ID Source | ID |
---|---|
PubMed CID | 108059 |
CHEMBL ID | 3707377 |
CHEBI ID | 135563 |
SCHEMBL ID | 1261001 |
MeSH ID | M0093226 |
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 |
Excerpt | Reference | Relevance |
---|---|---|
"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 |
Excerpt | Reference | Relevance |
---|---|---|
" 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 |
Excerpt | Relevance | Reference |
---|---|---|
" 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 |
Class | Description |
---|---|
corticosteroid hormone | Any 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] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
AID1794808 | Fluorescence-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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 10 (10.64) | 18.7374 |
1990's | 23 (24.47) | 18.2507 |
2000's | 26 (27.66) | 29.6817 |
2010's | 28 (29.79) | 24.3611 |
2020's | 7 (7.45) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (9.97) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 31 (31.96%) | 5.53% |
Reviews | 14 (14.43%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 52 (53.61%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
Clinical Evaluation of Daily Application of Nestorone® (NES) and Testosterone (T) Combination Gel for Male Contraception [NCT03452111] | Phase 2 | 420 participants (Actual) | Interventional | 2018-10-25 | Active, 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 3 | 1,143 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
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 1 | 44 participants (Actual) | Interventional | 2014-09-30 | Completed | ||
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 1 | 99 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
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 2 | 65 participants (Actual) | Interventional | 2016-01-31 | Completed | ||
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 2 | 50 participants | Interventional | 2003-03-31 | Completed | ||
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 1 | 140 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
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 1 | 12 participants (Actual) | Interventional | 2017-01-31 | Completed | ||
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 1 | 44 participants (Actual) | Interventional | 2015-04-30 | Completed | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |