is provided as a service by IQWiG to English-language readers. However, solely the German original text is absolutely authoritative and legally binding. Extract IQWiG Reports – Commission No. A21-112 Relugolix/estradiol/nor-ethisterone acetate (uterine fibroids) – Benefit assessment according to §35a Social Code Book V1 Extract of dossier assessment A22-112 Version 1.1 Relugolix/estradiol/norethisterone
derivative of ethisterone, is a steroid molecule with significant androgen activity and is effective in the treatment of adenomyosis and endometriosis. Its use is associated with androgenic side effects. Vaginal symptoms may benefit from a vaginal moisturizer, such as Replens, and/or low-dose vaginal estrogen, such as Vagifem or Femring. Although these have not been studied in adenomyosis, the lack
the characterization of a multivalent conjugate presenting two bioactive ethisterone ligands arrayed as spatially defined pendant groups on a peptoid oligomer. The conjugate, named Multivalent Peptoid Conjugate 6 (MPC6), suppressed the proliferation of multiple AR-expressing prostate cancer cell lines including those that failed to respond to enzalutamide and ARN509. The structure-activity relationships of MPC6 variants were evaluated, revealing that increased spacing between ethisterone moieties and changes in peptoid topology eliminated its antiproliferative effect, suggesting that both ethisterone ligand presentation and scaffold characteristics contribute to MPC6 activity. Mechanistically, MPC6 blocked AR coactivator-peptide interaction and prevented AR intermolecular interactions. Protease sensitivity
derivative of ethisterone, is a steroid molecule with significant androgen activity and is effective in the treatment of adenomyosis and endometriosis. Its use is associated with androgenic side effects. Vaginal symptoms may benefit from a vaginal moisturizer, such as Replens, and/or low-dose vaginal estrogen, such as Vagifem or Femring. Although these have not been studied in adenomyosis, the lack
derivative of ethisterone, is a steroid molecule with significant androgen activity and is effective in the treatment of adenomyosis and endometriosis. Its use is associated with androgenic side effects. Vaginal symptoms may benefit from a vaginal moisturizer, such as Replens, and/or low-dose vaginal estrogen, such as Vagifem or Femring. Although these have not been studied in adenomyosis, the lack
varies with the drug and dosage.[1]Androgens[edit]The only sex steroid currently utilized in women that can cause virilization of female fetuses when administered in usually administered doses is the androgen danazol, a derivative of ethisterone (ethinyltestosterone).[1]Fetal masculinization of female external genitalia has resulted from doses of danazol as low as 200 mg/day, whereas 800 mg/day is the usual initial dose when danazol is used to treat severe endometriosis.[1]Progestogens[edit]In general, pregnane derivatives (e.g., progesterone, dydrogesterone, hydroxyprogesterone caproate, medroxyprogesterone acetate, megestrol acetate) do not virilize even in high dose; testosterone derivatives (ethisterone) and 19-nortestosterone (norethisterone, norethisterone acetate, etc.) generally virilize