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Tibolone
Tibolone is a small molecule pharmaceutical. It is currently being investigated in clinical studies. It is known to target estrogen receptor.
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
signs and symptoms pathological conditionsD013568
behavior and behavior mechanismsD001520
physiological phenomenaD010829
integumentary system physiological phenomenaD055827
biological phenomenaD001686
Trade Name
FDA
EMA
No data
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
No data
Labels
FDA
EMA
No data
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
anxietyEFO_0005230D001007F41.1
hot flashes—D019584—
sweating—D013546—
Agency Specific
FDA
EMA
No data
Patent Expiration
No data
ATC Codes
G: Genito urinary system and sex hormones
— G03: Sex hormones and modulators of the genital system
— G03C: Estrogens, sex hormones and modulators of the genital system
— G03CX: Other estrogens in atc
— G03CX01: Tibolone
HCPCS
No data
Clinical
Clinical Trials
23 clinical trials
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
MenopauseD008593EFO_0003922N95—11215
EndometriosisD004715EFO_0001065N80———112
OsteoporosisD010024EFO_0003882M81.0——11—2
AmenorrheaD000568N91.2———1—1
Hot flashesD019584———1—1
PostmenopauseD017698———1—1
Metabolic bone diseasesD001851HP_0000938———1—1
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Breast neoplasmsD001943EFO_0003869C50—12——3
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Postmenopausal osteoporosisD015663EFO_0003854—1———1
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
DepressionD003863F33.91————1
Major depressive disorderD003865EFO_0003761F221————1
Indications Without Phase
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
LeiomyomaD007889HP_0000131D25————11
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameTIBOLONE
INNtibolone
Description
Tibolone is estran-3-one with a double bond between positions 5 and 10, and bearing both an ethynyl group and a hydroxy group at position 17 (R-configuration). A synthetic steroid hormone drug which acts as an agonist at all five type I steroid hormone receptors, it is used in the prevention of postmenopausal osteoporosis and for treatment of endometriosis. It has a role as a hormone agonist and a bone density conservation agent. It is a 17beta-hydroxy steroid and a terminal acetylenic compound.
Classification
Small molecule
Drug classanabolic steroids; steroids (not prednisolone derivatives)
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
C#C[C@]1(O)CC[C@H]2[C@H]3[C@H](CC[C@@]21C)C1=C(CC(=O)CC1)C[C@H]3C
Identifiers
PDB—
CAS-ID5630-53-5
RxCUI38260
ChEMBL IDCHEMBL2103774
ChEBI ID32223
PubChem CID444008
DrugBankDB09070
UNII IDFF9X0205V2 (ChemIDplus, GSRS)
Target
Agency Approved
No data
Alternate
ESR1
ESR1
Organism
Homo sapiens
Gene name
ESR1
Gene synonyms
ESR, NR3A1
NCBI Gene ID
Protein name
estrogen receptor
Protein synonyms
E2 receptor alpha, ER-alpha, Estradiol receptor, estrogen nuclear receptor alpha, estrogen receptor alpha E1-E2-1-2, estrogen receptor alpha E1-N2-E2-1-2, Nuclear receptor subfamily 3 group A member 1, oestrogen receptor alpha
Uniprot ID
Mouse ortholog
Esr1 (13982)
estrogen receptor (Q9QY52)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 1,513 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
Mock data
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61 adverse events reported
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