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Estradiol

Generic Name
Estradiol
Brand Names
Activella 1/0.5 28 Day, Activelle, Amabelz 0.5/0.1 28 Day, Angeliq 0.25/0.5 28 Day, Bijuva, Climara, Climara Pro, Combipatch, Divigel, Dotti, Elestrin, Estalis, Estrace, Estradot, Estring, Estrogel, Etyqa 0.5/0.1 28 Day, Evamist, Imvexxy 4 Mcg Starter Pack, Lopreeza 1/0.5 28 Day, Lyllana, Menostar, Mimvey, Minivelle, Myfembree, Oesclim, Oriahnn 28 Day Kit, Prefest 30 Day, Vagifem, Vivelle, Yuvafem
Drug Type
Small Molecule
Chemical Formula
C18H24O2
CAS Number
50-28-2
Unique Ingredient Identifier
4TI98Z838E
Background

Estradiol is a naturally occurring hormone circulating endogenously in females. It is commercially available in several hormone therapy products for managing conditions associated with reduced estrogen, such as vulvovaginal atrophy and hot flashes. Some available forms of estradiol include oral tablets, injections, vaginal rings, transdermal patches, sprays, gels, and creams.

When used for oral or IM administration, estradiol is commonly synthesized as a pro-drug ester (such as Estradiol acetate, Estradiol benzoate, Estradiol cypionate, Estradiol dienanthate, and Estradiol valerate). Because it has a low oral bioavailability on its own, estradiol is commonly formulated with an ester side-chain. Ethinylestradiol (EE) is a synthetic form of estradiol commonly used as the estrogenic component of most combination oral contraceptive pills (OCPs). Ethinyl estradiol is different from estradiol due to its higher biovailability and increased resistance to metabolism, rendering it more suitable for oral administration.

Indication

Estradiol is indicated in various preparations for the treatment of moderate to severe vasomotor symptoms and vulvar and vaginal atrophy due to menopause, for the treatment of hypoestrogenism due to hypogonadism, castration, or primary ovarian failure, and for the prevention of postmenopausal osteoporosis. It is also used for the treatment of breast cancer (only for palliation therapy) in certain men or women with metastatic disease, and for the treatment of androgen-dependent prostate cancer (only for palliation therapy). It is also used in combination with other hormones as a component of oral contraceptive pills for preventing pregnancy (most commonly as Ethinylestradiol, a synthetic form of estradiol).

A note on duration of treatment

Recommendations for treatment of menopausal symptoms changed drastically following the release of results and early termination of the Women's Health Initiative (WHI) studies in 2002 as concerns were raised regarding estrogen use. Specifically, the combined estrogen–progestin group was discontinued after about 5 years of follow up due to a statistically significant increase in invasive breast cancer and in cardiovascular events.

Following extensive critique of the WHI results, Hormone Replacement Therapy (HRT) is now recommended to be used only for a short period (for 3-5 years postmenopause) in low doses, and in women without a history of breast cancer or increased risk of cardiovascular or thromboembolic disease. Estrogen for postmenopausal symptoms should always be given with a progestin component due to estrogen's stimulatory effects on the endometrium; in women with an intact uterus, unopposed estrogen has been shown to promote the growth of the endometrium which can lead to endometrial hyperplasia and possibly cancer over the long-term.

Associated Conditions
Atrophic Vaginitis, Breast Cancer, Breast engorgement caused by Postpartum state, Heavy Menstrual Bleeding, Hypogonadism female, Kraurosis Vulvae, Metastatic Breast Cancer, Osteoporosis, Postmenopausal Osteoporosis, Premature Ovarian Failure (POF), Prostate Cancer, Severe Pain, Urogenital atrophy, Vasomotor Symptoms Associated With Menopause, Vulvo Vaginal Atrophy, Advanced androgen dependent Prostate cancer, Female castration, Hypoestrogenism
Associated Therapies
Contraception, Hormone Replacement Therapy, Palliative Treatment
Clinical Trials
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• ANI Pharmaceuticals has received FDA approval for its Abbreviated New Drug Application (ANDA) for Estradiol Gel, 0.06%, a generic version of EstroGel. • The launch of this product aims to provide readily accessible treatment options for customers and patients in need, addressing a limited-competition market. • According to August 2024 IQVIA data, the U.S. annual sales for Estradiol Gel, 0.06% total approximately $16.7 million, highlighting its market potential.

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• ANI Pharmaceuticals has received FDA approval for its Abbreviated New Drug Application (ANDA) for Estradiol Gel, 0.06%, a generic version of EstroGel. • The launch of this product expands ANI's portfolio of limited-competition pharmaceuticals, ensuring greater access for patients in need. • U.S. annual sales for Estradiol Gel, 0.06% total approximately $16.7 million, based on August 2024 moving annual total (MAT) IQVIA data.

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