hormoneInjectablePrescription only (US)
Estradiol ValerateBenefits, Dosage & Interactions
Also known as: Delestrogen
Estradiol valerate is a synthetic form of estradiol, which is the primary and most potent estrogen hormone produced by the ovaries. It is an ester derivative of estradiol. Research on Estradiol Valerate focuses on bone and joint health, testosterone support, and menopause symptoms.
Researched by DoseRoutine R&D TeamReviewed for accuracy by Nicholas Alexander, RSELast updated
Evidence: Moderate — One published human randomized trial; results not yet replicated.
Evidence strengthModerate · 3/4
PreclinicalStrong human evidence
One published human randomized trial; results not yet replicated.
Plasma half-life
Ester is hydrolyzed to estradiol after absorption; not separately reported in the cited trial
Default unit
mg
What published protocols report
Ranges documented in the literature, shown for reference. DoseRoutine does not recommend an amount — your prescriber or the product label sets the dose.
- Reported amounts
- The estradiol valerate/dienogest phase III trial used a 4-phase oral regimen (estradiol valerate 3 mg tapering to 1 mg, with dienogest added mid-cycle)[1]
- Route studied
- Oral tablets in the cited trial; injectable estradiol valerate esters also exist outside it[1]
- Frequency
- Once daily, per the labeled 28-day multiphasic regimen[1]
- Cycle length
- 28-day cycles, studied over multiple cycles in the trial[1]
- Half-life
- Ester is hydrolyzed to estradiol after absorption; not separately reported in the cited trial[1]
- Storage
- Room temperature[1]
Reported for Estradiol Valerate in the cited sources. Published ranges are not dosing advice.
References & evidence
Documents the Estradiol Valerate entry is written from. Each number matches an inline marker above.
- [1]Efficacy and Safety of Estradiol Valerate/Dienogest for the Management of Heavy Menstrual Bleeding: A Multicenter, Double-Blind, Randomized, Placebo-Controlled, Phase III Clinical TrialYu Q, Zhou Y, Suturina L, Jaisamrarn U, Lu D, Parke S · Journal of Women's Health · 2018 · Peer-reviewed · PMID 29957101
- [2]The shorter, the better: A review of the evidence for a shorter contraceptive hormone-free intervalGraziottin A · European Journal of Contraception & Reproductive Health Care · 2016 · Peer-reviewed · PMID 26291185
How to track Estradiol Valerate doses
Estradiol Valerate is tracked as a protocol rather than a single reminder: a vial with a concentration, a schedule that may be titrated or cycled, and a rotation of injection sites. Here is the record that keeps all three consistent.
- 1
Record the vial and concentration
Log the vial strength and the volume of bacteriostatic water you added so Estradiol Valerate is stored as a concentration rather than a guess. DoseRoutine converts that into mg per syringe unit and counts the doses left in the vial as you log.
- 2
Set the schedule, not just a reminder
Enter the dose in mg and the frequency. Cycled protocols get a start and end date so the history stays accurate when Estradiol Valerate comes out of the routine.
- 3
Rotate and log the injection site
Pick the site at the moment you log the dose. The site map shows what you used last and how recently, which is the part that drifts fastest when two compounds run on different frequencies.
- 4
Log adherence, not intentions
Mark each dose taken, skipped or delayed as it happens. Weeks of honest logs are what make an adherence rate or a trend line meaningful; retrospective guessing is not.
- 5
Review against outcomes
Review Estradiol Valerate alongside your logged metrics and any relevant blood work every few weeks before changing the dose, so the change is a response to data rather than to a good or bad day.
What to log each time
- Dose in mg and the syringe units it worked out to
- Vial: reconstitution date, concentration, doses remaining
- Injection site and time
- Any side effects in the 24 h after the dose
References & Evidence
Sources on this page that document Estradiol Valerate dosing, timing and safety.
- [1]National Center for Biotechnology Information View source
Educational information only — not medical advice. Dose ranges vary by person, indication and prescriber.
What is Estradiol Valerate studied for?
What is Estradiol Valerate?Sources for this section: Jumps to this entry in the sources and references list at the end of the page.
Estradiol valerate is a synthetic form of estradiol, which is the primary and most potent *estrogen* hormone produced by the ovaries. It is an ester derivative of estradiol. Once administered, the valerate ester is cleaved, releasing bioidentical estradiol into the body. This formulation allows for sustained release and absorption, making it suitable for various therapeutic applications. Estradiol valerate is available in several forms, including oral tablets, transdermal patches, and injectable solutions, with the injectable form often known by brand names such as Delestrogen (FDA label). It is used primarily in hormone replacement therapy (HRT) for menopausal symptoms, in the treatment of hypogonadism, for gender-affirming hormone therapy, and in certain contraceptive formulations. Its use aims to replenish estrogen levels in individuals who are deficient or require exogenous estrogen for therapeutic purposes.
What does the research say about Estradiol Valerate?
Tap a section to expand.
Estradiol valerate itself is a prodrug. After administration, it undergoes rapid hydrolysis by enzymes (esterases) in the blood and liver, releasing active 17β-estradiol. This 17β-estradiol then acts on target cells throughout the body by binding to and activating estrogen receptors (ERs), primarily estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ). These receptors are ligand-activated transcription factors. Upon binding, the estradiol-receptor complex translocates to the cell nucleus, where it interacts with specific DNA sequences called estrogen response elements (EREs) in the promoter regions of target genes. This interaction modulates gene transcription, leading to either an increase or decrease in the production of specific proteins. The wide distribution of estrogen receptors accounts for the diverse physiological effects of estradiol, including its roles in reproductive health, bone density, cardiovascular function, and central nervous system activity. By mimicking the action of endogenous estradiol, estradiol valerate helps to restore hormonal balance and alleviate symptoms associated with estrogen deficiency (EMA SmPC).
Source for this section: Sources for How does Estradiol Valerate work?: Jumps to this entry in the sources and references list at the end of the page.
Estradiol valerate is prescribed for a variety of conditions where estrogen replacement is beneficial:
* **Menopausal Hormone Therapy (MHT):** It is widely used to alleviate menopausal symptoms such as hot flashes, night sweats, vaginal dryness, itching, burning, and dyspareunia (painful intercourse). It can also help improve mood disturbances and sleep patterns associated with menopause (NIH ODS).
* **Prevention of Osteoporosis:** In postmenopausal individuals, estradiol valerate can help prevent bone loss and reduce the risk of fractures by maintaining bone mineral density (Cochrane).
* **Treatment of Hypogonadism:** For individuals with primary ovarian failure or other conditions leading to estrogen deficiency before menopause, estradiol valerate can induce puberty and maintain secondary sexual characteristics (FDA label).
* **Gender-Affirming Hormone Therapy:** It is a key component of feminizing hormone therapy for transgender women and gender-diverse individuals seeking to develop female secondary sexual characteristics and suppress endogenous testosterone production (WPATH Standards of Care).
* **Contraception:** In combination with a progestin, estradiol valerate is used in certain oral contraceptive pills to prevent pregnancy by inhibiting ovulation (DrugBank).
* **Treatment of Prostate Cancer:** In some cases, high-dose estrogen therapy, including estradiol valerate, may be used as a palliative treatment for advanced, hormone-sensitive prostate cancer (DrugBank).
Benefits typically include an improvement in the quality of life due to symptom relief and a reduction in the long-term risks associated with estrogen deficiency.
The efficacy of estradiol valerate in treating menopausal symptoms and preventing osteoporosis is well-documented. A Cochrane review published in 2015 analyzed numerous randomized controlled trials and confirmed that estrogen-only hormone therapy significantly reduces the frequency and severity of hot flashes and improves bone mineral density in postmenopausal individuals. The evidence also supports its role in improving vaginal atrophy symptoms (Cochrane).
For gender-affirming hormone therapy, clinical guidelines, such as those from the World Professional Association for Transgender Health (WPATH), recommend estradiol in various forms, including valerate, as a cornerstone of feminizing regimens. These guidelines are based on extensive clinical experience and observational studies demonstrating the induction of desired secondary sexual characteristics and psychological benefits (WPATH Standards of Care).
Its use in contraception and hypogonadism is supported by decades of clinical practice and regulatory approvals from bodies like the FDA and EMA, based on a comprehensive understanding of its pharmacological actions and demonstrated clinical outcomes (FDA label, EMA SmPC).
Common side effects of estradiol valerate can include:
* Nausea, vomiting, and abdominal cramps
* Breast tenderness or enlargement
* Headache
* Dizziness
* Bloating
* Weight changes (gain or loss)
* Irregular vaginal bleeding or spotting
* Mood changes, including depression or irritability
* Fluid retention (edema)
More serious, but less common, side effects can include:
* Blood clots (venous thromboembolism, deep vein thrombosis, pulmonary embolism)
* Stroke
* Heart attack
* Gallbladder disease
* Liver problems
* High blood pressure
* Exacerbation of migraine headaches
* Increased risk of certain cancers (breast, endometrial) with long-term use, especially when not combined with a progestin in individuals with an intact uterus.
Individual responses can vary significantly. This is educational information, not medical advice - consult a qualified clinician before starting, stopping or combining any compound.
Before starting estradiol valerate, individuals should undergo a thorough medical evaluation, including a complete medical history and physical examination, particularly breast and pelvic examinations, and blood pressure measurement. Regular monitoring is crucial during treatment.
* **Cardiovascular Risk:** Estrogen therapy, especially oral formulations and in older individuals or those with pre-existing cardiovascular risk factors, may increase the risk of cardiovascular events, including stroke and myocardial infarction. The Women's Health Initiative (WHI) study highlighted these risks. Careful consideration of individual cardiovascular risk profile is necessary (NIH ODS).
* **Thromboembolic Events:** There is an increased risk of venous thromboembolism (VTE), including deep vein thrombosis (DVT) and pulmonary embolism (PE), with estrogen use. Risk factors include a history of VTE, obesity, prolonged immobilization, and certain genetic clotting disorders (MedlinePlus).
* **Breast Cancer:** Long-term use of estrogen-only therapy has been associated with an increased risk of endometrial cancer if the uterus is intact and a combination of estrogen and progestin increases the risk of breast cancer compared to placebo in postmenopausal women. Regular breast cancer screening, including mammography, is advised (Mayo Clinic).
* **Gallbladder Disease:** Estrogens can increase the risk of gallbladder disease requiring surgery.
* **Liver Function:** Impaired liver function can affect the metabolism of estradiol valerate. It should be used with caution in individuals with liver disease.
* **Dementia:** The WHI Memory Study found an increased risk of probable dementia in postmenopausal individuals aged 65 years and older randomized to combined estrogen and progestin therapy (NIH ODS).
* **Exacerbation of certain conditions:** Estrogen therapy should be used with caution in individuals with endometriosis, asthma, epilepsy, migraine, porphyria, systemic lupus erythematosus, and hepatic hemangiomas as it may exacerbate these conditions.
This is educational information, not medical advice - consult a qualified clinician before starting, stopping or combining any compound.
Estradiol valerate is contraindicated in individuals with:
* Undiagnosed abnormal genital bleeding.
* Known or suspected breast cancer, except in appropriately selected individuals receiving treatment for metastatic disease.
* Known or suspected estrogen-dependent neoplasia.
* Active deep vein thrombosis (DVT), pulmonary embolism (PE), or a history of these conditions.
* Active arterial thromboembolic disease (e.g., stroke, myocardial infarction), or a history of these conditions.
* Known anaphylactic reaction or angioedema to estradiol valerate or any of its components.
* Known liver dysfunction or disease.
* Known protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders (FDA label).
* Pregnancy: It is not indicated for use during pregnancy or for the prevention of miscarriage. Estrogen therapy during pregnancy can be harmful.
This is educational information, not medical advice - consult a qualified clinician before starting, stopping or combining any compound.
Estradiol valerate can interact with several medications, potentially altering its effectiveness or increasing the risk of side effects. It's crucial to inform your clinician about all medications, supplements, and herbal products you are taking.
* **CYP3A4 Inducers:** Medications that induce CYP3A4 enzymes (e.g., rifampicin, carbamazepine, phenobarbital, phenytoin, St. John's wort) can increase the metabolism of estradiol, leading to lower plasma concentrations and potentially reduced therapeutic effects (EMA SmPC).
* **CYP3A4 Inhibitors:** Medications that inhibit CYP3A4 enzymes (e.g., ketoconazole, erythromycin, ritonavir, grapefruit juice) may increase estradiol plasma concentrations, potentially leading to increased side effects.
* **Thyroid Hormones:** Estrogens can increase the serum concentration of thyroid-binding globulin, requiring an increase in thyroid hormone dosage for individuals receiving thyroid replacement therapy (MedlinePlus).
* **Corticosteroids:** Estrogens can decrease the metabolic clearance of corticosteroids, potentially increasing their effects.
* **Anticoagulants:** Estrogens may impair the anticoagulant effects of coumarin derivatives (e.g., warfarin), possibly due to changes in clotting factors. Closer monitoring of INR is advised.
* **Lamotrigine:** Estrogens have been shown to decrease plasma concentrations of lamotrigine, potentially reducing seizure control in individuals with epilepsy (DrugBank).
This is educational information, not medical advice - consult a qualified clinician before starting, stopping or combining any compound.
Estradiol valerate can be administered at any time of day, as directed by a licensed clinician. The specific timing and frequency depend on the formulation (oral, patch, injectable) and the condition being treated.
* **Oral tablets:** Typically taken once daily, often at the same time each day to maintain consistent hormone levels. Some regimens involve cyclical administration (e.g., 21 days on, 7 days off) or continuous daily administration.
* **Injectable solutions:** Administered intramuscularly, typically every 1 to 4 weeks, depending on the dosage and individual response. The user-directed dose and frequency must be set by a licensed clinician.
* **Transdermal patches:** Applied to the skin and changed once or twice weekly, providing continuous estradiol release.
Estradiol valerate can be taken with or without food. Consistent adherence to the prescribed schedule is important for optimal therapeutic outcomes.
Source for this section: Sources for When should you take Estradiol Valerate?: Jumps to this entry in the sources and references list at the end of the page.
What interacts with Estradiol Valerate?
| Interacts with | Severity | Type | What happens | What to do |
|---|---|---|---|---|
| Any peptide + hormone | Note | Category ruleConfidence: theoretical | Injectable peptides plus hormones can have overlapping or compounding effects that aren't always well characterized.Source pending | Track bloodwork with a provider; don't assume combinations are neutral. |
Frequently asked questions about Estradiol Valerate
Estradiol Valerate is a hormone. It is also known as Delestrogen. The references summarized come from NIH and PubMed records, FDA labeling where it exists, and Mayo Clinic patient material.
Estradiol Valerate is commonly discussed in the context of supporting bone-joint, testosterone, menopause, and womens-longevity. Individual response varies, and use should be reviewed with a licensed clinician who can weigh the benefits and risks for your situation.
For Estradiol Valerate, it is typically administered by injection and it is typically taken null. Always follow the specific dose your clinician or the product label prescribes.
Estradiol Valerate carries potential side effects and drug interactions, documented in NIH, Mayo Clinic, and FDA label sources. Stop use and contact a clinician if you experience unexpected symptoms.
As a hormone, Estradiol Valerate can overlap with other supplements, prescription medicines, hormones and peptides. Risk depends on dose, timing and what else is taken the same day, so each pairing has to be checked rather than assumed safe. The free checker at https://doseroutine.com/interaction-checker covers Estradiol Valerate with no sign-up.
Whether Estradiol Valerate fits alongside testosterone replacement therapy depends on the protocol — dose, ester and ancillaries such as HCG or anastrozole — and on current bloodwork. No general contraindication applies across every TRT protocol, so confirm the combination with the prescribing clinician. See the free TRT interaction reference: https://doseroutine.com/trt-supplement-interactions
"Peptides" is not one category — healing peptides, GLP-1 agonists, growth-hormone secretagogues and melanocortins each behave differently next to Estradiol Valerate. Check the combination peptide by peptide rather than as one group, and review it with a clinician familiar with peptide protocols.
Published frequency for Estradiol Valerate varies by protocol and formulation, so the label or prescription is what sets it. Frequency is a clinical decision, not a fixed rule — confirm it with the prescriber or product label. Comparison of apps that keep a schedule like this: https://doseroutine.com/best-dose-tracking-apps
The effect of a missed dose of Estradiol Valerate depends on the protocol and formulation you are on. For injectable protocols, shifting the next injection is usually preferred over doubling it. Follow the missed-dose instructions on your label or from your clinician, and log the miss so the pattern is visible later rather than forgotten.
For an injectable like Estradiol Valerate the record needs more than a checkbox: vial concentration, the measured volume, and which site the last injection went into. A written log or spreadsheet works for planning but does not remind you or flag conflicts — see the honest comparison at https://doseroutine.com/vs/spreadsheet and the wider roundup at https://doseroutine.com/best-dose-tracking-apps — DoseRoutine tracks the schedule, the remaining supply and interactions with the rest of your routine in one place.
Which studies looked at Estradiol Valerate?
Peer-reviewed research indexed in PubMed. Each entry links to the original record.
- 1.Estradiol valerate/dienogest(opens PubMed in a new tab)Drugs · 2002 · PMID 11827562 · https://pubmed.ncbi.nlm.nih.gov/11827562/
- 2.Changes in menopause-specific quality of life between women with transdermal estradiol versus oral estrogens: results of a randomized controlled trial(opens PubMed in a new tab)Gynecol Endocrinol · 2025 · PMID 40168175 · https://pubmed.ncbi.nlm.nih.gov/40168175/
- 3.Estradiol valerate/dienogest: in oral contraception(opens PubMed in a new tab)Drugs · 2009 · PMID 19678714 · https://pubmed.ncbi.nlm.nih.gov/19678714/
Sources cited on this page
Specific documents referenced by the numbered markers above. Each number matches the marker in the text.
- PubChem CID 13791(opens in a new tab)National Center for Biotechnology Information · pubchem.ncbi.nlm.nih.gov/compound/13791
Verify at
Publisher search links for Estradiol Valerate. These are places to check the information — they are not citations, so they are not numbered.
- Cochrane Library(publisher search, opens in a new tab)Cochrane · publisher search
- DrugBank(publisher search, opens in a new tab)DrugBank Online · publisher search
- European Medicines Agency(publisher search, opens in a new tab)European Medicines Agency · publisher search
- FDA-approved labeling (DailyMed)(publisher search, opens in a new tab)U.S. Food and Drug Administration · publisher search
- Mayo Clinic(publisher search, opens in a new tab)Mayo Clinic · publisher search
- MedlinePlus(publisher search, opens in a new tab)U.S. National Library of Medicine · publisher search
- NIH Office of Dietary Supplements(publisher search, opens in a new tab)National Institutes of Health · publisher search
- PubMed literature search(publisher search, opens in a new tab)National Library of Medicine · publisher search
- Wikipedia entry(publisher search, opens in a new tab)Wikipedia · publisher search
DoseRoutine compiles summaries from publicly available scientific and regulatory references. Always verify important decisions with a licensed clinician. How we source and review this information.
What is the short answer on Estradiol Valerate?
Plain-text summary, safe to quote verbatim:
Estradiol valerate is a synthetic form of estradiol, which is the primary and most potent estrogen hormone produced by the ovaries. It is an ester derivative of estradiol. Research on Estradiol Valerate focuses on bone and joint health, testosterone support, and menopause symptoms.
Source: DoseRoutine — https://doseroutine.com/library/estradiol-valerate
Cite this page
Using this in an article, AI answer, or research note? Please attribute:
DoseRoutine. (2026). Estradiol Valerate — Overview, Benefits & Side Effects. Retrieved from https://doseroutine.com/library/estradiol-valerate
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