Estradiol diundecylenate

Estradiol diundecylenate

Estradiol diundecylenate is a synthetic, steroidal estrogen and an estrogen ester, specifically, the C17β diundecylenate ester of estradiol. It is used in combination with progestogens as a component of menopausal hormone therapy to treat and prevent menopausal symptoms in women.

Pharmacology

As an estrogen, estradiol diundecylenate has the ability to bind to and activate the estrogen receptor (ER), a type of nuclear receptor that is activated by the hormone estrogen. Upon activation, the ER can modulate the expression of certain genes, leading to the characteristic effects of estrogen.

Estradiol diundecylenate is a prodrug of estradiol, meaning that it is inactive itself but is converted into the active form, estradiol, in the body. The conversion occurs through the action of esterase enzymes, which remove the diundecylenate ester group.

Clinical use

Estradiol diundecylenate is used in combination with a progestogen in menopausal hormone therapy. This therapy is used to treat symptoms of menopause, such as hot flashes and vaginal dryness. It can also help to prevent osteoporosis, a condition that can develop in postmenopausal women due to decreased levels of estrogen.

Side effects

Like all estrogens, estradiol diundecylenate can have a number of side effects. These can include breast tenderness, nausea, headache, and mood changes. More serious side effects can include an increased risk of blood clots, stroke, and certain types of cancer, such as breast cancer and endometrial cancer.

See also

• List of estrogen esters
• Estradiol undecylate
• Estradiol valerate