estrone

Small moleculeapproved

Approved

Jun 12, 1941

Estrone, one of the major mammalian estrogens, is an aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone. It is produced in vivo from androstenedione or from testosterone via estradiol. It is produced primarily in the ovaries, placenta, and in peripheral tissues (especially adipose tissue) through conversion of adrostenedione. Estrone may be further metabolized to 16-alpha-hydroxyestrone, which may be reduced to estriol by estradiol dehydrogenase. It’s used as hameopatic in management of premenopausal and postmenopausal symptoms. In 1929, Butenandt isolated estrone from the urine of pregnant women. Estrone is known to be a carcinogen for human females as well as a cause of breast tenderness or pain, nausea, headache, hypertension, and leg cramps in the context of non-endogenous exposure. In men, estrone has been known to cause anorexia, nausea, vomiting, and erectile dysfunction. Estrone is relevant to health and disease states because of its conversion to estrone sulfate, a long-lived derivative. Estrone sulfate acts as a reservoir that can be converted as needed to the more active estradiol. — NCATS

Clinical trial activity

3 trials · 3 clinical orgs · 5 marketing orgs

Phase 1
2
Phase 2
0
Phase 3
0
Phase 4
0

Earliest trial started Jun 1, 2005 (NCT00239148)

Timeline

1920s

  1. Jul 1, 1929

    Evidence of US Marketing

1940s

  1. Jun 12, 1941

    Parke-Davis — Earliest FDA Approval

  2. Jun 12, 1941

    Parke-Davis — NDA Secondary Org

  3. Jun 12, 1941

    Parke-Davis — NDA Organization

1970s

  1. Feb 21, 1979

    Teva — Marketing Organization

  2. Feb 21, 1979

    Dr. Reddy's Laboratories — Marketing Organization

2000s

  1. Jan 1, 2005

    Earliest Phase 1 Sponsor(trial)

Indications

Mechanism of action

Approval history

  • approvedJun 12, 1941
  • approvedJul 1, 1929

Chemistry & pharmacology

Loading structure…

SMILES

Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2
Mol. weight
454.91 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Discontinued

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • 3-hydroxy-1,3,5(10)-estratrien-17-one
  • 3-hydroxy-1,3,5(10)-estratrien-17-one
  • e1
  • e1
  • estrogenic substance
  • estrogenic substance
  • estron
  • estrona
  • estrona
  • estrone
  • estrone
  • estrone
  • estrone
  • estrone
  • estrone
  • estrone
  • estrone
  • estrone
  • estrone
  • estronum
  • estronum
  • estrugenone
  • follicular hormone
  • follicular hormone
  • folliculin
  • folliculin
  • oestrin
  • oestrone
  • oestrone
  • oestrone
  • oestrone
  • theelin
  • theelin
  • theelin
  • thelin
  • thelin
  • thelin
  • thelin
  • thelin

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT00744211N/AJul 31, 2008Department of Veteran Affairs, Medical University of South Carolina
NCT00239187Phase 1Sep 1, 2005Transition Therapeutics
NCT00239148Phase 1Jun 1, 2005Transition Therapeutics
Showing 3 of 3 trials
Page 1 / 1

Organizations

Research & Development (3)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Transition TherapeuticsFor profit2212005
Department of Veteran AffairsGovernment1112008
Medical University of South CarolinaAcademic/Hospital1012008
3 organizations
Page 1 / 1

Marketing (6)

OrganizationOrg typeRelationshipDate
American Home ProductsFor profitMKTG
Dr. Reddy's LaboratoriesFor profitMKTGFeb 21, 1979
Parke-DavisFor profitNDA2Jun 12, 1941
Parke-DavisFor profitNDAJun 12, 1941
TevaFor profitMKTGFeb 21, 1979
Watson PharmaceuticalsFor profitMKTG