mestranol

Small moleculeapproved

Approved

Mar 9, 1961

Mestranol is a biologically inactive prodrug of estrogen agonist ethinylestradiol. Enovid, a combination of mestranol and noretynodrel, was first oral contraceptive approved by FDA in 1960. — NCATS

Clinical trial activity

0 trials · 0 clinical orgs · 5 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Timeline

1960s

Mar 9, 1961
G D Searle — Earliest FDA Approval
Mar 9, 1961
G D Searle — NDA Secondary Org
Mar 9, 1961
G D Searle — NDA Organization
Mar 5, 1964
Actavis — NDA Secondary Org
Aug 21, 1968
Johnson and Johnson — NDA Secondary Org

1980s

Apr 12, 1988
Heritage Pharma — Marketing Organization
Jul 1, 1988
Watson Pharmaceuticals — Marketing Organization

Indications

Approved for

Mechanism of action

Estrogen receptor alphaAGONIST
ESR1 agonist
- Estrogen receptor (ESR1) ↗

Combination products

enovi
with norethynodrel
Also known as enovid-e
ortho-novum
with norethindrone
Also known as norethin 1/50m
ovulen
with etynodiol acetate

Approval history

approvedMar 9, 1961

Chemistry & pharmacology

Loading structure…

SMILES

COC1=CC=C2[C@H]3CC[C@@]4(C)[C@@H](CC[C@@]4(O)C#C)[C@@H]3CCC2=C1

Mol. weight: 310.4299 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Single Stereoisomer
Inorganic: No
Polymer: No
Delivery: Oral
Availability: Discontinued

Oral

Yes

Parenteral

Topical

Prodrug

Sources

Also known as

33355
3-methoxyethynylestradiol
ee3-me
ee3-me
ethynylestradiol methyl ether
inostral
menophase
mestranol
mestranol
mestranol
mestranol
mestranol
mestranol
mestranol
mestranol
norquen

Organizations

Marketing (7)

Organization	Org type	Relationship	Date
Actavis	For profit	NDA2	Mar 5, 1964
G D Searle	For profit	NDA2	Mar 9, 1961
G D Searle	For profit	NDA	Mar 9, 1961
Heritage Pharma	For profit	MKTG	Apr 12, 1988
Johnson and Johnson	For profit	NDA2	Aug 21, 1968
Johnson and Johnson	For profit	SYN	May 21, 1962
Watson Pharmaceuticals	For profit	MKTG	Jul 1, 1988