Estradiol valerate is an estradiol prodrug used to treat some effects of menopause, hypoestrogenism, androgen dependant carcinoma of the prostate, and in combination products for endometriosis and contraception. Estradiol Valerate (also known as E2V) is a pro-drug ester of DB00783, a naturally occurring hormone that circulates endogenously within the human body.
- Mechanism
- Curator reviewed
Estradiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary.
Increases in the down-stream effects of ER binding reverses some of the symptoms of menopause, which are primarily caused by a loss of estrogenic activity.
- Primary indication
- Estradiol valerate is commercially available as an intramuscular injection as the product Delestrogen and is indicated for the treatment of moderate to severe vasomotor symptoms and vulvovaginal atrophy due to menopause, for the treatment of...Curator reviewed · 27 structured indications
- Formula / weight
- C23H32O3 · 356.4984 g/mol (avg)
- First approval
- Canada, 2000 · United States, 1954
- Brand names
Resolves to
RSEPBGGWRJCQGY-RBRWEJTLSA-NSMILES[H][C@@]12CC[C@H](OC(=O)CCCC)[C@@]1(C)CC[C@]1([H])C3=C(CC[C@@]21[H])C=C(O)C=C3What you can answer from here — as of September 30, 2026
Which drugs share a target with Estradiol valerate, and which of those have an active Phase 3 trial?
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