Trimegestone

Trimegestone, sold under the brand names Ondeva and Totelle among others, is a progestin medication which is used in menopausal hormone therapy and in the prevention of postmenopausal osteoporosis. It was also under development for use in birth control pills to prevent pregnancy, but ultimately was not marketed for this purpose. The medication is available alone or in combination with an estrogen. It is taken by mouth.

Trimegestone
Clinical data
Trade namesGinotex, Lovelle, Minique, Ondeva, Totelle, others
Other namesTMG; RU-27987; 21(S)-Hydroxypromegestone; 21β-Hydroxypromegestone; 21(S)-Hydroxy-17α,21-dimethyl-9-dehydro-19-norprogesterone; 21(S)-Hydroxy-17α,21-dimethyl-19-norpregna-4,9-dien-3,20-dione; 17β-(S)-Lactoyl-17α-methylestra-4,9-dien-3-one; 17β-((S)-2-Hydroxypropanoyl)-17α-methylestra-4,9-dien-3-one
Routes of
administration		By mouth
Drug classProgestogen; Progestin
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability100%
Protein binding98% (to albumin)
MetabolismMainly hydroxylation
Elimination half-lifeRange: 12–20 hours
Mean: 13.8–15.6 hours
Identifiers
  • (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
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard100.189.099
Chemical and physical data
FormulaC22H30O3
Molar mass342.479 g·mol−1
3D model (JSmol)
  • C[C@@H](C(=O)[C@]1(CC[C@@H]2[C@@]1(CCC3=C4CCC(=O)C=C4CC[C@@H]23)C)C)O
  • InChI=1S/C22H30O3/c1-13(23)20(25)22(3)11-9-19-18-6-4-14-12-15(24)5-7-16(14)17(18)8-10-21(19,22)2/h12-13,18-19,23H,4-11H2,1-3H3/t13-,18+,19-,21-,22+/m0/s1
  • Key:JUNDJWOLDSCTFK-MTZCLOFQSA-N

Side effects of trimegestone include headache, breast tenderness, nervousness, abdominal pain, bloating, muscle cramps, nausea, depression, and vaginal bleeding among others. Trimegestone 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 weak antiandrogenic and antimineralocorticoid activity and no other important hormonal activity.

Trimegestone was first described in 1979 and was introduced for medical use in 2001. It is sometimes described as a "fourth-generation" progestin. The medication is marketed throughout Europe and Latin America. It is not available in the United States or Canada.

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