Nomegestrol acetate is a synthetic progestin, a type of steroid hormone that mimics the effects of progesterone. It was first synthesized in the 1960s and is primarily used for its anti-proliferative properties. It is a potent inhibitor of the growth of uterine tissue and is used in the treatment of endometriosis, uterine fibroids, and breast cancer. Nomegestrol acetate is also used in hormone replacement therapy (HRT) to manage symptoms of menopause. It is available in oral, injectable, and topical formulations. Due to its potent anti-proliferative effects, nomegestrol acetate has been studied extensively for its potential therapeutic uses in a range of conditions, including endometrial cancer, prostate cancer, and ovarian cancer. Its efficacy in these areas is still under investigation.'
nomegestrol acetate: do not confuse with Solastic
ID Source | ID |
---|---|
PubMed CID | 91668 |
CHEMBL ID | 1476022 |
CHEBI ID | 135564 |
SCHEMBL ID | 37517 |
MeSH ID | M0115853 |
Synonym |
---|
AC-1119 |
nomegestrol 17-acetate |
smr001233420 |
MLS002154113 , |
BRD-K27351809-001-02-0 |
org-10486-0 |
uniplant |
tx-066 |
lutenyl |
nomegestrol acetate |
einecs 261-379-8 |
17-alpha-acetoxy-6-methyl-19-nor-4,6-pregnadiene-3,20-dione |
19-norpregna-4,6-diene-3,20-dione, 17-alpha-hydroxy-6-methyl-, acetate |
19-norpregna-4,6-diene-3,20-dione, 17-(acetyloxy)-6-methyl- |
tx 066 |
17-alpha-hydroxy-6-methyl-19-norpregna-4,6-diene-3,20-dione acetate |
BSPBIO_001245 |
NCGC00179247-01 |
BPBIO1_001370 |
PRESTWICK3_001033 |
AB00514012 |
CHEBI:135564 |
58652-20-3 |
D08281 |
nomegestrol acetate (usan) |
lutenyl (tn) |
[(8s,9s,10r,13s,14s,17r)-17-acetyl-6,13-dimethyl-3-oxo-1,2,8,9,10,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-17-yl] acetate |
HMS2098O07 |
HMS2230M23 |
org 10486-0 |
nomac |
83j78v5w05 , |
unii-83j78v5w05 |
nomegestrol acetate [usan] |
CHEMBL1476022 |
nomegestrol acetate [ep monograph] |
17-acetoxy-6-methyl-19-norpregn-4,6-dien-3,20-dione |
6-methyl-3,20-dioxo-19-norpregna-4,6-dien-17-yl acetate |
nomegestrol acetate [mart.] |
nomegestrol acetate [who-dd] |
AKOS015896563 |
CCG-221033 |
SCHEMBL37517 |
(17alpha)-17-acetyl-6-methyl-3-oxoestra-4,6-dien-17-yl acetate |
W-105372 |
DTXSID90207349 |
sr-01000841206 |
SR-01000841206-2 |
nomegestrol acetate, >=98% (hplc) |
nomegestrol acetate, european pharmacopoeia (ep) reference standard |
HMS3715O07 |
(8s,9s,13s,14s,17r)-17-acetyl-6,13-dimethyl-3-oxo-2,3,8,9,10,11,12,13,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthren-17-yl acetate |
nomegestrone acetate |
17-alpha-hydroxy-6-methyl-19-norpregna-4,6-diene-3,20-dioneacetate |
BCP08358 |
HY-105634A |
DB13981 |
Q7048519 |
nomegestrol-acetate |
NCGC00179247-04 |
CS-0101964 |
MS-25962 |
EN300-19769276 |
(1r,3as,3bs,9ar,9bs,11as)-1-acetyl-5,11a-dimethyl-7-oxo-1h,2h,3h,3ah,3bh,7h,8h,9h,9ah,9bh,10h,11h,11ah-cyclopenta[a]phenanthren-1-yl acetate |
Nomegestrol acetate (NOMAc) is a synthetic progesterone analog and classified as a fourth-generation progestin. It is structurally similar to 19-norprogesterone and characterized as a full agonist at the progester one receptor with no or minimal binding to other steroid receptors.
Excerpt | Reference | Relevance |
---|---|---|
"Nomegestrol acetate (NMGA) is a progestogen increasingly used in contraceptive formulations." | ( Inhibition of multidrug resistance-associated protein 2 (MRP2) activity by the contraceptive nomegestrol acetate in HepG2 and Caco-2 cells. Arana, MR; Domínguez, CJ; Mottino, AD; Rigalli, JP; Ruiz, ML; Tocchetti, GN; Villanueva, SSM; Weiss, J; Zecchinati, F, 2018) | 1.42 |
"Nomegestrol acetate (NOMAc) is a synthetic progesterone analog and classified as a fourth-generation progestin. " | ( Isolation, synthesis, and cytotoxicity evaluation of two impurities in nomegestrol acetate. Huang, YS; Song, SY; Sun, YT; Xie, BC; Xie, XY; Xu, DH; Zhang, XY, 2019) | 2.19 |
"Nomegestrol acetate (NOMAC) is a widely used progestin-like drug that could be suggested as an alternative for patients taking CPA." | ( Combined hormonal influence of cyproterone acetate and nomegestrol acetate on meningioma: a case report. Champagne, PO; Froelich, S; Passeri, T, 2019) | 1.48 |
"Nomegestrol acetate is a potent, orally active progestogen with a favourable tolerability profile and neutral metabolic characteristics." | ( Nomegestrol acetate: pharmacology, safety profile and therapeutic efficacy. Lello, S, 2010) | 2.52 |
"Nomegestrol acetate (NOMAC) is a potent, highly selective progestogen, which is structurally similar to 19-norprogesterone and characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors. " | ( Nomegestrol acetate, a novel progestogen for oral contraception. Mueck, AO; Sitruk-Ware, R, 2011) | 3.25 |
"Nomegestrol acetate/estradiol is a combined oral contraceptive with approval in many countries. " | ( Nomegestrol acetate/estradiol: in oral contraception. Plosker, GL; Yang, LP, 2012) | 3.26 |
"Nomegestrol acetate is a strong anti-sulfatase agent, in particular with cancerous breast tissues." | ( Control of sulfatase activity by nomegestrol acetate in normal and cancerous human breast tissues. Chetrite, GS; Cortes-Prieto, J; Pasqualini, JR; Philippe, JC; Shields-Botella, J; Thomas, JL, ) | 1.13 |
"Nomegestrol acetate implant is a second-generation single silastic implant containing 55 mg nomegestrol acetate with contraceptive effectiveness of 1-year duration." | ( Contraceptive implants. Coutinho, EM; Ladipo, O, 1994) | 1.01 |
"Nomegestrol acetate is an innovative and efficient molecule in the treatment of menstrual disorders. " | ( [Use of nomegestrol acetate in the treatment of menstruation disorders. Our experience in 56 cases]. Lombardi, PA; Lombardi, PL; Persiani, P; Radici, E, 1997) | 2.17 |
"Nomegestrol acetate appears to be a safe and appropriate contraceptive for women with sickle cell disease, showing evidence of being a "stimulant" for F-cell reactivation, independent of F hemoglobin total production increase." | ( Nomegestrol acetate contraceptive implant use by women with sickle cell disease. Coutinho, EM; Ladipo, OA; Nascimento, Mde L, 1998) | 3.19 |
"Nomegestrol acetate (NOMAC) is an orally active progestin widely prescribed for HRT." | ( Nomegestrol acetate and vascular reactivity: nonhuman primate experiments. Delansorne, R; Hermsmeyer, KR; Paris, JM; Williams, KJ, ) | 2.3 |
"Nomegestrol acetate is a potent progestogen and further studies are required to determine its lowest effective dose." | ( The effects of the addition of nomegestrol acetate to post-menopausal oestrogen therapy. Fraser, DI; Padwick, ML; Pryse-Davies, J; Ryder, TA; White, J; Whitehead, MI, 1989) | 1.28 |
Nomegestrol acetate has been used successfully for the treatment of some gynaecological disorders (menstrual disturbances, dysmenorrhoea) and as a component of HRT in combination with estradiol for the relief of menopausal symptoms. It has proven its neutral effects on lipid metabolism and does not alter the beneficial estrogen-induced lipid effects. Nomegestroacetate has a stimulatory effect on sulfotransferase activity.
Excerpt | Reference | Relevance |
---|---|---|
"Nomegestrol acetate has a stimulatory effect on sulfotransferase activity: at low doses (5 x 10(-8) and 5 x 10(-7) mol/l) this compound strongly increases the activity of this enzyme by 60.6% and 83%, respectively, in the MCF-7 cells and by 69.2% at 5 x 10(-7) mol/l in T-47D cells." | ( Effect of nomegestrol acetate on human estrogen sulfotransferase activity in the hormone-dependent MCF-7 and T-47D breast cancer cell lines. Chetrite, GS; Paris, J; Pasqualini, JR; Philippe, JC; Shields-Botella, J, ) | 1.26 |
"Nomegestrol acetate (NOMAC) has been successfully used for the treatment of some gynecological disorders, and as a combined oral contraceptive with approval in many countries. " | ( Nomegestrol Acetate Suppresses Human Endometrial Cancer RL95-2 Cells Proliferation In Vitro and In Vivo Possibly Related to Upregulating Expression of SUFU and Wnt7a. Ma, AY; Xie, SW; Zhou, JY; Zhu, Y, 2017) | 3.34 |
"Nomegestrol acetate has been used successfully for the treatment of some gynaecological disorders (menstrual disturbances, dysmenorrhoea, premenstrual syndrome) and as a component of HRT in combination with estradiol for the relief of menopausal symptoms; it has been approved in Europe as monotherapy for the treatment of the menopausal syndrome, uterine diseases and menorrhagia, and in combination with an estrogen for the treatment of menopausal symptoms." | ( Nomegestrol acetate: pharmacology, safety profile and therapeutic efficacy. Lello, S, 2010) | 2.52 |
"Nomegestrol acetate has proven its neutral effects on lipid metabolism and does not alter the beneficial estrogen-induced lipid effects." | ( [Effects of a 19-norprogesterone derivative, the fourth decade nomegestrol acetate, on lipids]. Colau, JC; Jamin, C; Pélissier, C, 2003) | 1.28 |
"Nomegestrol acetate has a stimulatory effect on sulfotransferase activity: at low doses (5 x 10(-8) and 5 x 10(-7) mol/l) this compound strongly increases the activity of this enzyme by 60.6% and 83%, respectively, in the MCF-7 cells and by 69.2% at 5 x 10(-7) mol/l in T-47D cells." | ( Effect of nomegestrol acetate on human estrogen sulfotransferase activity in the hormone-dependent MCF-7 and T-47D breast cancer cell lines. Chetrite, GS; Paris, J; Pasqualini, JR; Philippe, JC; Shields-Botella, J, ) | 1.26 |
Excerpt | Reference | Relevance |
---|---|---|
" In the investigational group, the most frequently reported adverse events were acne (16." | ( Efficacy, safety, and tolerability of a monophasic oral contraceptive containing nomegestrol acetate and 17β-estradiol: a randomized controlled trial. Bahamondes, L; Darney, P; Kaunitz, AM; Korver, T; Sommer, W; Verhoeven, C; Westhoff, C, 2012) | 0.61 |
Excerpt | Reference | Relevance |
---|---|---|
"We have previously shown that medroxyprogesterone acetate (MPA), either alone or combined with conjugated equine estrogens (CEE), significantly decreased insulin sensitivity (SI), compared with both untreated controls and those treated with CEE alone." | ( Insulin sensitivity and cardiovascular risk factors in ovariectomized monkeys with estradiol alone or combined with nomegestrol acetate. Cefalu, WT; Greaves, KA; Thomas, MJ; Wagner, JD; Williams, JK; Zhang, L, 1998) | 0.51 |
Excerpt | Reference | Relevance |
---|---|---|
" 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 |
" If a similar regulation took place in vivo, decreased bioavailability and therapeutic efficacy of NMGA-coadministered P-gp substrates could be expected." | ( Biphasic modulation of cAMP levels by the contraceptive nomegestrol acetate. Impact on P-glycoprotein expression and activity in hepatic cells. Arana, MR; Domínguez, CJ; Mottino, AD; Rigalli, JP; Ruiz, ML; Tocchetti, GN; Villanueva, SSM; Weiss, J; Zecchinati, F, 2018) | 0.73 |
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] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 65.8114 | 0.0447 | 17.8581 | 100.0000 | AID485294; AID485341 |
TDP1 protein | Homo sapiens (human) | Potency | 8.0965 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 44.6684 | 0.1000 | 22.9075 | 100.0000 | AID485364 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 28.1838 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 23.1093 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 0.2512 | 15.8432 | 39.8107 | AID504327 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 28.1838 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
virion membrane | Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus |
[Information is prepared from geneontology information from the June-17-2024 release] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 5 (3.73) | 18.7374 |
1990's | 36 (26.87) | 18.2507 |
2000's | 29 (21.64) | 29.6817 |
2010's | 52 (38.81) | 24.3611 |
2020's | 12 (8.96) | 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 strong demand-to-supply ratio for research on this compound.
| This Compound (49.90) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 46 (31.29%) | 5.53% |
Reviews | 19 (12.93%) | 6.00% |
Case Studies | 4 (2.72%) | 4.05% |
Observational | 6 (4.08%) | 0.25% |
Other | 72 (48.98%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |