Trimegestone

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Trimegestone
Trimegestone.png
Systematic (IUPAC) name
(8S,13S,14S,17S)-17-[(2S)-2-hydroxypropanoyl]-13,17-dimethyl-1,2,6,7,8,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one
Identifiers
CAS Number 74513-62-5
ATC code G03FA16 (WHO)
PubChem CID 68926
ChemSpider 62152
Synonyms RU-27987
Chemical data
Formula C22H30O3
Molar mass 342.472 g/mol

Trimegestone (INN) (brand name Ondeva), also known as 21-hydroxypromegestone, is a 19-norprogesterone derivative and steroidal progestin which was introduced in France in 2001 and is used as a hormonal contraceptive and in hormonal replacement therapy for postmenopausal symptoms.[1][2][3][4] It is a very potent and pure progestogen and is the most potent progestin of the 19-norprogesterone group (clinically effective in endometriosis at only 0.1 mg/day).[2][3][5] The drug has little activity at other steroid hormone receptors,[2][3] and in accordance, possesses no androgenic, antiandrogenic, or glucocorticoid properties.[5] However, it is said to have weak antimineralocorticoid activity.[5] The metabolites of trimgestone are active and have similar properties to the parent drug.[5]

Trimegestone has been described as both "fourth generation" and "second generation" (due to the use of different progestin generational schemes; in any case, it is considered to be of the most recent generation).[6][7]

See also[edit]

References[edit]

  1. ^ C.R. Ganellin; David J. Triggle (21 November 1996). Dictionary of Pharmacological Agents. CRC Press. pp. 2063–. ISBN 978-0-412-46630-4. 
  2. ^ a b c Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 208–. ISBN 978-3-527-62330-3. 
  3. ^ a b c Winnifred Cutler (30 March 2009). Hormones and Your Health: The Smart Woman's Guide to Hormonal and Alternative Therapies for Menopause. John Wiley & Sons. pp. 43–. ISBN 978-0-470-52553-1. 
  4. ^ Annual Reports in Medicinal Chemistry. Academic Press. 31 December 2012. pp. 273, 647. ISBN 978-0-12-397214-9. 
  5. ^ a b c d Kuhl, H (2009). "Pharmacology of estrogens and progestogens: influence of different routes of administration" (PDF). Climacteric 8 (sup1): 3–63. doi:10.1080/13697130500148875. ISSN 1369-7137. 
  6. ^ Ramesh N. Patel (26 September 2006). Biocatalysis in the Pharmaceutical and Biotechnology Industries. CRC Press. pp. 288–. ISBN 978-1-4200-1937-7. 
  7. ^ Sitruk-Ware R (2004). "New progestogens: a review of their effects in perimenopausal and postmenopausal women". Drugs Aging 21 (13): 865–83. doi:10.2165/00002512-200421130-00004. PMID 15493951.