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Description: Generally refers to the 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. In humans, it is produced primarily by the cyclic ovaries and the placenta. It is also produced by the adipose tissue of men and postmenopausal women. The 17-alpha-isomer of estradiol binds weakly to estrogen receptors (receptors, estrogen) and exhibits little estrogenic activity in estrogen-responsive tissues. Various isomers can be synthesized. [PubChem]
Drug Type: Small Molecule; Approved; Investigational
Pharmacology: Estradiol, the principal intracellular human estrogen, is substantially more active than its metabolites, estrone and estriol, at the cellular level.
Mechanism of Action: Estradiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. 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.
Indication: For the treatment of urogenital symptoms associated with post-menopausal atrophy of the vagina (such as dryness, burning, pruritus and dyspareunia) and/or the lower urinary tract (urinary urgency and dysuria).
Half Life: 36 hours
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Data Correlations | 58 studies

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Genes category icon Genes
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ESR1 100 100
9687 100 100
DEPDC6 88 88
MYBL1 85 85
DHRS3 84 84
MLPH 84 84
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Biogroups category icon Biogroups
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DNA Replication Reactome 100 100
P53 Signaling Pathway 99 99
All Peptidase Inhibitors 98 98
Cell Cycle G1 to S control Reactome 98 98
Pyrimidine Metabolism 98 98
Cell Cycle 98 98
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Individual Studies

  • Drug-Induced Renal Tubular Toxicity

    Rattus norvegicus Rattus norvegicus | RNA Expression   RNA Expression

    These data support the publication titled "A Gene Expression Signature that Predicts the Future Onset of Drug-Induced Renal Tubular Toxicity"

    Authors: Fielden MR, Eynon BP, Natsoulis G et al.

    Organization: Iconix Pharmaceuticals 325 E Middlefield…

  • Estrogen treatment of 3 breast cancer cell lines

    Homo sapiens Homo sapiens | RNA Expression   RNA Expression

    Three human ER+ breast cancer cell lines--MCF-7, T47-D, BT-474--grown with or without estradiol (E2).

    Authors: Rae J, Lippman M

    Organization: Baylor College of Medicine Biostatistics…
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Associated Researchers

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Thought leaders and organizations working on research involving Climara Pro.

View All Author iconAuthors
  • R E Szawka
  • J A Anselmo-Franci
  • Enhua Yang
  • V Ribeiro-Gouveia
  • Stina Garvin
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • Bayer
  • Assistance Publique - Hôpitaux de Paris
  • University Hospital, Toulouse
  • Hospices Civils de Lyon
  • Family Health International
View All Affiliations icon Organizations
  • 3M Drug Delivery Systems
  • Yale University School of Medicine
  • University of Southern California
  • Centre de Génétique Moléculaire et Cellulaire
  • Northwestern University

Clinical Trials | 8 trials

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