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Side effects of estradiol valerate include breast tenderness, breast enlargement, nausea, headache, and fluid retention. [15] [13] [14] Estradiol valerate is an estrogen and hence is an agonist of the estrogen receptor, the biological target of estrogens like estradiol. [5] [4] [16] It is an estrogen ester and a prodrug of estradiol in the body.
The combination of estradiol with a progestin, though not with oral progesterone, may increase the risk of breast cancer. [23] [24] Estradiol should not be used in women who are pregnant or breastfeeding or who have breast cancer, among other contraindications. [20]
The use of high-dose estrogen therapy in breast cancer has mostly been superseded by antiestrogen therapy due to the improved safety profile of the latter. [17] High-dose estrogen therapy was the standard of care for the palliative treatment of breast cancer in women up to the late 1970s or early 1980s. [18
Estradiol is an estrogen, or an agonist of the nuclear estrogen receptors (ERs), the estrogen receptor alpha (ERα) and the estrogen receptor beta (ERβ). [1] [2] [6] In one study, the EC 50 Tooltip half-maximal effective concentration value of estradiol for the human ERα was 50 pM (0.05 nM) and for the human ERβ was 200 pM (0.2 nM).
Estradiol valerate/gestonorone caproate (EV/GC), known by the developmental code names SH-834 and SH-8.0834, is a high-dose combination medication of estradiol valerate (EV), an estrogen, and gestonorone caproate (GC; norhydroxyprogesterone caproate), a progestin, which was developed and studied by Schering in the 1960s and 1970s for potential use in the treatment of breast cancer in women but ...
A study that used high- to very-high-dose oral estradiol to treat postmenopausal women with estrogen receptor-positive breast cancer found that mean steady-state estradiol levels in the 6 mg/day group were about 300 pg/mL and in the 30 mg/day group were about 2,400 pg/mL. [37]
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