
Estradiol ValerateBenefits, Dosage & Interactions
Also known as: Delestrogen
Estradiol valerate is an ester of estradiol, the main human estrogen, formulated so it releases slowly after injection or absorbs orally. It is used in menopausal hormone therapy, in feminizing hormone therapy, and in some combined oral contraceptives. Research on Estradiol Valerate focuses on bone and joint health, testosterone support, and menopause symptoms.
How much Estradiol Valerate do people take?
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). Route reported: Oral tablets in the cited trial; injectable estradiol valerate esters also exist outside it. Frequency reported: Once daily, per the labeled 28-day multiphasic regimen. These are amounts documented in the cited studies and labels for Estradiol Valerate — they are reported for reference, not a recommendation. Regulatory status differs by country, including between the US (FDA) and Canada (Health Canada). Confirm any amount with a licensed clinician before you take it.
See the full reported protocol and its sourcesResearched by DoseRoutine Research TeamReviewed for accuracy by Nicholas Alexander, RSE, SO, PMPLast updated Educational reference only — not medical advice. Always confirm dosing and safety decisions with a licensed clinician.
One published human randomized trial; results not yet replicated.
Quick answer
Estradiol valerate is an ester of estradiol, the main human estrogen, formulated so it releases slowly after injection or absorbs orally. It is used in menopausal hormone therapy, in feminizing hormone therapy, and in some combined oral contraceptives. Because it is bioidentical estradiol once cleaved, its side-effect profile is that of estrogen therapy generally rather than anything unique to the ester.
- What it is
- Ester (valerate) of bioidentical estradiol
- Forms
- Intramuscular oil injection and oral tablet
- Used in
- Menopausal hormone therapy, feminizing hormone therapy, some contraceptives
- Why the ester
- Slows release from the injection site, extending the interval between doses
- Common side effects
- Breast tenderness, headache, nausea, fluid retention, mood changes
- Boxed warning
- Estrogen therapy labels carry warnings on clots, stroke and certain cancers
Compiled by DoseRoutine from public sources including NIH/MedlinePlus, the FDA label, Mayo Clinic and PubChem. Educational information, not medical advice.
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.
Mixing Estradiol Valerate: bacteriostatic water and syringe units
The vial arrives as dry powder. How much water you add sets the strength, and the strength sets the mark you draw to on the syringe. The table assumes a 5 mg vial and a 250 mcg example draw on a U-100 insulin syringe, where 100 units is one millilitre. If your vial is a different size, scale it — the arithmetic is the same.
| Bacteriostatic water added | Resulting strength | 250 mcg draws to |
|---|---|---|
| 1 mL | 5 mg/mL | 5 units |
| 2 mL | 2.5 mg/mL | 10 units |
| 3 mL | 1.67 mg/mL | 15 units |
Units, not millilitres. Insulin syringes are marked in units, and mixing up mcg and mg on a peptide label is the single most common error people report. Check the label twice. Run your own vial through the calculator.
Storage and stability
- Before mixing
- Sealed and still as a dry powder, Estradiol Valerate vials are normally kept in the fridge at 2–8 °C, out of light. Short spells at room temperature during shipping are the norm for lyophilized peptides and are not, on their own, a sign the vial is spoiled.
- After mixing
- Once bacteriostatic water goes in, the vial belongs in the fridge and is generally treated as good for about 28 days — that is how long the benzyl alcohol in bacteriostatic water is relied on to hold back bacterial growth. Plain sterile water has no preservative, so a vial mixed with it is a single-session vial. Never freeze a reconstituted vial.
- When to throw it out
- A properly mixed vial is clear. Cloudiness, floating strands, a color change or powder that will not go into solution after gentle swirling all mean the vial should be discarded rather than used. Shaking a peptide vial hard is the usual cause — swirl it, or run the water down the inside wall of the vial instead of onto the powder.
Handling and shelf-life figures describe general practice for lyophilized peptides. They are not a dose and not medical advice — your prescriber or the product label sets the amount.
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
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.
What does the research say about Estradiol Valerate?
Tap a section to expand.
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.
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.
Put it into practice
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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
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
- 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 an ester of estradiol, the main human estrogen, formulated so it releases slowly after injection or absorbs orally. It is used in menopausal hormone therapy, in feminizing hormone therapy, and in some combined oral contraceptives. Research on Estradiol Valerate focuses on bone and joint health, testosterone support, and menopause symptoms.
Estradiol Valerate cheat sheet
DoseRoutine cheat sheet · Hormone
Estradiol Valerate
Estradiol valerate is an ester of estradiol, the main human estrogen, formulated so it releases slowly after injection or absorbs orally. It is used in menopausal hormone therapy, in feminizing hormone therapy, and in some combined oral contraceptives.
Evidence
Moderate
One published human randomized trial; results not yet replicated.
Studied range
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)
Route
Oral tablets in the cited trial; injectable estradiol valerate esters also exist outside it
Frequency studied
Once daily, per the labeled 28-day multiphasic regimen
Half-life
Ester is hydrolyzed to estradiol after absorption; not separately reported in the cited trial
Storage
Room temperature
Key references
Studied ranges, not dosing advice. Not medical advice — talk to a clinician. 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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