Estradiol Cypionate
Long-acting estradiol injection for menopause and perimenopause symptoms and for gender-affirming hormone therapy, given every one to two weeks. Prescribed and dosed by a licensed physician.
Injection
from $139/mo
Taken by mouth · Twice a week
Estrogen controlAromatase inhibitor
Anastrozole (Arimidex): aromatase inhibitor that blocks estrogen production, used twice weekly when estradiol is elevated during testosterone therapy. Requires recent estradiol lab before starting.
Disclaimer: Prescription products require an online evaluation with a licensed medical professional who will determine if a prescription is appropriate. Products are compounded by a licensed pharmacy. The FDA has not reviewed or approved compounded products for any use for safety, efficacy, or quality. Compounded medications are not FDA-approved brand-name products.
(a-NAS-tro-zole)
Anastrozole is an aromatase inhibitor (AI), an enzyme blocker that stops testosterone from converting to estrogen. It is used off-label in testosterone therapy when blood estradiol levels are too high, causing breast tenderness, mood changes, or water retention. Typical dose: 1 mg twice per week. It is only dosed when your latest estradiol lab shows elevation; routine use is not recommended.
Estradiol-dependent
only used when your recent lab shows high estradiol
Anastrozole requires a recent estradiol level before your physician starts it. Over-suppression of estrogen can harm bone density and cardiovascular health. Dose is adjusted or stopped based on follow-up labs.
Men on testosterone whose estradiol runs high on a blood test and who have symptoms from it.
The capsule comes in seven small strengths, so the dose can be set very low.
Too little estrogen causes joint pain, low mood and low libido. It is treated by a number on a blood test, not by guesswork.
estradiol levels drive decisions, not symptoms alone
tenderness and swelling typically improve in 2–4 weeks
when estrogen is in range, mood and water retention often normalize
avoiding over-suppression protects long-term health
Day 1
A US-licensed physician reviews your symptoms on testosterone (breast tenderness, mood changes, water retention). Estradiol lab is ordered; results guide decisions on aromatase inhibitors or tamoxifen.
1Week 1
Estradiol lab comes back. If high, your physician prescribes anastrozole 1 mg twice weekly or tamoxifen 10–20 mg daily, depending on the issue (high conversion vs. breast tissue sensitivity).
2Weeks 2–4
Symptoms from high estrogen (breast tenderness, mood swings, bloating) begin to improve. Some people feel better within days; others take 3–4 weeks.
3Week 6
Follow-up estradiol lab. If it is now in range, your physician adjusts or stops the AI/SERM. If still high, dose is increased or agent is switched.
4Beyond
Estradiol is monitored every 6–12 weeks. Your physician aims to keep estrogen in a healthy range, not suppressed, not elevated, to preserve bone and cardiovascular health.
5Individual results vary. Benefits reflect what Zepym Health members commonly report to their physician at check-ins; they are not the results of a clinical trial.
This is the starting dose the pharmacy prints on the label. Your physician sets yours and adjusts it with you.
A sample week
Twice a week
Aromatase inhibitors block the conversion of testosterone to estrogen in fat and muscle tissues. When estradiol is high during testosterone therapy, anastrozole reduces it back to physiologic range.
Aromatase inhibitors are standard in testosterone therapy when estradiol is elevated. Your physician decides based on symptoms and lab values, not routine use. Excessive suppression of estrogen carries its own risks.
Learn moreAromatase inhibitors (anastrozole, exemestane) and selective estrogen receptor modulators (tamoxifen) are prescribed off-label to manage estrogen during testosterone therapy. Estradiol must be tested before starting: over-suppression can reduce bone density and harm cardiovascular health. Common side effects: mild joint aches, hot flushes, mood changes. Tamoxifen carries a small risk of blood clots and endometrial changes with long-term use (>1 year). Tell your physician about bone health, prior thrombosis, or family history of clots. Stop and seek care for leg pain/swelling, chest pain, or signs of stroke.

1.Connect with a physician
Answer a few questions online and a US-licensed physician reviews your health, history and goals to make sure treatment is right for you. 100% online. No in-person visit required.

2.Get your discreet shipment
If approved, your treatment is compounded by a US-licensed, LegitScript-certified pharmacy, inspected for quality, and shipped discreetly to your door.

3.Receive continuous support
Start with one goal, then keep building over time. Unlimited physician messaging, easy refills and dose adjustments, all from the Zepym Health app.

Anastrozole educational content reviewed by our physician
Scott Nass, MDDoctor of Medicine, board-certified in Family Medicine
Charles R. Drew University and David Geffen School of Medicine at UCLA. Family Medicine residency at Ventura County Medical Center.
Taken by mouth, twice a week. The starting prescription is 1 capsule (0.1 mg) each time. Your physician sets your own dose and it is printed on your label.
The pharmacy carries 7: 0.1 mg, 0.125 mg, 0.25 mg, 0.4 mg, 0.5 mg, 0.75 mg, 1.1 mg. Your physician chooses which one you get.
9 capsules at the starting strength, shipped to your door from a licensed US pharmacy.
Only when your estradiol lab is elevated and you have symptoms like breast tenderness, mood swings, or bloating. Your physician orders an estradiol test, and if it is high, prescribes 1 mg twice per week. When your next lab shows estradiol in normal range, you may reduce or stop the dose.
No. Many men convert testosterone to estrogen at a normal rate and do not need an AI. Your physician orders an estradiol lab; if it is normal, no AI is needed. Only if estradiol is high and causing symptoms does your physician prescribe one.
Not typically. They work differently (tamoxifen blocks estrogen in breast tissue; AIs lower overall estrogen). Your physician chooses the right tool for your issue: high overall estrogen calls for an AI; breast tissue sensitivity calls for tamoxifen.
Long-term aromatase inhibitor use can reduce bone density over time. Your physician may recommend bone density screening (DEXA scan) and calcium/vitamin D supplementation if AI use extends beyond 1–2 years.
Initial check: before starting any AI or SERM. After starting or adjusting dose: 6 weeks. Then: every 3–6 months once stable, or when symptoms change. Annual bone health screening is recommended with long-term AI use.
Long-acting estradiol injection for menopause and perimenopause symptoms and for gender-affirming hormone therapy, given every one to two weeks. Prescribed and dosed by a licensed physician.
Injection
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A low-dose aromatase inhibitor for men on testosterone therapy whose blood work shows high estradiol, easing breast tenderness and water retention. Slow-release capsule, prescribed and dosed by a licensed physician.
Capsule
from $54/mo
The above statements have not been evaluated by the Food and Drug Administration. This product is not intended to diagnose, treat, cure, or prevent any disease. Prescription products require an online evaluation with a licensed medical professional who will determine if a prescription is appropriate. Individual results vary.
Endocrine Society Clinical Practice Guidelines for testosterone therapy: managing estrogen with aromatase inhibitors.
J Clin Endocrinol Metab, 2018Tamoxifen for gynecomastia in testosterone replacement therapy: a review of evidence.
J Clin Med, 2021Anastrozole Capsulesfrom $54/mo