Anastrozole

Men's healthHormone managementPhysician-directed

Anastrozole

RxPrescription onlyTaken by mouth · Twice a week · 0.25 mg · Men's health · Hormone management · Physician-directed

Starting at $63/mo

A compounded aromatase inhibitor (slow-release capsule, 0.25 mg twice weekly) used ONLY when a man on testosterone therapy has high estradiol on labs WITH symptoms and the physician directs it. Not a standalone treatment—the physician adds it to an existing testosterone plan.

How many capsules per month?

MonthlyEvery 3 months
9 capsulesper month

You'll receive 9 capsules per month. $79 billed monthly. Cancel anytime.

Start treatment· $79/mo

Real prices from our pharmacy. Longer plans cost less per month and are billed up front. Pause or cancel anytime.

  • Lowers high estradiol when testosterone therapy raises it too much
  • Taken only when labs show elevated estradiol and the physician approves
  • Prevents estradiol-related side effects (water retention, gynecomastia, mood changes)

Every plan includes

  • Personalized, physician-guided plan
  • 9 capsules per month, monthly and 3-month
  • Dispensed by a US-licensed compounding pharmacy
  • Unlimited protocol adjustments and messaging
  • Ongoing support and check-ins
  • Pause or cancel anytime
  • Reviewed by our in-house physicians
  • Physician-guided care
  • Ongoing, expert support
  • 100% online
  • Free, discreet shipping

What is anastrozole?

(a-NAS-truh-zole)

Anastrozole is an aromatase inhibitor (AI), an enzyme that converts testosterone into estradiol. When testosterone levels are high from therapy, aromatase can also run high, converting too much testosterone to estradiol. High estradiol in men causes water retention, fat gain in the chest, mood changes, and erectile dysfunction. Anastrozole blocks this conversion, lowering estradiol. It is compounded as a slow-release capsule, 0.25 mg twice weekly, and is prescribed only by your physician when labs confirm elevated estradiol AND you have symptoms.

How it is taken
Taken by mouth
How often
Twice a week
Dose range
0.25 mg
Form
Men's health · Hormone management · Physician-directed

Estradiol

the hormone anastrozole lowers, only when it's elevated on labs AND you have symptoms

Anastrozole is never a first-line choice or a standalone treatment. Your physician adds it to your testosterone plan only if labs show high estradiol with symptoms. Too-low estradiol has its own risks: joint pain, low libido, bone loss.

How it works,
week by week.

  1. Day 1

    Your physician reviews your testosterone labs, including estradiol. Only if it is elevated AND you report symptoms (water retention, mood changes, gynecomastia, erectile dysfunction) is anastrozole considered. The decision is individual.

  2. Week 1

    If prescribed, you take 0.25 mg twice weekly as a compounded capsule. Your physician may adjust your testosterone dose first—this alone often solves high estradiol without a second drug.

  3. Weeks 2–4

    Effects take a few weeks. Water retention may ease; mood and sexual function may improve. Your physician re-checks labs after 6–8 weeks to confirm estradiol is in range.

  4. Month 2–3

    Lab review. If estradiol is now appropriate and symptoms are gone, your physician may hold the dose steady or reduce it. The goal is the lowest effective dose.

  5. Beyond

    Anastrozole is reviewed at every testosterone check-in. Many men need it only briefly or intermittently. Your physician adjusts or stops it as your needs change.

What you may notice,
and when.

  • Normal estradiol levels

    when labs confirm excess has been reduced

  • Water retention eases

    and bloating decreases

  • Mood and sexual function return

    as estradiol comes into range

  • Energy improves

    without the fatigue of estradiol excess

Individual 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.

Safety first:
what to know before you start.

Important safety information and common side effects

Anastrozole is prescribed judiciously because too-low estradiol causes problems. Common side effects from excessive suppression include joint pain (sometimes severe), reduced sexual desire, erectile dysfunction, hot flashes, and mood changes. With appropriate dosing guided by labs, these are rare. Anastrozole can reduce bone density; your physician may monitor this if you're on it long-term. Do not take with tamoxifen or other aromatase inhibitors. Tell your physician about all medications, especially any other hormone treatments. Most importantly: anastrozole is added only if high estradiol is confirmed on labs AND you have symptoms. Without both, it is not indicated. Seek care for severe joint pain, loss of sexual function, or extreme mood changes.

The research behind
anastrozole.

Anastrozole is an aromatase inhibitor approved for breast cancer in women. In men it is used off-label to lower estradiol during testosterone therapy. Evidence in men is small and observational.

  • Estradiol on therapyestradiol lower

    In 2020, obese men with hypogonadism given anastrozole with a weight-loss programme for six months had higher testosterone and lower estradiol than men on placebo with the same programme (p 0.001 for estradiol). Symptoms and muscle strength did not differ between groups.

    Colleluori et al., Front Endocrinol 2020
  • Bone and estradiolestradiol matters

    A 2009 review found that in adult men estradiol is more strongly linked to bone density, bone turnover and bone loss than testosterone is. Lowering estradiol too far is therefore a bone caution, not a free benefit.

    Vandenput and Ohlsson, Nat Rev Endocrinol 2009
  • Male infertility reviewreview

    A 2021 review of aromatase inhibitors for male infertility. Read it for how the clinical evidence is graded before relying on any sperm or pregnancy claim.

    Yang et al., Hum Reprod Update 2021

What the studies found

  • Lowers estradiol while raising testosterone: men with obesity and hypogonadism given anastrozole with weight loss for six months had higher testosterone and lower estradiol than placebo (p 0.001 for estradiol; Colleluori et al., Front Endocrinol 2020).
  • Raises the testosterone-to-estradiol ratio more than clomiphene does: estradiol fell on anastrozole, while the ratio rose more than on clomiphene (Helo et al., J Sex Med 2015).
  • Improves semen parameters in infertile men in clinical studies reviewed in 2021, though the trials are small and mostly observational (Yang et al., Hum Reprod Update 2021).
Read the full research

Trial results are for men in a weight-loss context, not for men on testosterone alone. Compounded anastrozole and provider-only tablets were not the product studied, and estradiol targets vary between clinics.

What this does not say

  • No large randomized trial in men on testosterone shows that anastrozole improves symptoms or outcomes.
  • Lowering estradiol too far can harm bone and lipids.
  • Blood tests for estradiol are needed on treatment; the level, not the pill, is what the clinic should track.

The research
behind it.

In men on testosterone therapy with aromatase-driven estradiol elevation, anastrozole effectively lowers estradiol, but the goal is balance, not suppression. Your physician monitors this carefully.

Overuse of aromatase inhibitors in men causes low estradiol, which brings joint pain, loss of sexual interest, and bone density loss. This is why anastrozole is used judiciously, only when needed, and with ongoing lab monitoring.

Getting started
takes a few minutes.

  1. 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. 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. 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.

Start treatment

Frequently asked questions

Contact support
How do I take Anastrozole - Men?

Taken by mouth, twice a week. The starting prescription is 1 capsule (0.25 mg) each time. Your physician sets your own dose and it is printed on your label.

How much arrives in each shipment?

26 capsules at the starting strength, shipped to your door from a licensed US pharmacy.

When do I need anastrozole?

Only when your physician sees BOTH elevated estradiol on labs AND symptoms (water retention, gynecomastia, mood swings, erectile dysfunction). If your estradiol is normal or you have no symptoms, you don't need it. Your physician may adjust testosterone dose first, which can solve the problem without adding a second drug.

Why don't I just start anastrozole with testosterone?

Because most men do not have elevated estradiol from testosterone therapy alone, and adding an aromatase inhibitor to everyone would cause widespread low-estradiol problems (joint pain, bone loss, sexual dysfunction). Anastrozole is added only if labs show it is needed and you have symptoms.

What if my estradiol stays high?

Your physician may increase the anastrozole dose slightly or adjust your testosterone dose downward. Sometimes reducing testosterone is the answer—you still feel good on lower testosterone without needing a second drug. Your physician tries the simplest solution first.

Can low estradiol really be a problem?

Yes. Aromatase inhibitors used aggressively cause joint pain (especially knees and shoulders), loss of sexual interest, erectile dysfunction, mood swings, and reduced bone density. This is why anastrozole is used sparingly and with lab monitoring. The goal is normal balance, not suppression.

How long will I need it?

That depends. Some men need it only in the first few weeks while their body adjusts to testosterone. Others need it intermittently or for longer. Your physician reassesses at every check-in and adjusts the plan as your needs change.

Anastrozole educational content reviewed by our physician

Scott Nass, MD Doctor 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.

More options
in this area.

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    Gonadorelin

    A copy of the brain's own GnRH signal that keeps the testes producing testosterone and sperm, used alongside testosterone therapy and in fertility care. Prescribed and dosed by a licensed physician.

    Starting at $159/mo

  • Capsule

    Anastrozole Capsules

    Anastrozole, an aromatase inhibitor used in men to control estrogen levels during testosterone therapy. Prescribed and dosed by a licensed physician.

    9 capsules per month

    Starting at $63/mo

  • Tablet

    Anastrozole Tablets

    FDA-approved anastrozole tablets, an aromatase inhibitor used at low doses in men on testosterone therapy whose estradiol runs high. Prescribed by a licensed physician only after blood work.

    5 tablets per month

    Starting at $63/mo

  • Dissolving tablet

    Cabergoline Tablets

    Cabergoline, a dopamine agonist used to manage prolactin levels. Commercial formulation, prescribed and dosed by a licensed physician. Requires periodic monitoring for valvular heart disease with long-term use.

    Starting at $239/mo

References

  1. 1.Effects of aromatase inhibition on bone mineral density and bone turnover in older men with low testosterone levels. J Clin Endocrinol Metab, 2009
  2. 2.Testosterone Therapy in Men With Hypogonadism: An Endocrine Society Clinical Practice Guideline. J Clin Endocrinol Metab, 2018

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.