Promegestone
Chemical compound / From Wikipedia, the free encyclopedia
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Promegestone, sold under the brand name Surgestone, is a progestin medication which is used in menopausal hormone therapy and in the treatment of gynecological disorders.[4][1][5][6] It is taken by mouth.[1]
Clinical data | |
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Trade names | Surgestone |
Other names | PMG; R-5020; RU-5020; 17α,21-Dimethyl-δ9-19-norprogesterone; 17α,21-Dimethyl-19-norpregna-4,9-diene-3,20-dione |
Routes of administration | By mouth[1] |
Drug class | Progestogen; Progestin |
ATC code | |
Pharmacokinetic data | |
Protein binding | To albumin[1] |
Metabolism | Liver (hydroxylation)[1][2] |
Metabolites | • Trimegestone |
Elimination half-life | Promegestone: ? Trimegestone: 13.8–15.6 hours[1][3] |
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PubChem CID | |
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KEGG | |
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ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.207.681 |
Chemical and physical data | |
Formula | C22H30O2 |
Molar mass | 326.480 g·mol−1 |
3D model (JSmol) | |
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Side effects of promegestone include menstrual irregularities among others.[7] Promegestone is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone.[1] It has weak antiandrogenic, glucocorticoid, and antimineralocorticoid activity and no other important hormonal activity.[1][8][3] The medication is largely a prodrug of trimegestone.[7][1]
Promegestone was first described in 1973 and was introduced for medical use in France in 1983.[9][10][11] It has only been marketed in a few countries, including France, Portugal, Tunisia, and Argentina.[6][12] In addition to its use as a medication, promegestone has been widely used in scientific research as a radioligand of the progesterone receptor.[4][13]