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Anastrozole_Dosage, benefits & legal status

Also known as Arimidex, ANA, anastrozol

Published August 24, 2026 · Updated October 5, 2026

An aromatase inhibitor approved for postmenopausal breast cancer.

Estrogen controlAromatase inhibitor (oral, not a peptide)FDA-approvedNot a peptide
Dose1 mg per day
FrequencyDaily
RouteBy mouth (oral)
StatusFDA-approved
CycledContinuous, for years in the trials

Common vial size is what vendors typically sell, not a recommendation. Enter your own vial in the calculator.

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01

What is Anastrozole?

Plain language first. The technical label stays, but it never stands alone.

Overview

It stops the body making estrogen in the first place, so estrogen levels fall.

The technical version

Anastrozole is a non-steroidal aromatase inhibitor that blocks the enzyme converting androgens into estrogen, lowering circulating estrogen rather than blocking its receptor.

What it's used for

A breast cancer drug used on the research market to hold estrogen down during a testosterone or anabolic cycle.

02

How does Anastrozole work?

What it does in the body, and where.

Anastrozole works upstream of the receptor, on supply rather than on signal.

  1. 01
    It blocks aromatase
    Aromatase is the enzyme that turns androgens into estrogen.
  2. 02
    Circulating estrogen falls
    In postmenopausal women almost all remaining estrogen comes through this route, which is why the drug works there.
  3. 03
    Every tissue that needed estrogen notices
    Bone is the clearest one. Estrogen protects bone, and the trials measured bone loss within a year.
  4. 04
    It does nothing to the receptor itself
    This is the practical difference from tamoxifen, and the reason the label says not to take the two together.
Pathway
THE PEPTIDE
Anastrozole
ACTS ON
The aromatase enzyme
RESULT
Estrogen production falls
RESULT
Bone density falls with it

A schematic of the compound's mechanism, not a diagnostic image.

03

What else is it used for?

Each use below carries its own evidence level. Approved means regulators have cleared it for that purpose. Investigational means it is in trials. Early research means it is being studied and is not established.

  • Hormone receptor-positive breast cancer in postmenopausal womenFDA-approved
  • Holding estrogen down during testosterone therapy, off-labelClinical use
  • Controlling estrogen during an anabolic cycleResearch only

The published record

Research index

3,041

Papers and trials about Anastrozole

428 papers tagged human · 289 not reviews or lab · 126 clinical trial publications

494 registered trials · 31 with posted results

Furthest stage reached: Approved in the US

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Category 1, component of an FDA-approved drugRegulators
In animals42
In the lab3
Reviews51
Senior author shareSpread across many groups

Evidence summary

Counted from Europe PMC indexing, not read by a person; a human tag can land on reviews, commentary or lab papers; clinical trial publications is the narrower count. 500 papers and 100 trials indexed in detail.

Anastrozole vial rendering
Compound field notes

At a glance

Four things to know about Anastrozole

01

Evidence

FDA-approved

02

Category

Sexual and hormonal

03

Common vial

Varies

04

Half-life

About 50 hours

04

How much, and do you cycle it?

The range, and whether you take breaks.

1 mg per day, daily. Continuous, for years in the trials FDA label

Given daily and without a break for the duration of treatment. The intermittent twice-weekly dosing used alongside testosterone is a community pattern built around symptom control rather than anything from a trial.

Source: Arimidex prescribing information, DailyMed

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05

How long does it stay in the body?

The half-life, and where the figure comes from.

About 50 hoursFDA label

Mean terminal elimination half-life in postmenopausal women. Cleared mainly by the liver, about 85 percent, with roughly 10 percent through the kidneys. In children the label reports 46.8 hours, which is close enough to be the same figure.

Source: Arimidex label, section 12 Clinical Pharmacology, Excretion

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06

What does it cost?

Typical dose and cost, in plain numbers.

Anastrozole is not injected

It is taken by mouth (oral). The label is a single 1 mg tablet once a day, in every approved indication. The much smaller and less frequent doses used alongside testosterone, often a fraction of a tablet twice a week, are not on the label and were never studied for that purpose.

Cost per month
—
Cost per dose
—
Typical dose
1 mg–1 mg / dayFDA label
What it costs

Anastrozole starts at $64.03 across 4 vendors, typically $109.99 per mg.

5 listings, last read Oct 10, 2026. Shipping and card fees are not included.

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07

How do you store it?

Before mixing, and after.

Room temperature. Cool, dry, out of light.

Anastrozole is taken as a pill or capsule. Keep it in its original container at room temperature, away from heat, humidity, and direct sun. No fridge or mixing needed. Check the expiration date on the bottle.

08

What are the side effects and cautions?

Known cautions and warnings for this compound.

Who should avoid it

Check these before anything else.
  • Pregnancy
  • Existing osteoporosis or low bone density, without a plan to manage it
  • Known hypersensitivity to anastrozole
  • Pre-existing ischaemic heart disease, where the label notes more ischaemic events on anastrozole than on tamoxifen
  • Banned in drug-tested sport

Stop and get help

These are emergencies. Seek care.
  • Chest pain, or new breathlessness on exertion
  • A bone fracture from a minor fall or knock
  • Severe joint pain that stops you using a hand or walking
  • Signs of an allergic reaction such as face or throat swelling, hives, or trouble breathing

Common effects

Expected, and usually mild.
  • Joint pain and stiffness
  • Hot flushes
  • Fatigue
  • Low mood
  • Rising cholesterol
  • Falling bone density over months

Where this page says nothing is established, that means nobody has studied it, not that a compound is safe.

09

Is Anastrozole approved?

And where the numbers on this page come from.

Yes. Anastrozole is FDA approved and available on prescription in the United States.

What has happened recently

First approved in the US in 1995, for hormone receptor-positive breast cancer in postmenopausal women. There is no approved use in men and none in premenopausal women. The label warns on bone mineral density and on total cholesterol, and reports that in women with pre-existing ischaemic heart disease, ischaemic cardiovascular events were more common on anastrozole than on tamoxifen. It also says not to combine it with tamoxifen, because no added benefit was seen over tamoxifen alone. Prohibited in sport at all times by WADA under section S4.

What regulators say

From official documents

Banned in drug-tested sport. Most research peptides are prohibited under WADA's S0 category, which covers any substance with no approval from any regulatory authority for human use. That means a compound can be banned without ever being named on the prohibited list. Check with your own anti-doping authority rather than assuming absence from the list means permitted.

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Guides for this compound

Sources

Beyond these, 600 records are indexed. Browse the records