Mestranol

Estrogen

Key facts

Mestranol is an ofm drug in the Estrogen class catalogued in DrugCentral. It was first approved by the FDA in 1961. Its mechanism of action is classified as Estrogen Receptor Agonists. DrugCentral lists 6 molecular targets, including ESR1, SLC6A4 and SLC6A2. Recorded indications include Contraception, Endometriosis, Female hypogonadism syndrome and Menorrhagia.

• Approval status: ofm (first approved 1961 by the FDA).
• Drug class: Estrogen.
• Mechanism of action: Estrogen Receptor Agonists.
• Molecular targets: ESR1, SLC6A4, SLC6A2 and Ar (6 listed in DrugCentral).
• Indications: Contraception, Endometriosis, Female hypogonadism syndrome and Menorrhagia.
• Molecular formula: C21H26O2; molecular weight 310.44 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (4)

• Contraception
• Endometriosis
• Female hypogonadism syndrome
• Menorrhagia

Contraindications (39)

• Angina pectoris
• Benign mammary dysplasia
• Body fluid retention
• Carcinoma of female breast
• Cardiovascular event risk
• Cerebrovascular accident
• Cholestasis of pregnancy
• Deep venous thrombosis
• Depressive disorder
• Diabetes mellitus
• Disease of liver
• Disorder of coronary artery
• Disorder of gallbladder
• Endometrial carcinoma
• Estrogen receptor positive tumor
• Heart valve disorder
• Hypercholesterolemia
• Hyperglycemia
• Hyperlipidemia
• Hypertensive disorder
• Hypertensive urgency
• Hypertriglyceridemia
• Intermenstrual bleeding - irregular
• Liver function tests abnormal
• Major Surgery with Prolonged Post-Operative Immobilization
• Malignant neoplasm of liver
• Malignant tumor of cervix
• Migraine
• Myocardial infarction
• Nonspecific Abnormal Papanicolaou Smear of Cervix
• + 9 more

Mechanism & targets

• Mechanism of action (MoA): Estrogen Receptor Agonists
• Established pharmacologic class: Estrogen

Molecular targets (6)

Target	Gene	Action	Activity
Estrogen receptor	ESR1	agonist	Ki 8.28
Sodium-dependent serotonin transporter	SLC6A4	unknown	Ki 7.66
Sodium-dependent noradrenaline transporter	SLC6A2	unknown	Ki 5.86
Androgen receptor	Ar	unknown	Ki 5.15
Progesterone receptor	PGR	unknown	Ki 4.96
Cannabinoid receptor 1	CNR1	unknown	Ki 4.65

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1961-03-09	FDA	—	—

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Mestranol is on its molecule page.

• Molecular formula: C₂₁H₂₆O₂
• Molecular weight: 310.44 g/mol
• CAS number: 72-33-3
• InChIKey: IMSSROKUHAOUJS-MJCUULBUSA-N
• PubChem CID: 6291

COC1=CC2=C(C=C1)[C@H]1CC[C@@]3(C)[C@@H](CC[C@@]3(O)C#C)[C@@H]1CC2

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Mestranol used for?

DrugCentral lists the following indications for Mestranol: Contraception, Endometriosis, Female hypogonadism syndrome and Menorrhagia.

How does Mestranol work?

Mestranol is classified as Estrogen Receptor Agonists; its molecular targets in DrugCentral include ESR1 (agonist), SLC6A4, SLC6A2 and Ar.

When was Mestranol first approved?

Mestranol was first approved by the FDA in 1961.

What drug class does Mestranol belong to?

Mestranol is in the Estrogen class.

What is the chemical formula of Mestranol?

Mestranol has the molecular formula C21H26O2 and a molecular weight of 310.44 g/mol.

Sources

• DrugCentral drug card 1714 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201151 — compound record and bioactivity
• PubChem CID 6291 — chemical identifiers
• DrugBank DB01357 — drug record
• FDA UNII B2V233XGE7 — substance identity
• DailyMed: FDA labels for Mestranol — current prescribing information (label search)
• UniProt P03372 (ESR1) — target protein
• UniProt P31645 (SLC6A4) — target protein
• UniProt P23975 (SLC6A2) — target protein
• UniProt P21554 (CNR1) — target protein

How this page is built: methodology · editorial policy & corrections.