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Conjugated estrogens

Generic Name
Conjugated estrogens
Brand Names
Congest, Duavee, Duavive, Premarin, Premphase 28 Day, Prempro 0.625/2.5 28 Day
Drug Type
Small Molecule
CAS Number
12126-59-9
Unique Ingredient Identifier
IU5QR144QX

Overview

The conjugated estrogens are noncrystalline mixtures of purified female sex hormones obtained either by its isolation from the urine of pregnant mares or by synthetic generation from vegetal material. Both of these products are later conjugated to natrium sulfate by ester bonds in order to make them more water soluble. The conjugated estrogen product contains a mix of estrogen from which about 50% is represented by estrone sulfate followed by 25% of equilin sulfate, 15% of 17-alpha-dehydroequilenin sulfate, 3% of equilenin sulfate, 5% of 17-alpha and 17-beta-dihydroequilenin sulfate, 2% of 17-alpha-estradiolsulfate and 3% of 17-beta-estradiolsulfate. It also presents a large number of unidentified molecules with weak estrogenic activity as well as non-human molecules when it is obtained from pregnant mares urine. The conjugated estrogen mixture was approved for marketing in US in 1942 based on the efficacy against certain conditions. However, until 1986 official clinical trials were performed and this product was determined to be effective for the treatment of osteoporosis. The currently approved product of conjugated estrogens was developed by Wyeth Ayerst and FDA approved in 2003.

Background

The conjugated estrogens are noncrystalline mixtures of purified female sex hormones obtained either by its isolation from the urine of pregnant mares or by synthetic generation from vegetal material. Both of these products are later conjugated to natrium sulfate by ester bonds in order to make them more water soluble. The conjugated estrogen product contains a mix of estrogen from which about 50% is represented by estrone sulfate followed by 25% of equilin sulfate, 15% of 17-alpha-dehydroequilenin sulfate, 3% of equilenin sulfate, 5% of 17-alpha and 17-beta-dihydroequilenin sulfate, 2% of 17-alpha-estradiolsulfate and 3% of 17-beta-estradiolsulfate. It also presents a large number of unidentified molecules with weak estrogenic activity as well as non-human molecules when it is obtained from pregnant mares urine. The conjugated estrogen mixture was approved for marketing in US in 1942 based on the efficacy against certain conditions. However, until 1986 official clinical trials were performed and this product was determined to be effective for the treatment of osteoporosis. The currently approved product of conjugated estrogens was developed by Wyeth Ayerst and FDA approved in 2003.

Indication

The conjugated estrogens are indicated for several different conditions including:

Associated Conditions

  • Abnormal Uterine Bleeding
  • Atrophic Vaginitis
  • Atrophy of vulva
  • Kraurosis Vulvae
  • Menopause
  • Metastatic Breast Cancer
  • Moderate to Severe Vasomotor Symptoms
  • Osteoporosis
  • Androgen-dependent tumor Advanced Prostate Carcinoma
  • Hypoestrogenism
  • Moderate Dyspareunia
  • Moderate Vulvar and Vaginal Atrophy
  • Severe Dyspareunia
  • Severe Vulvar and Vaginal Atrophy

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2020/07/20
Phase 1
Recruiting
2020/05/07
Early Phase 1
Terminated
Carol Fabian, MD
2019/06/25
Phase 4
Completed
2019/06/10
Phase 3
UNKNOWN
2017/08/30
N/A
Completed
2017/01/11
Phase 4
Terminated
2016/08/09
Phase 4
Withdrawn
2016/04/06
Phase 2
Completed
2015/05/01
Phase 4
Completed
2014/08/11
Phase 4
Terminated
Medstar Health Research Institute

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Wyeth Pharmaceuticals LLC, a subsidiary of Pfizer Inc.
0046-1106
ORAL
0.45 mg in 1 1
5/6/2025
Physicians Total Care, Inc.
54868-3799
ORAL
0.625 mg in 1 1
11/1/2012
Wyeth Pharmaceuticals LLC, a subsidiary of Pfizer Inc.
0046-1107
ORAL
0.625 mg in 1 1
5/6/2025
Wyeth Pharmaceuticals LLC, a subsidiary of Pfizer Inc.
0046-1100
ORAL
0.3 mg in 1 1
9/20/2018
Aphena Pharma Solutions - Tennessee, Inc.
43353-688
ORAL
0.625 mg in 1 1
7/18/2012
State of Florida DOH Central Pharmacy
53808-0770
ORAL
0.625 mg in 1 1
5/27/2010
U.S. Pharmaceuticals
63539-122
ORAL
0.45 mg in 1 1
7/1/2022
Wyeth Pharmaceuticals LLC, a subsidiary of Pfizer Inc.
0046-1101
ORAL
0.45 mg in 1 1
9/20/2018
A-S Medication Solutions
50090-0573
ORAL
0.625 mg in 1 1
5/15/2019
Physicians Total Care, Inc.
54868-5540
ORAL
0.625 mg in 1 1
11/1/2012

EMA Drug Approvals

Approved Product
Authorization Holder
Status
Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
No HSA approvals found for this drug.

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
Conjugated Estrogens Tablets
国药准字H20090165
化学药品
片剂
4/2/2024
Conjugated Estrogens Tablets
国药准字H20090170
化学药品
片剂
4/2/2024
Conjugated Estrogens Tablets
国药准字H20090172
化学药品
片剂
4/2/2024
Conjugated Estrogens Cream
国药准字H20051718
化学药品
乳膏剂
8/21/2020

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
No PPB approvals found for this drug.
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