U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C23H30O4
Molecular Weight 370.4819
Optical Activity UNSPECIFIED
Defined Stereocenters 6 / 6
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SEGESTERONE ACETATE

SMILES

[H][C@@]12CC(=C)[C@](OC(C)=O)(C(C)=O)[C@@]1(C)CC[C@]3([H])[C@@]4([H])CCC(=O)C=C4CC[C@@]23[H]

InChI

InChIKey=CKFBRGLGTWAVLG-GOMYTPFNSA-N
InChI=1S/C23H30O4/c1-13-11-21-20-7-5-16-12-17(26)6-8-18(16)19(20)9-10-22(21,4)23(13,14(2)24)27-15(3)25/h12,18-21H,1,5-11H2,2-4H3/t18-,19+,20+,21-,22-,23-/m0/s1

HIDE SMILES / InChI
Molecular Formula C23H30O4
Molecular Weight 370.4819
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 6 / 6
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

Segesterone acetate (elcometrine), a progestin, is sold in combination with ethinyl estradiol under the brand name Annovera. Annovera is indicated for use by females of reproductive potential to prevent pregnancy. Segesterone acetate acts as an agonist of the progesterone receptor and it doesn’t possess estrogenic, androgenic, antiandrogenic, or antimineralocorticoid activity.

Originator

Approval Year

2018
436
Targets

Targets

Primary TargetPharmacologyConditionPotency
Progesterone receptor
61
Target ID: P06401
Gene ID: 5241.0
Gene Symbol: PGR
Target Organism: Homo sapiens (Human)
Agonist
2678
 56.0 nM [EC50]
Agonist
2678
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase II
1132
Unknown

Approved Use

Unknown
Preventing
Phase III
656
ELMETRIN

Approved Use

Unknown
Preventing
Approved
8429
ANNOVERA

Approved Use

is indicated for use by females of reproductive potential to prevent pregnancy

Launch Date

2018
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
294 pg/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
0.15 mg 1 times / day steady-state, vaginal
dose: 0.15 mg
route of administration: Vaginal
experiment type: STEADY-STATE
co-administered: ETHINYL ESTRADIOL
ETHINYL ESTRADIOL
 SEGESTERONE ACETATE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
1147 pg/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
0.15 mg 1 times / day steady-state, vaginal
dose: 0.15 mg
route of administration: Vaginal
experiment type: STEADY-STATE
co-administered: ETHINYL ESTRADIOL
ETHINYL ESTRADIOL
 SEGESTERONE ACETATE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
942.9 pg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29409834/
200 μg 1 times / day steady-state, vaginal
dose: 200 μg
route of administration: Vaginal
experiment type: STEADY-STATE
co-administered: ESTRADIOL
ESTRADIOL
 SEGESTERONE ACETATE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
3.9 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
0.15 mg 1 times / day steady-state, vaginal
dose: 0.15 mg
route of administration: Vaginal
experiment type: STEADY-STATE
co-administered: ETHINYL ESTRADIOL
ETHINYL ESTRADIOL
 SEGESTERONE ACETATE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
15 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
0.15 mg 1 times / day steady-state, vaginal
dose: 0.15 mg
route of administration: Vaginal
experiment type: STEADY-STATE
co-administered: ETHINYL ESTRADIOL
ETHINYL ESTRADIOL
 SEGESTERONE ACETATE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
38685.7 pg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29409834/
200 μg 1 times / day steady-state, vaginal
dose: 200 μg
route of administration: Vaginal
experiment type: STEADY-STATE
co-administered: ESTRADIOL
ESTRADIOL
 SEGESTERONE ACETATE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
4.5 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
0.15 mg 1 times / day steady-state, vaginal
dose: 0.15 mg
route of administration: Vaginal
experiment type: STEADY-STATE
co-administered: ETHINYL ESTRADIOL
ETHINYL ESTRADIOL
 SEGESTERONE ACETATE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
4.5 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
0.15 mg 1 times / day steady-state, vaginal
dose: 0.15 mg
route of administration: Vaginal
experiment type: STEADY-STATE
co-administered: ETHINYL ESTRADIOL
ETHINYL ESTRADIOL
 SEGESTERONE ACETATE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
5%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
0.15 mg 1 times / day steady-state, vaginal
dose: 0.15 mg
route of administration: Vaginal
experiment type: STEADY-STATE
co-administered: ETHINYL ESTRADIOL
ETHINYL ESTRADIOL
 SEGESTERONE ACETATE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
5%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
0.15 mg 1 times / day steady-state, vaginal
dose: 0.15 mg
route of administration: Vaginal
experiment type: STEADY-STATE
co-administered: ETHINYL ESTRADIOL
ETHINYL ESTRADIOL
 SEGESTERONE ACETATE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Disc. AE: Menometrorrhagia, Migraine headache...
Other AEs: Migraine headache, Nausea and vomiting...
AEs leading to
discontinuation/dose reduction:
Menometrorrhagia (1.7%)
Migraine headache (1.3%)
Vulvovaginal mycotic infection (1.3%)
Nausea and vomiting (1.2%)
Uterine myoma expulsion (1.4%)
Other AEs:
Migraine headache (38.6%)
Nausea and vomiting (25%)
Vulvovaginal mycotic infection (14.5%)
Abdominal pain lower (13.3%)
Dysmenorrhea (12.5%)
Vaginal discharge (11.8%)
Genitourinary tract infection (10%)
Breast discomfort (9.5%)
Disorder menstrual (7.5%)
Diarrhea (7.2%)
Pruritus genital (5.5%)
Thrombosis NOS (>= 2 patients)
Psychiatric disorder NOS (>= 2 patients)
Drug hypersensitivity (>= 2 patients)
Abortions spontaneous (>= 2 patients)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
AEs

AEs

AESignificanceDosePopulation
Nausea and vomiting 1.2%
Disc. AE
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Migraine headache 1.3%
Disc. AE
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Vulvovaginal mycotic infection 1.3%
Disc. AE
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Uterine myoma expulsion 1.4%
Disc. AE
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Menometrorrhagia 1.7%
Disc. AE
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Genitourinary tract infection 10%
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Vaginal discharge 11.8%
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Dysmenorrhea 12.5%
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Abdominal pain lower 13.3%
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Vulvovaginal mycotic infection 14.5%
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Nausea and vomiting 25%
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Migraine headache 38.6%
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Pruritus genital 5.5%
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Diarrhea 7.2%
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Disorder menstrual 7.5%
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Breast discomfort 9.5%
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Abortions spontaneous >= 2 patients
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Drug hypersensitivity >= 2 patients
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Psychiatric disorder NOS >= 2 patients
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Thrombosis NOS >= 2 patients
0.15 mg 1 times / day multiple, vaginal
Recommended
Dose: 0.15 mg, 1 times / day
Route: vaginal
Route: multiple
Dose: 0.15 mg, 1 times / day
Co-administed with::
ethinyl estradiol(0.013 mg/day)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
healthy, 18 - 40 years
n = 2308
Health Status: healthy
Age Group: 18 - 40 years
Sex: F
Population Size: 2308
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf
Page: 13
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737

inhibitor
1587

inducer
781
inhibitor
1767

inducer
389
inhibitor
1852

inducer
97
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2A6
707

CYP2B6
810

CYP2C8
911

CYP2C19
1478

CYP2E1
882
CYP1A2
701

CYP2B6
547

CYP2C19
293

CYP3A5
76
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1692
 unlikely
CYP1A2
1692
 unlikely
CYP2A6
739
 unlikely
CYP2B6
1001
 unlikely
CYP2B6
1001
 unlikely
CYP2C19
1553
 unlikely
CYP2C19
1553
 unlikely
CYP2C8
965
 unlikely
CYP2C9
1819
 unlikely
CYP2C9
1819
 unlikely
CYP2D6
1891
 unlikely
CYP2D6
1891
 unlikely
CYP2E1
970
 unlikely
CYP3A4
1925
 unlikely
CYP3A4
1925
 unlikely
CYP3A5
130
 unlikely
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1737
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEMBL
CHEMBL2107778
ChemIDplus
7690086
https://chem.nlm.nih.gov/chemidplus/id/0007690086
Compound Cloud
11823650
DrugBank
DB14584
https://www.drugbank.ca/drugs/DB14584
EPA DSSTox
DTXSID00998190
https://comptox.epa.gov/dashboard/DTXSID00998190
KEGG
D10987
http://www.genome.jp/dbget-bin/www_bget?dr:D10987
SureChEMBL
SCHEMBL7053392
https://www.surechembl.org/chemical/SCHEMBL7053392
Wikidata
Q24882947
ZINC
ZINC000033964021
http://zinc15.docking.org/substances/ZINC000033964021
PubMed

PubMed

TitleDatePubMed
Nestorone: a progestin with a unique pharmacological profile.
2000 Oct-Nov
Comparison of the impact of vaginal and oral administration of combined hormonal contraceptives on hepatic proteins sensitive to estrogen.
2007 Jun
Patents

Patents

US 3262950
2

Sample Use Guides

In Vivo Use Guide
Elcometrine is delivered within a single subdermal capsule of medical grade polydimethylsiloxane, containing 50 mg of elcometrine. In clinical trials, administration by a vaginal ring was investigated (150 mg of Nestorone and 15 mg of ethinyl estradiol). The development of transdermal gel containing elcometrine is also reported.
Route of Administration: Other
In Vitro Use Guide
Female Sprague–Dawley rats were ovariectomized and 1 week later, injected daily for 3 days with 1 mg 17 b-estradiol (E2) to induce synthesis of PR. The animals were killed on day 4, uteri were collected over dry ice and homogenized. Aliquot of cytosol were incubated overnight at 4°C in glass tubes with [3H]promegestone with or without cold nestorone at different concentrations. The bound and free radioactivity was separated by the dextran-charcoal method.
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:16:26 GMT 2023
Edited
by admin
on Fri Dec 15 15:16:26 GMT 2023
Record UNII
9AMX4Q13CC
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SEGESTERONE ACETATE
USAN  
USAN  
Official Name English
16-METHYLENE-17.ALPHA.-ACETOXY-19-NOR-PREGN-4-ENE-3,20-DIONE
Common Name English
19-NORPREGN-4-ENE-3,20-DIONE, 17-(ACETYLOXY)-16-METHYLENE-
Common Name English
ANNOVERA COMPONENT SEGESTERONE ACETATE
Brand Name English
Segesterone acetate [WHO-DD]
Common Name English
ELCOMETRINE [MI]
Common Name English
17-(ACETYOXY)-16- METHYLENE -19-NONPREGN-4-ENE-3,20-DIONE
Common Name English
ST-1435
Code English
NESTORONE
Brand Name English
SEGESTERONE ACETATE [ORANGE BOOK]
Common Name English
SEGESTERONE ACETATE [USAN]
Common Name English
SEGESTERONE ACETATE COMPONENT OF ANNOVERA
Brand Name English
ELCOMETRINE
MI  
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C776
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
Code System Code Type Description
NCI_THESAURUS
C152316
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
PRIMARY
DRUG BANK
DB14583
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
PRIMARY
USAN
DE-09
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
PRIMARY
WIKIPEDIA
Segesterone acetate
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
PRIMARY
FDA UNII
9AMX4Q13CC
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
PRIMARY
ChEMBL
CHEMBL3707377
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
PRIMARY
MERCK INDEX
m4856
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
PRIMARY Merck Index
RXCUI
2055977
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
PRIMARY
CAS
7759-35-5
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
PRIMARY
DAILYMED
9AMX4Q13CC
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
PRIMARY
EPA CompTox
DTXSID70998804
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
PRIMARY
PUBCHEM
108059
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
PRIMARY
DRUG CENTRAL
3175
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
PRIMARY
SMS_ID
300000034700
Created by admin on Fri Dec 15 15:16:26 GMT 2023 , Edited by admin on Fri Dec 15 15:16:26 GMT 2023
PRIMARY
Related Record Type Details
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
GLUCOCORTICOID RECEPTOR
TARGET -> AGONIST
EC50
PROGESTERONE RECEPTOR
TARGET -> AGONIST
EC50
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
MAJOR
Structure of GESTADIENOL ACETATE
TARGET->ANALOGUE
Related Record Type Details
Structure of 5.ALPHA.-DIHYDROSEGESTERONE ACETATE
METABOLITE -> PARENT
Structure of ((8R,9R,10S,13S,14S,17R)-17-(1-HYDROXYETHYL)-13-METHYL-16-METHYLENE-3-OXO-2,4,5,6,7,8,9,10,11,12,14,15-DODECAHYDRO-1H-CYCLOPENTA(A)PHENANTHREN-17-YL) ACETATE
METABOLITE INACTIVE -> PARENT
Structure of 3ALPHA, 5ALPHA-TETRAHYDROSEGESTERONE ACETATE
METABOLITE INACTIVE -> PARENT
Structure of 4, 5-DIHYDRO-17.ALPHA.-DEACETYLSEGESTERONE ACETATE
METABOLITE -> PARENT
Structure of 3BETA, 5ALPHA-TETRAHYDROSEGESTERONE ACETATE
METABOLITE -> PARENT
Related Record Type Details
Structure of SEGESTERONE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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