Drug intelligence / Profile preview

dimethisterone

Development stage
Discontinued
Lead developer
GSK
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Dimethisterone is a **synthetic progestin (progestogen)**, formerly used orally as a component of birth control pills and for the treatment of gynecological disorders[1][4][3][5]. It acts as an **agonist of the progesterone receptor** (PR), with well-marked progestational properties and negligible androgenic or estrogenic activity, and some minor antimineralocorticoid activity[1][4][3]. Dimethisterone was introduced in the 1950s by British Drug Houses and became marketed primarily under the brand names Lutagan and Secrosteron, as well as in combination products with ethinylestradiol (for contraception). Despite increased potency compared to ethisterone, dimethisterone was one of the weakest oral progestogens known and was eventually discontinued, primarily due to a failure to adequately mitigate estrogen-induced endometrial cancer risk in combination formulations[1][4]. Mechanistically, it does not demonstrate important activity at other hormone receptors[1][4][3][5].

Brand names
LutaganSecrosteronOracon (only in combination with ethinylestradiol)Ovin (only in combination)Secrodyl (only in combination)Secrovin (only in combination)Tova (only in combination)
Other names
DimethindroneDimethisteronDimethisterone MonohydrateDimethisterone AnhydrousDimetisteroneDimethisteroniumDimetisteronaDimethisteronum
02

Targets

PR (Progesterone receptor)MR (Mineralocorticoid receptor)

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