Page last updated: 2024-12-07

st 1435

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID108059
CHEMBL ID3707377
CHEBI ID135563
SCHEMBL ID1261001
MeSH IDM0093226

Synonyms (48)

Synonym
AC-6844
HY-13071
st-1435
nestorone
elcometrine
19-norpregn-4-ene-3,20-dione, 17-hydroxy-16-methylene-, acetate
16-methylene-17-alpha-acetoxy-19-nor-4-pregnene-3,20-dione
19-norpregn-4-ene-3,20-dione, 17-(acetyloxy)-16-methylene-
st 1435
17-hydroxy-16-methylene-19-norpregn-4-ene-3,20-dione acetate
16-methylene-17alpha-acetoxy-19-nor-4-pregnen-3,20-dione
7759-35-5
CHEBI:135563
nestoron
9amx4q13cc ,
segesterone acetate
unii-9amx4q13cc
segesterone acetate [usan]
CS-0411
17-(acetyoxy)-16- methylene -19-nonpregn-4-ene-3,20-dione
segesterone acetate component of annovera
annovera component segesterone acetate
segesterone acetate [who-dd]
elcometrine [mi]
segesterone acetate [orange book]
16-methylene-17.alpha.-acetoxy-19-nor-pregn-4-ene-3,20-dione
CHEMBL3707377
SCHEMBL1261001
AKOS025402243
nestorone, >=97% (hplc)
D10986
segesterone acetate (usan)
nestorone (tn)
(8r,9s,10r,13s,14s,17r)-17-acetyl-13-methyl-16-methylene-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl acetate
DB14583
BCP12737
Q1978481
NCGC00487114-02
segesterone-acetate
1-tert-butoxycarbonylamino-cyclopent-3-enecarboxylicacid
MS-25961
DTXSID70998804
E89278
EN300-19790341
(1r,3as,3br,9ar,9bs,11as)-1-acetyl-11a-methyl-2-methylidene-7-oxo-1h,2h,3h,3ah,3bh,4h,5h,7h,8h,9h,9ah,9bh,10h,11h,11ah-cyclopenta[a]phenanthren-1-yl acetate
16-methylene-17-hydroxy-19-norpregn-4-ene-3,20-dione acetate
A914499
elcometrine;nestorone;st-1435

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" The purpose of this study was to determine the pharmacokinetic parameters of ST 1435 after single oral or intravenous administration or after long-term treatment with subdermal implants in women."( Pharmacokinetics and bioavailability of ST 1435 administered by different routes.
Croxatto, HB; Heikinheimo, O; Maturana, X; Noé, G; Salvatierra, A, 1993
)
0.78
" Conventional pharmacokinetic parameters were calculated."( An initial pharmacokinetic study with a Metered Dose Transdermal Systemfor delivery of the progestogen Nestorone as a possible future contraceptive.
Fraser, IS; Humberstone, AJ; Kumar, N; Kumar, S; McCrossin, L; Shaw, D; Sitruk-Ware, R; Tsong, YY; Weisberg, E, 2007
)
0.34
" The apparent elimination half-life of NES after the last dose on Day 5 was 26."( An initial pharmacokinetic study with a Metered Dose Transdermal Systemfor delivery of the progestogen Nestorone as a possible future contraceptive.
Fraser, IS; Humberstone, AJ; Kumar, N; Kumar, S; McCrossin, L; Shaw, D; Sitruk-Ware, R; Tsong, YY; Weisberg, E, 2007
)
0.34
"This early pharmacokinetic trial of a new transdermal steroid delivery system has demonstrated the feasibility of achieving serum levels of NES sufficient to block ovulation and potentially provide effective contraception."( An initial pharmacokinetic study with a Metered Dose Transdermal Systemfor delivery of the progestogen Nestorone as a possible future contraceptive.
Fraser, IS; Humberstone, AJ; Kumar, N; Kumar, S; McCrossin, L; Shaw, D; Sitruk-Ware, R; Tsong, YY; Weisberg, E, 2007
)
0.34
" Thereafter, the concentration of drug steadily declined through 96-h postdose with a terminal elimination half-life (t(1/2)) of 15."( Single-dose pharmacokinetics of Nestorone, a potential female-contraceptive.
Bashir, M; Kumar, N; Prasad, PV; Sitruk-Ware, R, 2010
)
0.36

Compound-Compound Interactions

ExcerptReferenceRelevance
"This was an open-label, randomized, crossover, drug-drug interaction study conducted over three menstrual cycles in healthy women with regular menses."( Effects of concurrent vaginal miconazole treatment on the absorption and exposure of Nestorone® (segesterone acetate) and ethinyl estradiol delivered from a contraceptive vaginal ring: a randomized, crossover drug-drug interaction study.
Alami, M; Creasy, G; Han, L; Hoskin, E; Kumar, N; Merkatz, R; Plagianos, M; Roberts, K; Simmons, KB; Variano, B, 2018
)
0.48

Bioavailability

ExcerptReferenceRelevance
" Since studies with this drug have shown good contraceptive efficacy and low bioavailability after oral intake, ST-1435 is a good candidate for lactational contraception."( Milk and plasma concentrations of the progestin ST-1435 in women treated parenterally with ST-1435.
Croxatto, H; Diaz, S; Lähteenmäki, P; Lähteenmäki, PL; Miranda, P, 1990
)
0.28
" A peak concentration of 240 ng ST-1435/ml was found in portal plasma 75 minutes after administration, indicating that the steroid is well absorbed from the small intestine."( Intestinal absorption of ST-1435 in rats.
Lähteenmäki, PL, 1984
)
0.27
"1 mg indicated that the bioavailability of ST 1435 is low."( The progestin ST 1435--rapid metabolism in man.
Haukkamaa, M; Heikinheimo, O; Lähteenmäki, P; Noe, G, 1994
)
0.91
" After oral administration, the bioavailability was about 10% of the dose."( Pharmacokinetics and bioavailability of ST 1435 administered by different routes.
Croxatto, HB; Heikinheimo, O; Maturana, X; Noé, G; Salvatierra, A, 1993
)
0.55
" This delivery system provides many advantages over oral contraceptives (OCs), including avoidance of the first-pass effect through the liver, constant serum steroid levels, longer duration of use, and greater bioavailability of the hormones."( Contraceptive vaginal rings.
Harwood, B; Mishell, DR, 2001
)
0.31
" The biological actions of progestins are primarily determined by their interactions with steroid receptors, and factors such as metabolism, pharmacokinetics, bioavailability and the regulation of endogenous steroid hormone biosynthesis are often overlooked."( Fourth-Generation Progestins Inhibit 3β-Hydroxysteroid Dehydrogenase Type 2 and Modulate the Biosynthesis of Endogenous Steroids.
Africander, D; Louw-du Toit, R; Perkins, MS; Snoep, JL; Storbeck, KH, 2016
)
0.43
"Our previous studies showed that intranasal delivery of progesterone offers a good bioavailability and neuroprotective efficacy after experimental stroke."( Sex differences in the cerebroprotection by Nestorone intranasal delivery following stroke in mice.
Fréchou, M; Guennoun, R; Kumar, N; Mattern, C; Schumacher, M; Sitruk-Ware, R; Zhu, X, 2021
)
0.62

Dosage Studied

ExcerptRelevanceReference
" With this dosage level, ovulation is inhibited and side effects are minimized."( Contraception with subdermal implants releasing the progestin ST-1435: a dose-finding study.
Haukkamaa, M; Heikinheimo, O; Laurikka-Routti, M; Moo-Young, A, 1992
)
0.28
" Protection is ensured with a low drug dosage and no estrogen, and fertility is readily reversible once the implants are removed."( Subdermal contraceptive implants.
Croxatto, H; Diaz, S; Peralta, O, 1995
)
0.29
" This study aimed to test metered spray delivery of a precise dosage of Nestorone (NES) progestogen as a possible transdermal progestogen-only contraceptive."( An initial pharmacokinetic study with a Metered Dose Transdermal Systemfor delivery of the progestogen Nestorone as a possible future contraceptive.
Fraser, IS; Humberstone, AJ; Kumar, N; Kumar, S; McCrossin, L; Shaw, D; Sitruk-Ware, R; Tsong, YY; Weisberg, E, 2007
)
0.34
" Each subject was studied on two occasions with multiple blood sampling for assay of NES over a 24-h period: on the first occasion, after a single dosage of 3 x 90 microL NES sprays using a specially devised, precisely metered delivery device; on the second occasion, following the fifth in a series of five daily transdermal dosages of 3 x 90 microL of NES spray."( An initial pharmacokinetic study with a Metered Dose Transdermal Systemfor delivery of the progestogen Nestorone as a possible future contraceptive.
Fraser, IS; Humberstone, AJ; Kumar, N; Kumar, S; McCrossin, L; Shaw, D; Sitruk-Ware, R; Tsong, YY; Weisberg, E, 2007
)
0.34
" The dose-response relationship of nestorone showed that the 6-h post-ischemic administration of 10 μg/kg nestorone resulted in greater reductions in infarct sizes 48 h after MCAO than the other two doses tested (5 and 80 μg/kg), and this dose of nestorone significantly decreased astrocyte activation in the peri-infarct cortical region."( Nestorone exerts long-term neuroprotective effects against transient focal cerebral ischemia in adult male rats.
Ogaeri, T; Samsonov, M; Sokabe, M; Tanaka, M, 2019
)
0.51
"One hundred fifty-one women completed the study, and 82 women had complete data available for the bone marker analyses; the three dosage groups were balanced with regard to baseline characteristics."( Bone turnover markers in women participating in a dose-finding trial of a contraceptive vaginal ring releasing Nestorone and estradiol.
Blithe, DL; Cohen, A; Cremers, S; Sitruk-Ware, R; Tiedeken, M; Westhoff, CL, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
corticosteroid hormoneAny of a class of steroid hormones that are produced in the adrenal cortex.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (94)

TimeframeStudies, This Drug (%)All Drugs %
pre-199010 (10.64)18.7374
1990's23 (24.47)18.2507
2000's26 (27.66)29.6817
2010's28 (29.79)24.3611
2020's7 (7.45)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 9.97

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index9.97 (24.57)
Research Supply Index4.86 (2.92)
Research Growth Index4.83 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.97)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials31 (31.96%)5.53%
Reviews14 (14.43%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other52 (53.61%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (9)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Clinical Evaluation of Daily Application of Nestorone® (NES) and Testosterone (T) Combination Gel for Male Contraception [NCT03452111]Phase 2420 participants (Actual)Interventional2018-10-25Active, not recruiting
A Multicenter, Open-label Study on the Efficacy, Cycle Control and Safety of a Contraceptive Vaginal Ring Delivering a Daily Dose of 150µg of Nestorone® and 15µg of Ethinyl Estradiol (150/15 NES/EE CVR) [NCT00455156]Phase 31,143 participants (Actual)Interventional2006-12-31Completed
A Double-Blind, Placebo-Controlled, Randomized, Crossover Design Study With an Open-Label Active Control to Evaluate the Potential of Nestorone® to Delay Cardiac Repolarization in Healthy Female Volunteers: A Thorough QT/QTc Study [NCT02236026]Phase 144 participants (Actual)Interventional2014-09-30Completed
A Multicenter, Randomized, Double-Blind Comparator Trial of the Safety and Sperm and Gonadotropin Suppression Resulting From Combined Use of Nestorone® Gel (0, 8 or 12 mg NES) and Testosterone Gel (10 g) Compared With Testosterone Gel in Normal Men [NCT00891228]Phase 199 participants (Actual)Interventional2009-05-31Completed
A Dose Finding Study to Evaluate Serum Estradiol Levels With Use of Contraceptive Vaginal Rings Releasing Nestorone® and Escalating Doses of Estradiol in Normal Cycling Women [NCT02626208]Phase 265 participants (Actual)Interventional2016-01-31Completed
A Randomized, Open-Label Study Comparing the Effect of a Contraceptive Vaginal Ring Delivering Daily Doses of 150 Micrograms Nestorone and 15 Micrograms Ethinyl Estradiol to an Oral Contraceptive Containing 150 Micrograms of Levonorgestrel and 30 Microgra [NCT00213096]Phase 250 participants Interventional2003-03-31Completed
A Randomized, Open Label Clinical Trial to Evaluate if Nestorone Gel Has Gonadotropin Suppressive Activity and if Nestorone in Combination With Testosterone Will Have an Additive Effect on Gonadotropin Suppression When Applied Transdermally in Healthy Men [NCT00229593]Phase 1140 participants (Actual)Interventional2005-09-30Completed
An Open-Label Study of Serum Testosterone and Nestorone in Females After Secondary Exposure to Nestorone ® (NES) + Testosterone (T) Combined Gel Applied to Shoulders and Upper Arms in Males: Effect of Washing or Clothing Barrier to the Application [NCT02994602]Phase 112 participants (Actual)Interventional2017-01-31Completed
A Randomized, Two Center, Double-Blind Trial to Evaluate the Pharmacokinetics and Gonadotropin Suppression of Nestorone®-Testosterone (NES/T) Combination Gel in Healthy Men [NCT02432261]Phase 144 participants (Actual)Interventional2015-04-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00891228 (5) [back to overview]The Impact on Sperm Morphology in Men Who Are Not Azoospermic
NCT00891228 (5) [back to overview]The Number of Men Who Have Azoospermia
NCT00891228 (5) [back to overview]The Number of Men Who Have Suppression of Sperm Production ≤1Million/mL Million/mL When Using a Daily Regimen of Nestorone® Gel (0, 8 or 12 mg) and Testosterone Gel Applied Transdermally.
NCT00891228 (5) [back to overview]The Number of Men Who Have Suppression of Sperm Production ≤3 Million/mL ≤ 3 Million/mL or Azoospermia When Using a Daily Regimen of Nestorone® Gel (0, 8 or 12 mg) and Testosterone Gel.
NCT00891228 (5) [back to overview]The Impact on Sperm Motility in Men Who Are Not Azoospermic Azoospermic.

The Impact on Sperm Morphology in Men Who Are Not Azoospermic

(NCT00891228)
Timeframe: 24 weeks

Interventionpercentage normal morphology (Mean)
Testosterone Gel 10 g and Nestorone® 0 mg Per Day12.3
Testosterone Gel 10 g and Nestorone® 8 mg Per Day10.8
Testosterone Gel 10 g Plus Nestorone® Gel 12 mg Per Day9.1

[back to top]

The Number of Men Who Have Azoospermia

(NCT00891228)
Timeframe: 24 Weeks

Interventionparticipants (Number)
Testosterone Gel 10 g and Nestorone® 0 mg Per Day5
Testosterone Gel 10 g and Nestorone® 8 mg Per Day14
Testosterone Gel 10 g Plus Nestorone® Gel 12 mg Per Day11

[back to top]

The Number of Men Who Have Suppression of Sperm Production ≤1Million/mL Million/mL When Using a Daily Regimen of Nestorone® Gel (0, 8 or 12 mg) and Testosterone Gel Applied Transdermally.

(NCT00891228)
Timeframe: 24 Weeks

Interventionparticipants (Number)
Testosterone Gel 10 g and Nestorone® 0 mg Per Day5
Testosterone Gel 10 g and Nestorone® 8 mg Per Day15
Testosterone Gel 10 g Plus Nestorone® Gel 12 mg Per Day13

[back to top]

The Number of Men Who Have Suppression of Sperm Production ≤3 Million/mL ≤ 3 Million/mL or Azoospermia When Using a Daily Regimen of Nestorone® Gel (0, 8 or 12 mg) and Testosterone Gel.

(NCT00891228)
Timeframe: 24 Weeks

Interventionparticipants (Number)
Testosterone Gel 10 g and Nestorone® 0 mg Per Day5
Testosterone Gel 10 g and Nestorone® 8 mg Per Day15
Testosterone Gel 10 g Plus Nestorone® Gel 12 mg Per Day14

[back to top]

The Impact on Sperm Motility in Men Who Are Not Azoospermic Azoospermic.

(NCT00891228)
Timeframe: 24 Weeks

,,
Interventionpercentage of sperm (Mean)
Percent Progressive (week 24)Percent Non Progressive (week 24)
Testosterone Gel 10 g and Nestorone® 0 mg Per Day52.810.4
Testosterone Gel 10 g and Nestorone® 8 mg Per Day31.97.4
Testosterone Gel 10 g Plus Nestorone® Gel 12 mg Per Day29.68.3

[back to top]