As one of the endogenous estrogen female sex hormones, estradiol is used in hormone replacement therapy associated with menopause and helps prevent osteoporosis in older women. Estradiol is the principal estrogen found in a woman's body during her reproductive years and is produced by her ovaries. It is much more potent than estriol, and acts an inhibitor of ovulation by inhibiting the release of follicle-stimulating hormone (FSH).

Estradiol is widely found in nature, but also is synthesized as a white, crystalline solid that is chemically described as estra-1,3,5(10)-triene-3,17-beta-diol. Metabolic products of cholesterol include the adrenal corticosteroids, such as corticosterone, and the estrogen female sex hormones, estrone and estradiol. Estradiol is responsible for maintaining the secondary sexual characteristics of a woman.

Adverse effects of estrogen therapy with estradiol include increased risks of gallbladder disease, cardiovascular disease, elevated blood pressure, and endometrial cancer. Concurrent usage of progestin with estradiol may reduce higher cancer risks. Uterine bleeding and massive elevations of blood triglycerides have also been reported as unwanted side effects. In the growing field of palliative medicine, estradiol is sometimes prescribed for women with metastatic breast cancer, and for men with advanced, androgen-dependent prostate cancer. As a side benefit of estradiol therapy, there appears to be a reduction of coronary artery disease that may be related to increases in the liver's production of the major protein component of high-density lipids (HDLs) and a reduction in the capture of low-density lipids (LDLs). An assay of estradiol in the bloodstream, when elevated, may indicate ovarian tumors, while depressed levels may be symptomatic of Turner's syndrome, a rare genetic disorder (1 out of 3,000 births) where the female's cells are missing one of paired X chromosomes (XO instead of XX).

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