Estradiol

Highest phase reached

Approved

www.ebi.ac.uk

Drug type

Small molecule

www.ebi.ac.uk

First approval year

1975

www.ebi.ac.uk

First approval year: 1975
www.ebi.ac.uk

Listing at source: Listed

Highest phase reached: Approved
www.ebi.ac.uk

Drug type: Small molecule
www.ebi.ac.uk

Drug name: Estradiol
www.ebi.ac.uk

Molecular weight: 272.39
www.ebi.ac.uk

Structure (SMILES): C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CC[C@@H]2O
www.ebi.ac.uk

adgyn estro
Adgyn estro
alora
Alora
aquagen
Aquagen
bedol
Bedol
climara
Climara
dermestril 100
Dermestril 100
dermestril 25
Dermestril 25
dermestril 50
Dermestril 50
dermestril septem 25
Dermestril septem 25
dermestril septem 50
Dermestril septem 50
dermestril septem 75
Dermestril septem 75
divigel
Divigel
e cypionate

And 113 more, listed on the interactive page.

0 25mg drsp 0 5mg e2 bay86 4891
17 .beta.-estradiol
17 beta estradiol
17 beta oestradiol
17 β estradiol
17 β-estradiol
17-.beta.-oestradiol
17-beta estradiol
17-beta-estradiol (drug)
17-beta-oestradiol
17-ß estradiol
17-β estradiol
17.beta.-estradiol
17beta estradiol
17beta Estradiol
17beta-estradiol
17ß-estradiol
17β-estradiol
17β-estradiol 10 mcg
1mg 17 beta-estradiol
2008-2009 FluMist LAIV (Intranasal)
activella component estradiol
ACTIVELLA COMPONENT ESTRADIOL
aerodiol
Aerodiol

And 95 more, listed on the interactive page.

ATC classification codes

G03CA03

Sources for recorded values

www.ebi.ac.uk

CAS registry numbers

50-28-2

ChEMBL ID: CHEMBL135
www.ebi.ac.uk

InChIKey: VOXZDWNPVJITMN-ZBRFXRBCSA-N
www.ebi.ac.uk

PubChem compound IDs

5757

FDA ingredient codes (UNII)

4TI98Z838E

4083
24395
236859

Applicant: BAYER HLTHCARE
Approval date: 22 Dec 1994
Application number: NDA020375

Patents: 24
Designations: 1
Earliest recorded loss of exclusivity: 2 Feb 2034
First in class: No
Fast track: No
Breakthrough designation: No
Orphan designation: No
Priority review: No
Orphan exclusivity: No
Accelerated approval: No
Availability: Prescription only
Boxed warning: Yes

Pharmacology name: 17β-estradiol
Type: Metabolite
Drug name stem: estr-
Approval recorded by Guide to Pharmacology: Yes

Administration routes

Oral
topical

Action
Activator
Action type
ACTIVATOR
Target
KCa1.1
Gene symbol
KCNMA1
Protein identifier
Q12791
Median affinity
5.6
Affinity units
pEC50
Action
Agonist
Action type
Agonist
Target
Pregnane X receptor
Gene symbol
NR1I2
Protein identifier
O75469
Action
Agonist
Action type
Agonist
Target
Estrogen receptor-α
Gene symbol
ESR1
Protein identifier
P03372
Median affinity
9.82
Affinity units
pKi
Primary target
Yes
Action
Agonist
Action type
Agonist
Target
Estrogen receptor-β
Gene symbol
ESR2
Protein identifier
Q92731
Median affinity
9.34
Affinity units
pKi
Mechanism
Estrogen receptor alpha agonist
Action type
Agonist
Target
Estrogen receptor
Protein identifier
P03372
Action
Full agonist
Action type
FULL_AGONIST
Target
GPER
Gene symbol
GPER1
Protein identifier
Q99527
Affinity units
pKi
Action
Inhibition
Action type
Inhibitor
Target
Proton-coupled Amino acid Transporter 1
Gene symbol
SLC36A1
Protein identifier
Q7Z2H8
Affinity units
pIC50

Open Targets mechanisms

Mechanism
Estrogen receptor alpha agonist
Action type
Agonist
Target
Estrogen receptor

Action type
ACTIVATOR
Gene symbol
KCNMA1
Protein identifier
Q12791
Organism
Homo sapiens
Target development level
Clinical
Action type
Agonist
Gene symbol
ESR1
Protein identifier
P03372
Organism
Homo sapiens
Target development level
Clinical

Condition
HIV Infections
Highest recorded phase
2
Condition identifier
EFO:0000180
Subject identifier
D015658
Condition
Breast Neoplasms
Highest recorded phase
4
Condition identifier
EFO:0000305
Subject identifier
D001943
Condition
Diabetes Mellitus
Highest recorded phase
1
Condition identifier
EFO:0000400
Subject identifier
D003920
Condition
Infertility
Highest recorded phase
3
Condition identifier
EFO:0000545
Subject identifier
D007246
Condition
Polycystic Ovary Syndrome
Highest recorded phase
1
Condition identifier
EFO:0000660
Subject identifier
D011085
Condition
HIV Infections
Highest recorded phase
2
Condition identifier
EFO:0000764
Subject identifier
D015658
Condition
Endometriosis
Highest recorded phase
3
Condition identifier
EFO:0001065
Subject identifier
D004715
Condition
Obesity
Highest recorded phase
3
Condition identifier
EFO:0001073
Subject identifier
D009765
Condition
Stress Disorders, Post-Traumatic
Highest recorded phase
3
Condition identifier
EFO:0001358
Subject identifier
D013313
Condition
Coronary Disease
Highest recorded phase
3
Condition identifier
EFO:0001645
Subject identifier
D003327
Condition
Prostatic Neoplasms
Highest recorded phase
2
Condition identifier
EFO:0001663
Subject identifier
D011471
Condition
Urinary Tract Infections
Highest recorded phase
2
Condition identifier
EFO:0003103
Subject identifier
D014552
Condition
Heart Diseases
Highest recorded phase
3
Condition identifier
EFO:0003777
Subject identifier
D006331
Condition
Pain
Highest recorded phase
3
Condition identifier
EFO:0003843
Subject identifier
D010146
Condition
Osteoporosis, Postmenopausal
Highest recorded phase
4
Condition identifier
EFO:0003854
Subject identifier
D015663
Condition
Breast Neoplasms
Highest recorded phase
4
Condition identifier
EFO:0003869
Subject identifier
D001943
Condition
Osteoporosis
Highest recorded phase
4
Condition identifier
EFO:0003882
Subject identifier
D010024
Condition
Atherosclerosis
Highest recorded phase
2
Condition identifier
EFO:0003914
Subject identifier
D050197
Condition
Carcinoid Tumor
Highest recorded phase
2
Condition identifier
EFO:0004243
Subject identifier
D002276
Condition
Primary Ovarian Insufficiency
Highest recorded phase
4
Condition identifier
EFO:0004266
Subject identifier
D016649
Condition
Sexual Dysfunction, Physiological
Highest recorded phase
3
Condition identifier
EFO:0004714
Subject identifier
D012735
Condition
Bulimia Nervosa
Highest recorded phase
2
Condition identifier
EFO:0005204
Subject identifier
D052018
Condition
Psychotic Disorders
Highest recorded phase
2
Condition identifier
EFO:0005411
Subject identifier
D011618
Condition
Triple Negative Breast Neoplasms
Highest recorded phase
2
Condition identifier
EFO:0005537
Subject identifier
D064726
Condition
Depression, Postpartum
Highest recorded phase
2
Condition identifier
EFO:0007453
Subject identifier
D019052

And 30 more, listed on the interactive page.

Condition identifier
EFO_0000180
Highest recorded phase
2
Condition identifier
EFO_0000400
Highest recorded phase
1
Condition identifier
EFO_0000545
Highest recorded phase
3
Condition identifier
EFO_0000660
Highest recorded phase
1
Condition identifier
EFO_0000764
Highest recorded phase
1
Condition identifier
EFO_0001065
Highest recorded phase
3
Condition identifier
EFO_0001073
Highest recorded phase
3
Condition identifier
EFO_0001358
Highest recorded phase
3
Condition identifier
EFO_0001663
Highest recorded phase
2
Condition identifier
EFO_0002950
Highest recorded phase
3
Condition identifier
EFO_0003103
Highest recorded phase
2
Condition identifier
EFO_0003854
Condition identifier
EFO_0003869
Highest recorded phase
2
Condition identifier
EFO_0003882
Condition identifier
EFO_0003914
Condition identifier
EFO_0004243
Highest recorded phase
2
Condition identifier
EFO_0004266
Condition identifier
EFO_0004320
Highest recorded phase
2
Condition identifier
EFO_0004517
Condition identifier
EFO_0004714
Highest recorded phase
2
Condition identifier
EFO_0005204
Highest recorded phase
2
Condition identifier
EFO_0005411
Highest recorded phase
3
Condition identifier
EFO_0005422
Condition identifier
EFO_0005940
Highest recorded phase
2
Condition identifier
EFO_0007453
Highest recorded phase
2

And 102 more, listed on the interactive page.

Warning
Black Box Warning
Effect
carcinogenicity
Warning
Black Box Warning
Effect
cardiotoxicity
Warning
Black Box Warning
Effect
neurotoxicity
Warning
Black Box Warning
Effect
respiratory toxicity
Warning
Black Box Warning
Effect
vascular toxicity

Warning
Black Box Warning
Effect
carcinogenicity
Country
United States
Warning
Black Box Warning
Effect
cardiotoxicity
Country
United States
Warning
Black Box Warning
Effect
neurotoxicity
Country
United States
Warning
Black Box Warning
Effect
respiratory toxicity
Country
United States
Warning
Black Box Warning
Effect
vascular toxicity
Country
United States

Event
abnormal withdrawal bleeding
Reports
70
Reporting signal score
335.846
Event
abortion induced
Reports
97
Reporting signal score
135.415
Event
application site burn
Reports
42
Reporting signal score
123.921
Event
application site erythema
Reports
216
Reporting signal score
545.29
Event
application site irritation
Reports
139
Reporting signal score
410.474
Event
application site pain
Reports
76
Reporting signal score
145.748
Event
application site pruritus
Reports
208
Reporting signal score
585.669
Event
application site rash
Reports
302
Reporting signal score
1,045.28
Event
application site reaction
Reports
82
Reporting signal score
233.59
Event
application site vesicles
Reports
56
Reporting signal score
132.459
Event
blood oestrogen decreased
Reports
42
Reporting signal score
165.86
Event
breast cancer
Reports
153
Reporting signal score
152.659
Event
breast tenderness
Reports
83
Reporting signal score
205.777
Event
deep vein thrombosis
Reports
568
Reporting signal score
797.316
Event
device adhesion issue
Reports
95
Reporting signal score
161.036
Event
dysmenorrhoea
Reports
91
Reporting signal score
210.403
Event
fungal infection
Reports
130
Reporting signal score
145.22
Event
hot flush
Reports
657
Reporting signal score
1,411.42
Event
hypercoagulation
Reports
62
Reporting signal score
172.042
Event
incorrect product administration duration
Reports
85
Reporting signal score
158.254
Event
intentional medical device removal by patient
Reports
57
Reporting signal score
199.388
Event
intracranial venous sinus thrombosis
Reports
44
Reporting signal score
132.758
Event
medical device site discomfort
Reports
62
Reporting signal score
238.921
Event
meningioma
Reports
110
Reporting signal score
298.774
Event
menopausal symptoms
Reports
83
Reporting signal score
281.436

And 22 more, listed on the interactive page.

NCT00000559
clinicaltrials.gov
NCT00160173
clinicaltrials.gov
NCT00160316
clinicaltrials.gov
NCT00184795
clinicaltrials.gov
NCT00185328
clinicaltrials.gov
NCT00195455
clinicaltrials.gov
NCT00251082
clinicaltrials.gov
NCT00302731
clinicaltrials.gov
NCT00431093
clinicaltrials.gov
NCT00455962
clinicaltrials.gov
NCT00623311
clinicaltrials.gov
NCT00727129
clinicaltrials.gov
NCT00775242
clinicaltrials.gov
NCT00864214
clinicaltrials.gov
NCT00905723
clinicaltrials.gov
NCT01174524
clinicaltrials.gov
NCT01293747
clinicaltrials.gov
NCT01477632
clinicaltrials.gov
NCT01596010
clinicaltrials.gov
NCT01705249
clinicaltrials.gov
NCT01822288
clinicaltrials.gov
NCT01942668
clinicaltrials.gov
NCT02224313
clinicaltrials.gov
NCT02467673
clinicaltrials.gov
NCT02516202
clinicaltrials.gov

And 101 more, listed on the interactive page.

Dose: 0.5mg estradiol/100mg progesterone
Route: Oral
How often: Once daily

Conditions of use

Take with food

Hydrogen bond acceptors: 2
Hydrogen bond donors: 2
Polar surface area: 40.46
Calculated partition coefficient (ALogP): 3.61
Calculated partition coefficient (XLogP): 4
Prodrug: No
Chirality: Single enantiomer
Inorganic: No
Rule-of-five violations: 0
Rotatable bonds: 0
Heavy atoms: 20
Molecular formula: C18H24O2
Monoisotopic mass: 272.177630004
Natural product: Yes

0013-1042
0037-4801
0093-3223
0093-3541
0093-5455
0169-5176
0378-3349
0378-3350
0378-3351
0378-3352
0378-3360
0378-3361
0378-4619
0378-4620
0378-4621
0378-4622
0378-4623
0378-4640
0378-4641
0378-4642
0378-4643
0378-4644
0378-8770
0430-3754
0555-0886

And 245 more, listed on the interactive page.

Recorded assays: 6,466
Active assays: 685

Confirmatory
Other
Screening
Summary

Estrogens
id.nlm.nih.gov

These details could not be displayed.

Related records

Trials (676)

"Effect of Central Insulin Administration on Whole-body Insulin Sensitivity in Women"
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A Clinical Study to Assess the Safety of a New Influenza Vaccine
A Clinical Study to Evaluate the Safety and Efficacy of Elagolix in Participants With Moderate to Severe Endometriosis-Associated Pain
A Comparison of Beclomethasone Aqueous Spray and Aerosol Delivery Systems in Nasal Polyps
A Comparison of Estradiol Vaginal Cream to Estrace® Cream in 350 Postmenopausal Females With Atrophic Vaginitis
A Comparison of Side Effects in Hypogonadal Men Treated With Natesto Versus Testosterone Injections
A Definitive Estrogen Patch Study (ADEPT)
A Dose-Finding Study to Evaluate Ovarian Function and Vaginal Bleeding in Next Generation Rings (P06109/MK-8175A/MK-8342B-012)
A Human Controlled Infection Study with Neisseria Lactamica in Malian Adults
A Non-randomised, Non-inferiority Comparative Study of Oral Actiskenan (Morphine Sulfate) Versus Intranasal Sufentanil in the Early Management of Severe Acute Pain in Emergency Departments.
A Pharmacokinetic Evaluation of Bioidentical Compounded Estrogen Cream and Natural Progesterone
A Pharmacokinetic Study of Intravenous and Intranasal Oxytocin in Healthy Subjects
A Phase 2 Study to Evaluate Immune Responses of FluMist®
A Phase 2, Dose-finding, Cross-over Study to Evaluate the Effect of a NES/E2 Transdermal Gel Delivery on Ovulation Suppression in Normal Ovulating Women
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A Randomized Controlled Trial of Oral Naproxen and Transdermal Estradiol for Bleeding in LNG-IUC
A Randomized, Single Center Pilot Study Comparing Hyaluronic Acid to Vaginal Estrogen for Treatment of Genitourinary Syndrome of Menopause

Approved for (10)

Breast cancer
Breast carcinoma
Breast neoplasm
Hypogonadism
Osteoporosis
Postmenopausal atrophic vaginitis
Postmenopausal osteoporosis
Premature ovarian failure 1
Primary ovarian failure
Psychologic dyspareunia

In development for (39)

Alzheimer disease Phase 2
Amenorrhea Phase 3
Anorexia nervosa Phase 3
Atherosclerosis Phase 2
Blood coagulation disease Early phase 1
Bulimia nervosa Phase 2
Carcinoid tumor Phase 2
Cerebral arterial disease Early phase 1
Coronary artery disorder Phase 3
COVID-19 Phase 2
Depressive disorder Phase 2
Diabetes mellitus Phase 1
Dry eye syndrome Phase 2
Dysmenorrhea Phase 3
Endometriosis Phase 3
Heart disorder Phase 3
Hereditary breast ovarian cancer syndrome Phase 2
HIV infectious disease Phase 2
Infertility disorder Phase 3
Metabolic bone disorder Phase 3

Targets (1)

ESR1 Estrogen receptor alpha agonist

Estradiol

Development status

Names and chemistry

Brand names (138)

Other names (120)

Identifiers

RxNorm IDs (RxCUI) (3)

Regulatory information

United States

Other regulatory facts

Pharmacology

Drug classification

Administration routes

Mechanisms of action (7)

Open Targets mechanisms

DrugCentral mechanisms (2)

Investigated indications (55)

Open Targets indications (127)

Warnings (5)

Open Targets warnings (5)

Reported adverse events (47)

Trial references (126)

Dosing

Conditions of use

Chemical properties

National Drug Codes

Evidence counts

Active assay types (4)

Pharmacologic actions

Biological measurements

Related records

Trials (676)

Approved for (10)

In development for (39)

Other linked conditions (1)

Targets (1)