Demegestone Clinical data Trade names Lutionex Synonyms Dimegestone; R-2453; RU-2453; 17α-Methyl-δ 9-19-norprogesterone; 17α-Methyl-19-norpregna-4,9-diene-3,20-dione Routes of administration By mouth  Drug class Progestin; Progestogen ATC code Pharmacokinetic data Bioavailability Good  Metabolism Hydroxylation, others  Metabolites • 21-Hydroxydemegestone  • Others  Excretion Urine  Identifiers
(8 S,13 S,14 S,17 S)-17-acetyl-13,17-dimethyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[ a]phenanthren-3-one CAS Number PubChem CID ChemSpider UNII KEGG ChEBI ChEMBL ECHA InfoCard 100.030.278 Chemical and physical data Formula C 21 H 28 O 2 Molar mass 312.446 g/mol g·mol −1 3D model ( JSmol)
Demegestone, sold under the brand name Lutionex, is a progestin medication which was previously used to treat luteal insufficiency but is now no longer marketed.     It is taken  by mouth. 
Demegestone is a progestin, or a
synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone.   It has no  androgenic activity.
Demegestone was first described in 1966 and was introduced for medical use in
France in 1974.  It has only been marketed in France, and has since been discontinued in this country.  
Demegestone has been used to treat
luteal insufficiency. It has also been studied in combination with  estrogens, such as moxestrol, as an oral contraceptive and treatment for infertility.  
Demegestone is a
progestogen, and hence is an agonist of the progesterone receptor (PR).   It is a highly  potent progestogen, showing 50 times the potency of progesterone in the Clauberg test. The  ovulation-inbhiting dosage of demegestone is 2.5 mg/day, while the endometrial transformation dosage is 100 mg per cycle. The medication is devoid of  androgenic activity, and instead has some  antiandrogenic activity. Demegestone has low  affinity for the glucocorticoid receptor. In a particular  bioassay, both demegestone and progesterone showed antiglucocorticoid rather than glucocorticoid activity. The major  metabolite of demegestone, a 21- hydroxylated metabolite, is a moderately potent progestogen (4 times the potency of progesterone) and a weak mineralocorticoid (2% of the potency of deoxycorticosterone).
Demegestone has good
bioavailability. The initial  volume of distribution of demegestone is 31 L. Demegestone is  metabolized by hydroxylation at the C21, C1, C2, and C11 positions, which is eventually followed by A-ring aromatization after 1,2- dehydration. The major metabolite of demegestone is a 21-  hydroxy derivative. The  metabolic clearance rate of demegestone is 20 L/h. Its  biological half-lives are 2.39 and 0.24 hours with intravenous injection. Demegestone and/or its metabolites are  excreted, at least in part, in urine.
Demegestone, also known as 17α-methyl-δ
9-19-norprogesterone or as 17α-methyl-19-norpregna-4,9-diene-3,20-dione, is a synthetic norpregnane steroid and a derivative of progesterone.   It is specifically a combined derivative of  17α-methylprogesterone and 19-norprogesterone, or of 17α-methyl-19-norprogesterone.   Related derivatives of 17α-methyl-19-norprogesterone include  promegestone and trimegestone. 
Demegestone was first described in the literature in 1964 and was introduced for medical use in 1974 in
France.  It was developed by  Roussel Uclaf.
Society and culture
Demegestone is the generic name of the drug and its . INN It is also known by its developmental code name  R-2453 or RU-2453.
Demegestone was marketed under the brand name Lutionex.
Demegestone is no longer marketed and hence is no longer available in any country.
It was previously available in  France. 
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