Estrone
Estrogenic Substance, Theelin (estrone) is a small molecule pharmaceutical. Estrone was first approved as Theelin on 1982-01-01. It is used to treat breast neoplasms, hot flashes, hypogonadism, menorrhagia, and premature menopause amongst others in the USA. The pharmaceutical is active against estrogen receptor. In addition, it is known to target estrogen receptor beta, solute carrier organic anion transporter family member 1A2, solute carrier organic anion transporter family member 1C1, solute carrier organic anion transporter family member 2B1, solute carrier organic anion transporter family member 4A1, solute carrier organic anion transporter family member 3A1, and solute carrier organic anion transporter family member 1B1.
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Commercial
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)
Estrone
Tradename | Company | Number | Date | Products |
|---|---|---|---|---|
| THEELIN | Parkedale Pharmaceuticals | N-003977 DISCN | 1982-01-01 | 3 products |
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Labels
FDA
EMA
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Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| breast neoplasms | EFO_0003869 | D001943 | C50 |
| hot flashes | — | D019584 | — |
| hypogonadism | HP_0000815 | D007006 | E23.0 |
| menorrhagia | HP_0000132 | D008595 | N92.0 |
| premature menopause | HP_0008209 | D008594 | E28.31 |
| primary ovarian insufficiency | EFO_0004266 | D016649 | E28.3 |
| prostatic neoplasms | — | D011471 | C61 |
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
— G03CA: Natural and semisynthetic estrogens, plain
— G03CA07: Estrone
— G03CC: Estrogens, combinations with other drugs
— G03CC04: Estrone
HCPCS
Code | Description |
|---|---|
| J1435 | Injection, estrone, per 1 mg |
Clinical
Clinical Trials
70 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Healthy volunteers/patients | — | 5 | 1 | 1 | 3 | 1 | 10 | ||
| Adenomatous polyposis coli | D011125 | — | — | — | 2 | — | 2 | ||
| Asthma | D001249 | EFO_0000270 | J45 | — | — | — | 1 | — | 1 |
| Acne vulgaris | D000152 | EFO_0003894 | L70 | — | — | — | 1 | — | 1 |
| Bronchiolitis obliterans | D001989 | EFO_0007183 | — | — | — | 1 | — | 1 | |
| Obesity | D009765 | EFO_0001073 | E66.9 | — | — | — | 1 | — | 1 |
| Blepharitis | D001762 | EFO_0009536 | H01.0 | — | — | — | 1 | — | 1 |
| Pancreatitis | D010195 | EFO_0000278 | K85 | — | — | — | 1 | — | 1 |
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Pneumonia | D011014 | EFO_0003106 | J18 | — | — | 1 | — | 2 | 3 |
| Chlamydia infections | D002690 | EFO_0007205 | A74.9 | — | 1 | 1 | — | — | 2 |
| Non-small-cell lung carcinoma | D002289 | — | — | 1 | — | 1 | 2 | ||
| Hiv infections | D015658 | EFO_0000764 | B20 | 1 | — | 1 | — | — | 2 |
| Premature rupture fetal membranes | D005322 | HP_0001788 | O42 | — | — | 1 | — | — | 1 |
| Gastrointestinal hemorrhage | D006471 | K92.2 | — | — | 1 | — | — | 1 | |
| Hematemesis | D006396 | HP_0002248 | K92.0 | — | — | 1 | — | — | 1 |
| Epidermolysis bullosa | D004820 | Q81 | — | — | 1 | — | — | 1 | |
| Chronic obstructive pulmonary disease | D029424 | EFO_0000341 | J44.9 | — | 1 | 1 | — | — | 1 |
| Ophthalmia neonatorum | D009878 | A54.31 | — | — | 1 | — | — | 1 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Gastroparesis | D018589 | EFO_1000948 | K31.84 | — | 2 | — | — | — | 2 |
| Breast neoplasms | D001943 | EFO_0003869 | C50 | — | 2 | — | — | — | 2 |
| Feeding and eating disorders | D001068 | F50 | — | 1 | — | — | 1 | 2 | |
| Metabolic syndrome | D024821 | EFO_0000195 | E88.81 | 1 | 1 | — | — | — | 1 |
| Pulmonary fibrosis | D011658 | J84.10 | 1 | 1 | — | — | — | 1 | |
| Hermanski-pudlak syndrome | D022861 | E70.331 | 1 | 1 | — | — | — | 1 | |
| Oculocutaneous albinism | D016115 | E70.32 | 1 | 1 | — | — | — | 1 | |
| Platelet storage pool deficiency | D010981 | EFO_1001112 | 1 | 1 | — | — | — | 1 | |
| Pancreatic neoplasms | D010190 | EFO_0003860 | C25 | — | 1 | — | — | — | 1 |
| Stomach neoplasms | D013274 | EFO_0003897 | C16 | — | 1 | — | — | — | 1 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Hepacivirus | D016174 | 1 | — | — | — | — | 1 | ||
| Renal insufficiency | D051437 | HP_0000083 | N19 | 1 | — | — | — | — | 1 |
| B-cell chronic lymphocytic leukemia | D015451 | C91.1 | 1 | — | — | — | — | 1 | |
| Pharmacokinetics | D010599 | 1 | — | — | — | — | 1 | ||
| Type 1 diabetes mellitus | D003922 | EFO_0001359 | E10 | 1 | — | — | — | — | 1 |
| Neoplasms | D009369 | C80 | 1 | — | — | — | — | 1 | |
| Hepatocellular carcinoma | D006528 | C22.0 | 1 | — | — | — | — | 1 |
Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Liver cirrhosis | D008103 | EFO_0001422 | K74.0 | — | — | — | — | 2 | 2 |
| Pregnancy | D011247 | EFO_0002950 | Z33.1 | — | — | — | — | 1 | 1 |
| Delirium | D003693 | R41.0 | — | — | — | — | 1 | 1 | |
| Inflammation | D007249 | — | — | — | — | 1 | 1 | ||
| Parkinson disease | D010300 | EFO_0002508 | G20 | — | — | — | — | 1 | 1 |
| Sepsis | D018805 | A41.9 | — | — | — | — | 1 | 1 | |
| Septic shock | D012772 | A48.3 | — | — | — | — | 1 | 1 | |
| Skin diseases | D012871 | L00-L99 | — | — | — | — | 1 | 1 | |
| Whooping cough | D014917 | EFO_0000650 | A37 | — | — | — | — | 1 | 1 |
| Postoperative nausea and vomiting | D020250 | EFO_0004888 | — | — | — | — | 1 | 1 |
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Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | ESTRONE |
| INN | estrone |
| Description | Estrone is a 17-oxo steroid that is estra-1,3,5(10)-triene substituted by an hydroxy group at position 3 and an oxo group at position 17. It has a role as an estrogen, a bone density conservation agent, an antineoplastic agent, a human metabolite and a mouse metabolite. It is a 3-hydroxy steroid, a phenolic steroid, a member of phenols and a 17-oxo steroid. It derives from a hydride of an estrane. |
| Classification | Small molecule |
| Drug class | estrogens |
| Image (chem structure or protein) | |
| Structure (InChI/SMILES or Protein Sequence) | C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O |
Identifiers
| PDB | 3HM1 |
| CAS-ID | 53-16-7 |
| RxCUI | 4103 |
| ChEMBL ID | CHEMBL1405 |
| ChEBI ID | 17263 |
| PubChem CID | 5870 |
| DrugBank | DB00655 |
| UNII ID | 2DI9HA706A (ChemIDplus, GSRS) |
Target
Agency Approved
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)
Alternate
ESR2
ESR2
SLCO1A2
SLCO1A2
SLCO1C1
SLCO1C1
SLCO2B1
SLCO2B1
SLCO4A1
SLCO4A1
SLCO3A1
SLCO3A1
SLCO1B1
SLCO1B1
Organism
Homo sapiens
Gene name
ESR2
Gene synonyms
ESTRB, NR3A2
NCBI Gene ID
Protein name
estrogen receptor beta
Protein synonyms
estrogen receptor beta 2, estrogen receptor beta 4, Nuclear receptor subfamily 3 group A member 2, oestrogen receptor beta
Uniprot ID
Mouse ortholog
Esr2 (13983)
estrogen receptor beta (O08537)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
0 adverse events reported
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