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Overview
| Trade Names: | Aquacrine; Crinovaryl; Cristallovar; Crystogen; Destrone; Disynformon; Endofolliculina; Esterone; Estrin; Estrogenic Substance; Estrol; Estron; Estrona; Estrona [INN-Spanish]; Estrona [Spanish]; Estrone [Usan:Inn]; Estrone-A; Estronum [INN-Latin]; Estrovarin; Estrugenone; Estrusol; Femestrone Inj.; Femestrone Injection; Femidyn; Fermidyn; Folikrin; Folipex; Folisan; Follestrine; Follestrol; Follicular Hormone; Folliculin; Folliculine; Folliculine Benzoate; Follicunodis; Follidrin; GSS 33; Glandubolin; Hiestrone; Hormestrin; Hormofollin; Hormovarine; Kestrone; Ketodestrin; Ketohydroxy-Estratriene; Ketohydroxyestrin; Ketohydroxyoestrin; Ketophydroxyestrin; Kolpon; Menagen; Menformon; Menformon A; Mestronaq; OVEX; Oestrin; Oestroform; Oestrone; Oestrone [Steroidal Oestrogens]; Oestronum; Oestroperos; Ovifollin; Penncap M; Perlatan; Sinafid M-48; Solliculin; Theelin; Thelestrin; Thelykinin; Thynestron; Tokokin; Unden; Wynestron; Wynestronpencap M |
|---|---|
| Brand Mixtures: | Cimicifuga Plex (Caulophyllum Thalictroides + Cimicifuga Racemosa + Copper + Cotton Plant + Estrone + Histamine Dihydrochloride + Hypothalamus + Magnesium Phosphate Dibasic + Pituitary Whole + Platinum + Sepia Officinalis L + Thyroid); Holis 98 (Dioscorea Vilosa + Estrone + Salvia + Saw Palmetto) |
| PharmGKB Accession Id: | PA449512 |
Description
An aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from androstenedione directly, or from testosterone via estradiol. In humans, it is produced primarily by the cyclic ovaries, placenta, and the adipose tissue of men and postmenopausal women. PubChem (source: Drug Bank)
Indication
For management of Menopausal and postmenopausal disorders (source: Drug Bank)
ATC Therapeutic Categories
- G03CA:Natural and semisynthetic estrogens, plain
- G03CC:Estrogens, combinations with other drugs
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Estrogens enter the cells of responsive tissues (e.g., female organs, breasts, hypothalamus, pituitary) where they interact with a protein receptor, estrogen receptors, subsequently increasing the rate of synthesis of DNA, RNA, and some proteins. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. (source: Drug Bank)
Pharmacology
Estrone, a synthetically prepared or naturally occurring steroidal estrogen obtained from pregnant equine urine, is the primary circulating estrogen after menopause. Estrone is naturally derived from the peripheral conversion of androstenedione by an aromatase enzyme found in adipose tissues and is converted to estradiol in peripheral tissues. Estropipate is piperazine-stabilized estrone sulfate. Estrone, and estropipate are used to treat abnormalities related to gonadotropin hormone dysfunction, vasomotor symptoms, atrophic vaginitis, and vulvar atrophy associated with menopause, and for the prevention of osteoporosis due to estrogen deficiency. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic. (source: Drug Bank)
Protein Binding
>95% (source: Drug Bank)
Absorption
43% (source: Drug Bank)
Toxicity
Symptoms of overdose include nausea and vomiting. Withdrawal bleeding may occur in females. (source: Drug Bank)
Isomeric SMILES Code:
C[C@]12CC[C@@H]3c4ccc(cc4CC[C@H]3[C@@H]1CCC2=O)O (source: Drug Bank)
Curated Annotations (
)
-
rs45511401
at chr16:16080733
in
ABCC1
system: membrane vessicles from HEK cells transfected with WT and variant; FA: transport of leukotriene C4, 17beta-estradiol 17beta-(D)-glucuronide, and estrone sulfate were the same for WT and variant- Variant Name:
- G671V
- Related Drugs:
- estradiol, estrone
- Evidence:
-
PMID:11721885
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
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ABCC1 |
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Variants |
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CYP3A4 |
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Publications |
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CYP3A43 |
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Publications |
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CYP3A5 |
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Publications |
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CYP3A7 |
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Publications |
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NR1I2 |
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Publications |
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SLC22A8 |
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Publications |
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SLCO1C1 |
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Publications |
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SLCO2B1 |
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Publications |
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SLCO3A1 |
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Publications |
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SLCO4A1 |
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Publications |
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UGT1A3 |
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Publications |
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UGT1A8 |
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Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| ALB |
|
(source: Drug Bank) |
| CYP1B1 |
|
(source: Drug Bank) |
| ESR1 |
|
(source: Drug Bank) |
| SHBG |
|
(source: Drug Bank) |
| STS |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
- Anti-estrogen Pathway (Aromatase Inhibitor)
- Anti-estrogen Pathway (Estrogen metabolism)
- Anti-estrogen Pathway (Summary)
BioCarta Pathways†
- carm1 and regulation of the estrogen receptor - (BioCarta via Pathway Interaction Database)
- downregulated of mta-3 in er-negative breast tumors - (BioCarta via Pathway Interaction Database)
- estrogen responsive protein efp controls cell cycle and breast tumors growth - (BioCarta via Pathway Interaction Database)
- overview of telomerase protein component gene htert transcriptional regulation - (BioCarta via Pathway Interaction Database)
- pelp1 modulation of estrogen receptor activity - (BioCarta via Pathway Interaction Database)
Reactome Pathways†
- Cytosolic sulfonation of small molecules - (Reactome via Pathway Interaction Database)
- Endogenous sterols - (Reactome via Pathway Interaction Database)
- Estrogen biosynthesis - (Reactome via Pathway Interaction Database)
- Peptide ligand-binding receptors - (Reactome via Pathway Interaction Database)
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
|
|
anastrozole |
|
Publications |
|
|
letrozole |
|
Publications |
A list of non-curated publications that mention this drug along with other drugs is available.
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Curated Phenotype Datasets
These datasets are sorted alphabetically by title.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
Downloads
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LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.