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 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, estrogen receptor beta, solute carrier organic anion transporter family member 3A1, and solute carrier organic anion transporter family member 1B1.
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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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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
763 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Infertility | D007246 | EFO_0000545 | — | 24 | 29 | 47 | 69 | 99 | 257 |
| Female infertility | D007247 | EFO_0008560 | N97 | 12 | 6 | 7 | 8 | 31 | 60 |
| Contraception | D003267 | — | — | 8 | 9 | 18 | 15 | 5 | 54 |
| Polycystic ovary syndrome | D011085 | EFO_0000660 | E28.2 | 3 | 3 | 7 | 7 | 28 | 47 |
| Syndrome | D013577 | — | — | 3 | 6 | 7 | 6 | 23 | 44 |
| Healthy volunteers/patients | — | — | — | 33 | 1 | 4 | 1 | 4 | 42 |
| Fertilization in vitro | D005307 | — | — | 1 | 3 | 3 | 12 | 10 | 28 |
| Ovulation induction | D010062 | — | — | 3 | 7 | 5 | 4 | 6 | 24 |
| Primary ovarian insufficiency | D016649 | EFO_0004266 | E28.3 | 5 | 4 | 2 | 1 | 11 | 20 |
| Breast neoplasms | D001943 | EFO_0003869 | C50 | 4 | 4 | 2 | 1 | 8 | 17 |
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Endometriosis | D004715 | EFO_0001065 | N80 | 2 | 1 | 2 | — | 13 | 17 |
| Pregnancy | D011247 | EFO_0002950 | Z33.1 | — | — | 1 | — | 10 | 11 |
| Neoplasms | D009369 | — | C80 | 5 | 1 | 1 | — | 2 | 8 |
| Lymphoma | D008223 | — | C85.9 | 3 | 4 | 1 | — | 2 | 8 |
| Thyroid diseases | D013959 | — | E00-E07 | 1 | 4 | 2 | — | — | 7 |
| Pituitary diseases | D010900 | — | E23.7 | — | 1 | 3 | — | 3 | 7 |
| Premenstrual syndrome | D011293 | — | N94.3 | — | 2 | 4 | — | 1 | 7 |
| Thyroid neoplasms | D013964 | EFO_0003841 | — | — | 4 | 2 | — | — | 6 |
| Male infertility | D007248 | EFO_0004248 | N46 | — | 1 | 1 | — | 4 | 5 |
| Prostatic neoplasms | D011471 | — | C61 | 2 | 1 | 1 | — | 1 | 4 |
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Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Ovarian reserve | D065851 | EFO_0004770 | — | — | 1 | — | — | 5 | 6 |
| Metrorrhagia | D008796 | — | N92.1 | — | 3 | — | — | 1 | 4 |
| Papillary thyroid cancer | D000077273 | — | — | — | 3 | — | — | — | 3 |
| Follicular adenocarcinoma | D018263 | — | — | — | 3 | — | — | — | 3 |
| Leiomyoma | D007889 | — | D25 | 1 | 1 | — | — | 2 | 3 |
| Carcinoma | D002277 | — | C80.0 | 1 | 3 | — | — | — | 3 |
| Hemostasis | D006487 | — | — | — | 1 | — | — | 1 | 2 |
| Non-hodgkin lymphoma | D008228 | — | C85.9 | — | 2 | — | — | — | 2 |
| Ovarian diseases | D010049 | — | — | — | 1 | — | — | 1 | 2 |
| Hodgkin disease | D006689 | — | C81 | 1 | 2 | — | — | — | 2 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Therapeutic equivalency | D013810 | — | — | 9 | — | — | — | — | 9 |
| Pharmacokinetics | D010599 | — | — | 5 | — | — | — | — | 5 |
| Diabetes mellitus | D003920 | EFO_0000400 | E08-E13 | 1 | — | — | — | 3 | 4 |
| Drug interactions | D004347 | — | — | 4 | — | — | — | — | 4 |
| Hiv | D006678 | — | O98.7 | 1 | — | — | — | 2 | 3 |
| Type 2 diabetes mellitus | D003924 | EFO_0001360 | E11 | 3 | — | — | — | — | 3 |
| Non-alcoholic fatty liver disease | D065626 | EFO_0003095 | K75.81 | 3 | — | — | — | — | 3 |
| Fibrosis | D005355 | — | — | 2 | — | — | — | 1 | 3 |
| Cystic fibrosis | D003550 | EFO_0000390 | E84 | 2 | — | — | — | 1 | 3 |
| Overweight | D050177 | — | E66.3 | 2 | — | — | — | 1 | 3 |
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Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Menstrual cycle | D008597 | — | — | — | — | — | — | 6 | 6 |
| Covid-19 | D000086382 | — | U07.1 | — | — | — | — | 6 | 6 |
| Fertility | D005298 | — | — | — | — | — | — | 5 | 5 |
| Ovarian cysts | D010048 | — | N83.1 | — | — | — | — | 3 | 3 |
| Metabolic syndrome | D024821 | EFO_0000195 | E88.810 | — | — | — | — | 3 | 3 |
| Type 1 diabetes mellitus | D003922 | EFO_0001359 | E10 | — | — | — | — | 3 | 3 |
| Oxidative stress | D018384 | EFO_1001905 | — | — | — | — | — | 3 | 3 |
| Sclerosis | D012598 | — | — | — | — | — | — | 2 | 2 |
| In vitro oocyte maturation techniques | D059471 | — | — | — | — | — | — | 2 | 2 |
| Endocrine system diseases | D004700 | EFO_0001379 | E34.9 | — | — | — | — | 2 | 2 |
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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 | — |
| CAS-ID | 53-16-7 |
| RxCUI | — |
| ChEMBL ID | CHEMBL1405 |
| ChEBI ID | 17263 |
| PubChem CID | 5870 |
| DrugBank | DB00655 |
| UNII ID | 2DI9HA706A (ChemIDplus, GSRS) |
Target
Agency Approved
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Alternate
ESR2
ESR2
SLCO2B1
SLCO2B1
SLCO3A1
SLCO3A1
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
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Estrone
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Trends
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Safety
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352 adverse events reported
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