20+,21+/m1/s1
IUPAC Name
(1S,9R,10R,11S,14R,15S)-14-ethynyl-14-hydroxy-9,15-dimethyltetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadec-2(7)-en-5-one
SMILES
[H][[email protected]@]12CC[[email protected]@](O)(C#C)[[email protected]@]1(C)CC[[email protected]]1([H])C3=C(CC(=O)CC3)C[[email protected]@]([H])(C)[[email protected]@]21[H]
Pharmacology
IndicationNot Available
Structured Indications Not Available
PharmacodynamicsNot Available
Mechanism of action
TargetKindPharmacological actionActionsOrganismUniProt ID
Estrogen receptor alphaProteinyes
agonist
HumanP03372 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organismsNot Available
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
16-BromoepiandrosteroneThe serum concentration of 16-Bromoepiandrosterone can be increased when it is combined with Tibolone.Investigational
19-norandrostenedioneThe serum concentration of 19-norandrostenedione can be increased when it is combined with Tibolone.Experimental, Illicit
5-androstenedioneThe serum concentration of 5-androstenedione can be increased when it is combined with Tibolone.Experimental, Illicit
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypotensive activities of Tibolone.Experimental
AbciximabTibolone may increase the anticoagulant activities of Abciximab.Approved
AcebutololAcebutolol may increase the hypotensive activities of Tibolone.Approved
AcenocoumarolTibolone may increase the anticoagulant activities of Acenocoumarol.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Tibolone.Approved
AlclometasoneThe serum concentration of Alclometasone can be increased when it is combined with Tibolone.Approved
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Tibolone.Experimental
AlfuzosinAlfuzosin may increase the hypotensive activities of Tibolone.Approved, Investigational
AliskirenAliskiren may increase the hypotensive activities of Tibolone.Approved, Investigational
AlprenololAlprenolol may increase the hypotensive activities of Tibolone.Approved, Withdrawn
AmbrisentanTibolone may increase the hypotensive activities of Ambrisentan.Approved, Investigational
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be increased when it is combined with Tibolone.Experimental
AmcinonideThe serum concentration of Amcinonide can be increased when it is combined with Tibolone.Approved
AmifostineTibolone may increase the hypotensive activities of Amifostine.Approved, Investigational
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Tibolone.Approved
AmlodipineAmlodipine may increase the hypotensive activities of Tibolone.Approved
AnastrozoleThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Tibolone.Approved, Investigational
AncrodTibolone may increase the anticoagulant activities of Ancrod.Investigational
AndrostenedioneThe serum concentration of 4-Androstenedione can be increased when it is combined with Tibolone.Experimental, Illicit
AnecortaveThe serum concentration of Anecortave can be increased when it is combined with Tibolone.Investigational
Anthrax immune globulin humanTibolone may increase the thrombogenic activities of Anthrax immune globulin human.Approved
Antithrombin III humanTibolone may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanTibolone may increase the anticoagulant activities of Apixaban.Approved
ArdeparinTibolone may increase the anticoagulant activities of Ardeparin.Approved, Withdrawn
ArgatrobanTibolone may increase the anticoagulant activities of Argatroban.Approved, Investigational
AtenololAtenolol may increase the hypotensive activities of Tibolone.Approved
BecaplerminTibolone may increase the anticoagulant activities of Becaplermin.Approved, Investigational
Beclomethasone dipropionateThe serum concentration of Beclomethasone dipropionate can be increased when it is combined with Tibolone.Approved, Investigational
BenazeprilBenazepril may increase the hypotensive activities of Tibolone.Approved, Investigational
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Tibolone.Approved
BenmoxinBenmoxin may increase the hypotensive activities of Tibolone.Withdrawn
BepridilBepridil may increase the hypotensive activities of Tibolone.Approved, Withdrawn
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Tibolone.Approved, Vet Approved
BetaxololBetaxolol may increase the hypotensive activities of Tibolone.Approved
BethanidineBethanidine may increase the hypotensive activities of Tibolone.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Tibolone.Approved, Investigational
BimatoprostBimatoprost may increase the hypotensive activities of Tibolone.Approved, Investigational
BisoprololBisoprolol may increase the hypotensive activities of Tibolone.Approved
BivalirudinTibolone may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BosentanBosentan may increase the hypotensive activities of Tibolone.Approved, Investigational
BretyliumBretylium may increase the hypotensive activities of Tibolone.Approved
BrimonidineBrimonidine may increase the hypotensive activities of Tibolone.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Tibolone.Approved
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Tibolone.Approved
BupranololBupranolol may increase the hypotensive activities of Tibolone.Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Tibolone.Approved
CandesartanCandesartan may increase the hypotensive activities of Tibolone.Approved
CandoxatrilCandoxatril may increase the hypotensive activities of Tibolone.Experimental
CaptoprilCaptopril may increase the hypotensive activities of Tibolone.Approved
CaroxazoneCaroxazone may increase the hypotensive activities of Tibolone.Withdrawn
CarteololCarteolol may increase the hypotensive activities of Tibolone.Approved
CarvedilolCarvedilol may increase the hypotensive activities of Tibolone.Approved, Investigational
CelecoxibCelecoxib may increase the thrombogenic activities of Tibolone.Approved, Investigational
CeliprololCeliprolol may increase the hypotensive activities of Tibolone.Approved, Investigational
CertoparinTibolone may increase the anticoagulant activities of Certoparin.Approved
Chenodeoxycholic acidThe therapeutic efficacy of Chenodeoxycholic acid can be decreased when used in combination with Tibolone.Approved
ChlorothiazideChlorothiazide may increase the hypotensive activities of Tibolone.Approved, Vet Approved
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Tibolone.Approved
Choline C 11The therapeutic efficacy of Choline C 11 can be decreased when used in combination with Tibolone.Approved
CiclesonideThe serum concentration of Ciclesonide can be increased when it is combined with Tibolone.Approved, Investigational
CilazaprilCilazapril may increase the hypotensive activities of Tibolone.Approved
Citric AcidTibolone may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClobetasolThe serum concentration of Clobetasol can be increased when it is combined with Tibolone.Investigational
Clobetasol propionateThe serum concentration of Clobetasol propionate can be increased when it is combined with Tibolone.Approved
ClocortoloneThe serum concentration of Clocortolone can be increased when it is combined with Tibolone.Approved
ClonidineClonidine may increase the hypotensive activities of Tibolone.Approved
Conestat alfaTibolone may increase the thrombogenic activities of C1 Esterase Inhibitor (Recombinant).Approved
Cortisone acetateThe serum concentration of Cortisone acetate can be increased when it is combined with Tibolone.Approved
CryptenamineCryptenamine may increase the hypotensive activities of Tibolone.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Tibolone.Approved, Investigational
CyclothiazideCyclothiazide may increase the hypotensive activities of Tibolone.Approved
Dabigatran etexilateTibolone may increase the anticoagulant activities of Dabigatran etexilate.Approved
DalteparinTibolone may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidTibolone may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarexabanTibolone may increase the anticoagulant activities of Ym150.Investigational
DebrisoquinDebrisoquin may increase the hypotensive activities of Tibolone.Approved
DeserpidineTibolone may increase the hypotensive activities of Deserpidine.Approved
DesirudinTibolone may increase the anticoagulant activities of Desirudin.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Tibolone.Approved
DesoximetasoneThe serum concentration of Desoximetasone can be increased when it is combined with Tibolone.Approved
Desoxycorticosterone acetateThe serum concentration of Desoxycorticosterone acetate can be increased when it is combined with Tibolone.Approved
Desoxycorticosterone PivalateThe serum concentration of Desoxycorticosterone Pivalate can be increased when it is combined with Tibolone.Experimental, Vet Approved
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Tibolone.Approved, Investigational, Vet Approved
Dexamethasone isonicotinateThe serum concentration of Dexamethasone isonicotinate can be increased when it is combined with Tibolone.Vet Approved
DextranTibolone may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Tibolone may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Tibolone may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Tibolone may increase the anticoagulant activities of Dextran 75.Approved
DiazoxideDiazoxide may increase the hypotensive activities of Tibolone.Approved
DicoumarolTibolone may increase the anticoagulant activities of Dicoumarol.Approved
DiflorasoneThe serum concentration of Diflorasone can be increased when it is combined with Tibolone.Approved
DifluocortoloneThe serum concentration of Difluocortolone can be increased when it is combined with Tibolone.Approved
DifluprednateThe serum concentration of Difluprednate can be increased when it is combined with Tibolone.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Tibolone.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Tibolone.Approved
DihydralazineTibolone may increase the hypotensive activities of Dihydralazine.Investigational
DiltiazemDiltiazem may increase the hypotensive activities of Tibolone.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Tibolone.Approved, Investigational
DorzolamideDorzolamide may increase the hypotensive activities of Tibolone.Approved
DoxazosinDoxazosin may increase the hypotensive activities of Tibolone.Approved
DyphyllineThe serum concentration of Dyphylline can be increased when it is combined with Tibolone.Approved
Edetic AcidTibolone may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanTibolone may increase the anticoagulant activities of Edoxaban.Approved
EfonidipineTibolone may increase the hypotensive activities of Efonidipine.Approved
EnalaprilEnalapril may increase the hypotensive activities of Tibolone.Approved, Vet Approved
EnalaprilatTibolone may increase the hypotensive activities of Enalaprilat.Approved
EnoxaparinTibolone may increase the anticoagulant activities of Enoxaparin.Approved
EpoprostenolEpoprostenol may increase the hypotensive activities of Tibolone.Approved
EprosartanEprosartan may increase the hypotensive activities of Tibolone.Approved
EquileninThe serum concentration of Equilenin can be increased when it is combined with Tibolone.Experimental
EquilinThe serum concentration of Equilin can be increased when it is combined with Tibolone.Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Tibolone.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be increased when it is combined with Tibolone.Approved
Ethyl biscoumacetateTibolone may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtodolacEtodolac may increase the thrombogenic activities of Tibolone.Approved, Investigational, Vet Approved
EtoricoxibEtoricoxib may increase the thrombogenic activities of Tibolone.Approved, Investigational
ExemestaneThe therapeutic efficacy of Exemestane can be decreased when used in combination with Tibolone.Approved, Investigational
FelodipineFelodipine may increase the hypotensive activities of Tibolone.Approved, Investigational
FenoldopamFenoldopam may increase the hypotensive activities of Tibolone.Approved
fluasteroneThe serum concentration of fluasterone can be increased when it is combined with Tibolone.Investigational
FludrocortisoneThe serum concentration of Fludrocortisone can be increased when it is combined with Tibolone.Approved
FluindioneTibolone may increase the anticoagulant activities of Fluindione.Investigational
FlumethasoneThe serum concentration of Flumethasone can be increased when it is combined with Tibolone.Approved, Vet Approved
FlunisolideThe serum concentration of Flunisolide can be increased when it is combined with Tibolone.Approved, Investigational
Fluocinolone AcetonideThe serum concentration of Fluocinolone Acetonide can be increased when it is combined with Tibolone.Approved, Investigational, Vet Approved
FluocinonideThe serum concentration of Fluocinonide can be increased when it is combined with Tibolone.Approved, Investigational
FluocortoloneThe serum concentration of Fluocortolone can be increased when it is combined with Tibolone.Approved, Withdrawn
FluorometholoneThe serum concentration of Fluorometholone can be increased when it is combined with Tibolone.Approved
FluprednideneThe serum concentration of Fluprednidene can be increased when it is combined with Tibolone.Approved, Withdrawn
FluprednisoloneThe serum concentration of Fluprednisolone can be increased when it is combined with Tibolone.Approved
FlurandrenolideThe serum concentration of Flurandrenolide can be increased when it is combined with Tibolone.Approved
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Tibolone.Approved
Fluticasone propionateThe serum concentration of Fluticasone Propionate can be increased when it is combined with Tibolone.Approved
FondaparinuxTibolone may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumTibolone may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
FormestaneThe serum concentration of Formestane can be increased when it is combined with Tibolone.Approved, Investigational, Withdrawn
FosinoprilFosinopril may increase the hypotensive activities of Tibolone.Approved
FurazolidoneFurazolidone may increase the hypotensive activities of Tibolone.Approved, Vet Approved
GabexateTibolone may increase the anticoagulant activities of Gabexate.Investigational
GuanabenzGuanabenz may increase the hypotensive activities of Tibolone.Approved
GuanadrelGuanadrel may increase the hypotensive activities of Tibolone.Approved
GuanethidineGuanethidine may increase the hypotensive activities of Tibolone.Approved
GuanfacineGuanfacine may increase the hypotensive activities of Tibolone.Approved, Investigational
HE3286The serum concentration of HE3286 can be increased when it is combined with Tibolone.Investigational
HeparinTibolone may increase the anticoagulant activities of Heparin.Approved, Investigational
HexamethoniumHexamethonium may increase the hypotensive activities of Tibolone.Experimental
Human C1-esterase inhibitorTibolone may increase the thrombogenic activities of C1 Esterase Inhibitor (Human).Approved
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Tibolone.Approved, Investigational
HydracarbazineHydracarbazine may increase the hypotensive activities of Tibolone.Experimental
HydralazineHydralazine may increase the hypotensive activities of Tibolone.Approved
HydrochlorothiazideHydrochlorothiazide may increase the hypotensive activities of Tibolone.Approved, Vet Approved
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Tibolone.Approved, Vet Approved
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Tibolone.Approved
IdraparinuxTibolone may increase the anticoagulant activities of idraparinux.Investigational
IloprostIloprost may increase the hypotensive activities of Tibolone.Approved, Investigational
ImidaprilTibolone may increase the hypotensive activities of Imidapril.Investigational
IndapamideIndapamide may increase the hypotensive activities of Tibolone.Approved
IndenololIndenolol may increase the hypotensive activities of Tibolone.Withdrawn
IndoraminIndoramin may increase the hypotensive activities of Tibolone.Withdrawn
IproclozideIproclozide may increase the hypotensive activities of Tibolone.Withdrawn
IproniazidIproniazid may increase the hypotensive activities of Tibolone.Withdrawn
IrbesartanIrbesartan may increase the hypotensive activities of Tibolone.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Tibolone.Approved
IsradipineIsradipine may increase the hypotensive activities of Tibolone.Approved
IstaroximeThe serum concentration of Istaroxime can be increased when it is combined with Tibolone.Investigational
KetanserinTibolone may increase the hypotensive activities of Ketanserin.Investigational
LabetalolLabetalol may increase the hypotensive activities of Tibolone.Approved
LacidipineTibolone may increase the hypotensive activities of Lacidipine.Approved
LatanoprostLatanoprost may increase the hypotensive activities of Tibolone.Approved, Investigational
LenalidomideTibolone may increase the thrombogenic activities of Lenalidomide.Approved
LepirudinTibolone may increase the anticoagulant activities of Lepirudin.Approved
LercanidipineLercanidipine may increase the hypotensive activities of Tibolone.Approved, Investigational
LevothyroxineThe therapeutic efficacy of Levothyroxine can be decreased when used in combination with Tibolone.Approved
LiothyronineThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Tibolone.Approved, Vet Approved
LiotrixThe therapeutic efficacy of Liotrix can be decreased when used in combination with Tibolone.Approved
LisinoprilLisinopril may increase the hypotensive activities of Tibolone.Approved, Investigational
LofexidineLofexidine may increase the hypotensive activities of Tibolone.Approved, Investigational
LosartanLosartan may increase the hypotensive activities of Tibolone.Approved
LumiracoxibLumiracoxib may increase the thrombogenic activities of Tibolone.Approved, Investigational
MacitentanTibolone may increase the hypotensive activities of Macitentan.Approved
ManidipineTibolone may increase the hypotensive activities of Manidipine.Approved
ME-609The serum concentration of ME-609 can be increased when it is combined with Tibolone.Investigational
MebanazineMebanazine may increase the hypotensive activities of Tibolone.Withdrawn
MecamylamineMecamylamine may increase the hypotensive activities of Tibolone.Approved
MedrysoneThe serum concentration of Medrysone can be increased when it is combined with Tibolone.Approved
MelengestrolThe serum concentration of Melengestrol can be increased when it is combined with Tibolone.Vet Approved
MethyldopaMethyldopa may increase the hypotensive activities of Tibolone.Approved
Methylene blueMethylene blue may increase the hypotensive activities of Tibolone.Investigational
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Tibolone.Approved, Investigational
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Tibolone.Approved, Vet Approved
MetipranololMetipranolol may increase the hypotensive activities of Tibolone.Approved
MetolazoneMetolazone may increase the hypotensive activities of Tibolone.Approved
MetoprololMetoprolol may increase the hypotensive activities of Tibolone.Approved, Investigational
MetyrosineTibolone may increase the hypotensive activities of Metyrosine.Approved
MibefradilMibefradil may increase the hypotensive activities of Tibolone.Withdrawn
MinaprineMinaprine may increase the hypotensive activities of Tibolone.Approved
MinoxidilMinoxidil may increase the hypotensive activities of Tibolone.Approved
MoclobemideMoclobemide may increase the hypotensive activities of Tibolone.Approved
MoexiprilMoexipril may increase the hypotensive activities of Tibolone.Approved
MolsidomineMolsidomine may increase the hypotensive activities of Tibolone.Approved
MometasoneThe serum concentration of Mometasone can be increased when it is combined with Tibolone.Approved, Vet Approved
MoxonidineTibolone may increase the hypotensive activities of Moxonidine.Approved
NabumetoneNabumetone may increase the thrombogenic activities of Tibolone.Approved
NadololNadolol may increase the hypotensive activities of Tibolone.Approved
NadroparinTibolone may increase the anticoagulant activities of Nadroparin.Approved
NafamostatTibolone may increase the anticoagulant activities of Nafamostat.Approved, Investigational
NaftopidilTibolone may increase the hypotensive activities of Naftopidil.Investigational
NCX 1022The serum concentration of NCX 1022 can be increased when it is combined with Tibolone.Investigational
NebivololNebivolol may increase the hypotensive activities of Tibolone.Approved, Investigational
NialamideNialamide may increase the hypotensive activities of Tibolone.Withdrawn
NicardipineNicardipine may increase the hypotensive activities of Tibolone.Approved
NicorandilTibolone may increase the hypotensive activities of Nicorandil.Approved
NiguldipineTibolone may increase the hypotensive activities of Niguldipine.Experimental
NilvadipineNilvadipine may increase the hypotensive activities of Tibolone.Approved
NimodipineNimodipine may increase the hypotensive activities of Tibolone.Approved
NisoldipineNisoldipine may increase the hypotensive activities of Tibolone.Approved
NitrendipineNitrendipine may increase the hypotensive activities of Tibolone.Approved
NitroprussideNitroprusside may increase the hypotensive activities of Tibolone.Approved
ObinutuzumabTibolone may increase the hypotensive activities of Obinutuzumab.Approved
OctamoxinOctamoxin may increase the hypotensive activities of Tibolone.Withdrawn
OleandrinAnvirzel may decrease the cardiotoxic activities of Tibolone.Experimental
Oleoyl-estroneThe serum concentration of Oleoyl estrone can be increased when it is combined with Tibolone.Investigational
OlmesartanOlmesartan may increase the hypotensive activities of Tibolone.Approved, Investigational
OmapatrilatOmapatrilat may increase the hypotensive activities of Tibolone.Investigational
OspemifeneThe risk or severity of adverse effects can be increased when Tibolone is combined with Ospemifene.Approved
OtamixabanTibolone may increase the anticoagulant activities of Otamixaban.Investigational
OuabainOuabain may decrease the cardiotoxic activities of Tibolone.Approved
OxprenololOxprenolol may increase the hypotensive activities of Tibolone.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Tibolone.Approved, Vet Approved
ParamethasoneThe serum concentration of Paramethasone can be increased when it is combined with Tibolone.Approved
ParecoxibParecoxib may increase the thrombogenic activities of Tibolone.Approved
PargylinePargyline may increase the hypotensive activities of Tibolone.Approved
PenbutololPenbutolol may increase the hypotensive activities of Tibolone.Approved, Investigational
PentoliniumPentolinium may increase the hypotensive activities of Tibolone.Approved
Pentosan PolysulfateTibolone may increase the anticoagulant activities of Pentosan Polysulfate.Approved
PentoxifyllinePentoxifylline may increase the hypotensive activities of Tibolone.Approved, Investigational
PerindoprilPerindopril may increase the hypotensive activities of Tibolone.Approved
PhenelzinePhenelzine may increase the hypotensive activities of Tibolone.Approved
PhenindioneTibolone may increase the anticoagulant activities of Phenindione.Approved
PheniprazinePheniprazine may increase the hypotensive activities of Tibolone.Withdrawn
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Tibolone.Approved
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Tibolone.Withdrawn
PhenprocoumonTibolone may increase the anticoagulant activities of Phenprocoumon.Approved
PhentolaminePhentolamine may increase the hypotensive activities of Tibolone.Approved
PinacidilPinacidil may increase the hypotensive activities of Tibolone.Withdrawn
PindololPindolol may increase the hypotensive activities of Tibolone.Approved
PirlindolePirlindole may increase the hypotensive activities of Tibolone.Approved
PivhydrazinePivhydrazine may increase the hypotensive activities of Tibolone.Withdrawn
PolythiazidePolythiazide may increase the hypotensive activities of Tibolone.Approved
PrasteroneThe risk or severity of adverse effects can be increased when Prasterone is combined with Tibolone.Approved, Nutraceutical
Prasterone sulfateThe serum concentration of dehydroepiandrosterone sulfate can be increased when it is combined with Tibolone.Investigational
PrazosinPrazosin may increase the hypotensive activities of Tibolone.Approved
PrednicarbateThe serum concentration of Prednicarbate can be increased when it is combined with Tibolone.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Tibolone.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Tibolone.Approved, Vet Approved
PregnenoloneThe serum concentration of Pregnenolone can be increased when it is combined with Tibolone.Experimental
PropranololPropranolol may increase the hypotensive activities of Tibolone.Approved, Investigational
Protein CTibolone may increase the anticoagulant activities of Protein C.Approved
Protein S humanTibolone may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeTibolone may increase the anticoagulant activities of Protocatechualdehyde.Approved
QuinaprilQuinapril may increase the hypotensive activities of Tibolone.Approved, Investigational
QuinineQuinine may increase the hypotensive activities of Tibolone.Approved
RamiprilRamipril may increase the hypotensive activities of Tibolone.Approved
RasagilineRasagiline may increase the hypotensive activities of Tibolone.Approved
RemikirenRemikiren may increase the hypotensive activities of Tibolone.Approved
RescinnamineTibolone may increase the hypotensive activities of Rescinnamine.Approved
ReserpineReserpine may increase the hypotensive activities of Tibolone.Approved
ReviparinTibolone may increase the anticoagulant activities of Reviparin.Approved
RilmenidineTibolone may increase the hypotensive activities of Rilmenidine.Investigational
RimexoloneThe serum concentration of Rimexolone can be increased when it is combined with Tibolone.Approved
RiociguatTibolone may increase the hypotensive activities of Riociguat.Approved
RituximabTibolone may increase the hypotensive activities of Rituximab.Approved
RivaroxabanTibolone may increase the anticoagulant activities of Rivaroxaban.Approved
RofecoxibRofecoxib may increase the thrombogenic activities of Tibolone.Investigational, Withdrawn
RopiniroleThe serum concentration of Ropinirole can be increased when it is combined with Tibolone.Approved, Investigational
SafrazineSafrazine may increase the hypotensive activities of Tibolone.Withdrawn
SaprisartanSaprisartan may increase the hypotensive activities of Tibolone.Experimental
SelegilineSelegiline may increase the hypotensive activities of Tibolone.Approved, Investigational, Vet Approved
SelexipagTibolone may increase the hypotensive activities of Selexipag.Approved
SildenafilSildenafil may increase the antihypertensive activities of Tibolone.Approved, Investigational
SitaxentanTibolone may increase the hypotensive activities of Sitaxentan.Approved, Investigational, Withdrawn
SomatotropinThe therapeutic efficacy of Somatropin recombinant can be decreased when used in combination with Tibolone.Approved, Investigational
SpiraprilSpirapril may increase the hypotensive activities of Tibolone.Approved
SulodexideTibolone may increase the anticoagulant activities of Sulodexide.Approved, Investigational
TadalafilTadalafil may increase the antihypertensive activities of Tibolone.Approved, Investigational
TelmisartanTelmisartan may increase the hypotensive activities of Tibolone.Approved, Investigational
TemocaprilTemocapril may increase the hypotensive activities of Tibolone.Experimental, Investigational
TerlipressinTerlipressin may increase the hypotensive activities of Tibolone.Approved, Investigational
ThalidomideTibolone may increase the thrombogenic activities of Thalidomide.Approved, Investigational, Withdrawn
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Tibolone.Approved
Thyroid, porcineThe therapeutic efficacy of Thyroid, porcine can be decreased when used in combination with Tibolone.Approved
TicrynafenTicrynafen may increase the hypotensive activities of Tibolone.Withdrawn
TimololTimolol may increase the hypotensive activities of Tibolone.Approved
TipranavirTibolone may increase the dermatologic adverse activities of Tipranavir.Approved, Investigational
TixocortolThe serum concentration of Tixocortol can be increased when it is combined with Tibolone.Approved
TolazolineTolazoline may increase the hypotensive activities of Tibolone.Approved, Vet Approved
ToloxatoneToloxatone may increase the hypotensive activities of Tibolone.Approved
TorasemideTorasemide may increase the hypotensive activities of Tibolone.Approved
TrandolaprilTrandolapril may increase the hypotensive activities of Tibolone.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Tibolone.Experimental
TranylcypromineTranylcypromine may increase the hypotensive activities of Tibolone.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Tibolone.Approved, Investigational
TravoprostTravoprost may increase the hypotensive activities of Tibolone.Approved
TreprostinilTreprostinil may increase the hypotensive activities of Tibolone.Approved, Investigational
TriamcinoloneThe serum concentration of Triamcinolone can be increased when it is combined with Tibolone.Approved, Vet Approved
TrichlormethiazideTrichlormethiazide may increase the hypotensive activities of Tibolone.Approved, Vet Approved
TrimazosinTibolone may increase the hypotensive activities of Trimazosin.Experimental
TrimethaphanTrimethaphan may increase the hypotensive activities of Tibolone.Approved
UdenafilUdenafil may increase the antihypertensive activities of Tibolone.Approved, Investigational
UnoprostoneUnoprostone may increase the hypotensive activities of Tibolone.Approved
Ursodeoxycholic acidThe therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Tibolone.Approved, Investigational
ValdecoxibValdecoxib may increase the thrombogenic activities of Tibolone.Investigational, Withdrawn
ValsartanValsartan may increase the hypotensive activities of Tibolone.Approved, Investigational
VardenafilVardenafil may increase the antihypertensive activities of Tibolone.Approved
VinpocetineTibolone may increase the hypotensive activities of Vinpocetine.Investigational
Vitamin CThe serum concentration of Tibolone can be increased when it is combined with Vitamin C.Approved, Nutraceutical
WarfarinTibolone may increase the anticoagulant activities of Warfarin.Approved
XimelagatranTibolone may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
XylometazolineXylometazoline may increase the hypotensive activities of Tibolone.Approved
YohimbineYohimbine may decrease the antihypertensive activities of Tibolone.Approved, Vet Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesG03CX01 — Tibolone
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1Unknown StatusTreatmentDepressive State / Major Depressive Disorder (MDD)1
2CompletedTreatmentCancer, Breast / Menopause / Postmenopausal Bone Loss1
3CompletedOtherPostmenopausal Women1
3CompletedTreatmentCancer, Breast1
3CompletedTreatmentCancer, Breast / Climacteric Symptoms1
3CompletedTreatmentSexual Dysfunctions1
3CompletedTreatmentBone destruction1
4CompletedPreventionCholesterol, HDL1
4CompletedTreatmentMenopause2
4CompletedTreatmentOsteopenia1
4CompletedTreatmentVasomotor Symptoms1
4CompletedTreatmentBone destruction / One to five years postmenopausal1
4Not Yet RecruitingTreatmentAmenorrhea / Endometriosis / Quality of Life1
4RecruitingTreatmentMenopausal Depression1
4RecruitingTreatmentMenopausal Syndromes1
4TerminatedTreatmentPerimenopausal Depression1
Not AvailableCompletedTreatmentFlow-mediated Dilation Evaluation of the Brachial Artery1
Not AvailableCompletedTreatmentMenopause1
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.00722 mg/mLALOGPS
logP2.69ALOGPS
logP3.1ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)16.27ChemAxon
pKa (Strongest Basic)-1.7ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area37.3 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity91.73 m3·mol-1ChemAxon
Polarizability36.77 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET featuresNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-qTof , PositiveNot Available
LC-MS/MSLC-MS/MS Spectrum - , positivesplash10-0002-0971000000-09912161a9fdfe89ed83View in MoNA
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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as oxosteroids. These are steroid derivatives carrying a C=O group attached to steroid skeleton.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassOxosteroids
Direct ParentOxosteroids
Alternative Parents3-oxosteroids / 17-hydroxysteroids / Cyclohexenones / Ynones / Tertiary alcohols / Cyclic alcohols and derivatives / Acetylides / Organic oxides / Hydrocarbon derivatives
Substituents3-oxosteroid / Hydroxysteroid / Oxosteroid / 17-hydroxysteroid / Cyclohexenone / Ynone / Cyclic alcohol / Tertiary alcohol / Ketone / Cyclic ketone
Molecular FrameworkAliphatic homopolycyclic compounds
External Descriptorsterminal acetylenic compound, 17beta-hydroxy steroid (CHEBI:32223 )

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription fact...
Gene Name:
ESR1
Uniprot ID:
P03372
Uniprot Name:
Estrogen receptor
Molecular Weight:
66215.45 Da
References
  1. Escande A, Servant N, Rabenoelina F, Auzou G, Kloosterboer H, Cavailles V, Balaguer P, Maudelonde T: Regulation of activities of steroid hormone receptors by tibolone and its primary metabolites. J Steroid Biochem Mol Biol. 2009 Aug;116(1-2):8-14. doi: 10.1016/j.jsbmb.2009.03.008. Epub 2009 Apr 2. [PubMed:19464167 ]
Drug created on May 14, 2015 09:49 / Updated on September 01, 2017 12:01