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Onapristone
Onapristone is a small molecule pharmaceutical. It is currently being investigated in clinical studies. It is known to target glucocorticoid receptor, mineralocorticoid receptor, and progesterone receptor.
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Commercial
Therapeutic Areas
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Trade Name
FDA
EMA
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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
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Indications
FDA
EMA
No data
Agency Specific
FDA
EMA
No data
Patent Expiration
No data
ATC Codes
No data
HCPCS
No data
Clinical
Clinical Trials
8 clinical trials
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Indications Phases 4
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Indications Phases 3
No data
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Breast neoplasmsD001943EFO_0003869C50324
Endometrial neoplasmsD016889EFO_000423022
NeoplasmsD009369C8011
Triple negative breast neoplasmsD06472611
Prostatic neoplasmsD011471C61111
Castration-resistant prostatic neoplasmsD064129111
Endometrioid carcinomaD01826911
Acinar cell carcinomaD01826711
Indications Phases 1
No data
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameONAPRISTONE
INNonapristone
Description
Onapristone (INN) (developmental code names ZK-89299, ZK-299) is a synthetic and steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering and described in 1984 but was never marketed. It is a silent antagonist of the progesterone receptor (PR), in contrast to the related antiprogestogen mifepristone (which is a weak partial agonist of the receptor). Moreover, compared to mifepristone, onapristone has reduced antiglucocorticoid activity, shows little antiandrogenic activity, and has 10- to 30-fold greater potency as an antiprogestogen. The medication was under development for clinical use, for instance in the treatment of breast cancer and as an endometrial contraceptive, but was discontinued during phase III clinical trials in 1995 due to findings that liver function abnormalities developed in a majority patients.
Classification
Small molecule
Drug classsteriodal compounds acting on progesterone receptors (excluding-gest- compounds); progesterone receptor antagonists
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
CN(C)c1ccc([C@H]2C[C@]3(C)[C@@H](CC[C@]3(O)CCCO)[C@@H]3CCC4=CC(=O)CCC4=C32)cc1
Identifiers
PDB
CAS-ID96346-61-1
RxCUI
ChEMBL IDCHEMBL1908373
ChEBI ID
PubChem CID5311505
DrugBankDB12637
UNII IDH6H7G23O3N (ChemIDplus, GSRS)
Target
Agency Approved
No data
Alternate
NR3C1
NR3C1
NR3C2
NR3C2
PGR
PGR
Organism
Homo sapiens
Gene name
NR3C1
Gene synonyms
GRL
NCBI Gene ID
Protein name
glucocorticoid receptor
Protein synonyms
Nuclear receptor subfamily 3 group C member 1, nuclear receptor subfamily 3 group C member 1 variant hGR-B(54), nuclear receptor subfamily 3 group C member 1 variant hGR-B(77), nuclear receptor subfamily 3 group C member 1 variant hGR-B(93), nuclear receptor subfamily 3, group C, member 1 (glucocorticoid receptor)
Uniprot ID
Mouse ortholog
Nr3c1 (14815)
glucocorticoid receptor (Q61629)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 269 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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7 adverse events reported
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