Drug intelligence / Profile preview

estradiol + cyproterone acetate

Development stage
Unknown
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral, Topical
01

Overview

Estradiol + cyproterone acetate is a combination hormonal regimen evaluated in the MESURE clinical trial, sponsored by University Hospital, Rouen, for the management of deep infiltrating rectal endometriosis. The regimen consists of cyproterone acetate, a synthetic progestogen with potent anti-androgenic properties, and estradiol, a natural estrogen. Cyproterone acetate acts by suppressing the hypothalamic-pituitary-ovarian axis, leading to a reduction in gonadotropin levels and subsequent inhibition of ovarian steroidogenesis, which helps to atrophy endometriotic lesions. Estradiol is administered as 'add-back therapy' (often via a percutaneous gel) to maintain physiological estrogen levels, thereby preventing bone mineral density loss and vasomotor symptoms typically associated with profound hypoestrogenism. This medical approach is being compared to curative rectal surgery to determine which management strategy yields superior digestive functional outcomes and quality of life in women who do not intend to become pregnant.

Other names
estradiol and cyproterone acetatecyproterone acetate plus estradiolestradiol + cyproterone acetate-University Hospital, Rouen-rectal endometriosis
02

Targets

GR (Glucocorticoid receptor)PR (Progesterone receptor)AR (Adrenergic receptors)ER (Estrogen receptor)

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