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
SMILES
[H][C@@]12CC[C@](OC(C)=O)(C(C)=O)[C@@]1(C)CC[C@]3([H])[C@@]4([H])CCC(=O)C=C4C(C)=C[C@@]23[H]
InChI
InChIKey=IIVBFTNIGYRNQY-YQLZSBIMSA-N
InChI=1S/C23H30O4/c1-13-11-20-18(17-6-5-16(26)12-19(13)17)7-9-22(4)21(20)8-10-23(22,14(2)24)27-15(3)25/h11-12,17-18,20-21H,5-10H2,1-4H3/t17-,18-,20-,21+,22+,23+/m1/s1
DescriptionSources: http://adis.springer.com/drugs/800010246Curator's Comment: Description was created based on several sources, including
http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/001213/WC500115831.pdf | https://www.ncbi.nlm.nih.gov/pubmed/20329803 | https://www.ncbi.nlm.nih.gov/pubmed/22364709
Sources: http://adis.springer.com/drugs/800010246
Curator's Comment: Description was created based on several sources, including
http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/001213/WC500115831.pdf | https://www.ncbi.nlm.nih.gov/pubmed/20329803 | https://www.ncbi.nlm.nih.gov/pubmed/22364709
Nomegestrol acetate (NOMAC) is a 19-norprogesterone derivative with high biological activity at the progesterone receptor, a weak anti-androgenic effect, but with no binding to estrogen, glucocorticoid or mineralocorticoid receptors. Nomegestrol has been developed by the Monaco-based company Théramex SAM (a Teva subsidiary). Nomegestrol acetate has been used successfully for the treatment of some gynaecological disorders (menstrual disturbances, dysmenorrhoea, premenstrual syndrome) and as a component of hormone replacement therapy 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 in combination with estradiol is used as an oral contraceptive.
CNS Activity
Sources: https://www.tga.gov.au/auspar/auspar-nomegestrol-acetate-oestradiol | https://www.ncbi.nlm.nih.gov/pubmed/25168884
Curator's Comment: Nomegestrol acetate is CNS penetrant in animals. No human data available.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL208 |
4.0 nM [Kd] | ||
Target ID: CHEMBL1871 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21757063 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Preventing | ZOELY Approved UseZOELY is used for oral contraception. Launch Date2011 |
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Primary | NOGEST Approved UseNOGEST (nomegestrol acetate) is used:
In women before menopause: for the treatment of menstrual cycle disorders caused by the absence or low secretion of progesterone. These troubles of the menstrual cycle can be:
- Menstrual cycle length abnormalities,
- Bleeding abnormalities during or outside menstruation,
- Painful menstruation,
- Troubles before menstruation such as nervousness or irritability (premenstrual syndrome),
- Breast tenderness.
In post menopausal women: as Hormone Replacement Therapy (HRT) for the treatment of menopause disorders in addition with a treatment containing estrogen in non-hysterectomized women with at least 6 months since their last natural period. |
Sample Use Guides
ZOELY (2.5 mg nomegestrol acetate/1.5 mg estradiol) tablets:
One tablet is to be taken daily for 28 consecutive days. Each pack starts with 24 white active tablets, followed by 4 yellow placebo tablets. A subsequent pack is started immediately after finishing the previous pack, without a break in daily tablet intake and irrespective of presence or absence of withdrawal bleeding. Withdrawal bleeding usually starts on day 2-3 after intake of the last white tablet and may not have finished before the next pack is started.
NOGEST (nomegestrol acetate): the usual dosage is one tablet per day (5 mg/day)
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25961213
0.5-50 uM nomegestrol acetate inhibits aromatase activity in a stable aromatase-expressing human breast cancer cell line
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C776
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EMA ASSESSMENT REPORTS |
ZOELY (AUTHORIZED: CONTRACEPTION)
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EMA ASSESSMENT REPORTS |
IOA (WITHDRAWN: CONTRACEPTION)
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261-379-8
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58652-20-3
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1957
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100000090279
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DTXSID90207349
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UU-158
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SUB03449MIG
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Nomegestrol acetate
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C038501
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C87244
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91668
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83J78V5W05
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DB13981
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53744
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CHEMBL1476022
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METABOLITE (PARENT)
PARENT (METABOLITE LESS ACTIVE)
SUBSTANCE RECORD