Formestane (4-hydroxyandrostenedione)

CGP-32349, Lentaron, 4-OHA, 4-OH-androstenedione

Forms: Historically a depot injection for breast cancer (Lentaron); in sport, unregulated creams and capsules.

Hormone control & recoveryNot approved for humansWADA S4 · prohibitedEvidence: limited human data

A steroidal aromatase inhibitor that disables the enzyme permanently. Once a breast-cancer injection that paved the way for today's oral inhibitors; in sport, sold as unregulated creams.

What it gives

What people use it for and what the sources report. Strength is a general category from the literature: mild, clear or strong.

Purpose

It was the first selective aromatase inhibitor on the market, given by injection for advanced breast cancer after menopause, and was later withdrawn. In sport, steroid users apply creams or take capsules to curb estrogen from aromatizing steroids; these products are not approved medicines.

What people seek and what studies show

In postmenopausal women with breast cancer the injection lowered estradiol and worked about as well as tamoxifen. In men, and for creams or capsules, there are no studies of effects or safety: human data come from anti-doping work, such as a single skin application in six volunteers to track its breakdown. In lab tests it and several metabolites acted as androgens.

Effects

Side-effect control

Evidence: Limited human data — some human studies, small or short

Possible side effects

Possible does not mean certain: whether they appear depends on dose, duration, individual response and monitoring. Below — what to watch for and how to notice it early.

5 possible side effects

level · how often it is reported
Moderate
Unknown long-term safety (little human data)
Creams and capsules have never been studied in men; effects and long-term safety outside the old breast-cancer injection are unknown.
How to notice: Nothing to notice — the risk is what is not yet known.
common
Moderate
Black-market quality risk (fakes, contamination)
Products on the market are not approved medicines; content and strength are unverified.
How to notice: Unexpected effects, pain or infection, a stronger or weaker effect than expected.
common
Moderate
Too-low estrogen (joints, libido, mood, lipids)
If it works as sold, estradiol can drop too low: aching joints, low libido, flat mood and, over time, bone loss. Unknown product strength makes this hard to judge.
How to notice: Aching, stiff joints, low libido, flat mood, poor sleep.
possible
MenLow
WomenElevated
Virilization in women (often irreversible)
It and its metabolites acted as androgens in lab tests; women may notice a deeper voice or new facial hair, which can become permanent. Human data are lacking.
How to notice: Hoarse or deeper voice, new facial or body hair, menstrual changes, clitoral enlargement.
rare
MenLow
WomenModerate
Acne, oily skin
It and several of its metabolites acted as androgens in lab tests, so it may add to androgenic effects such as acne; human data are lacking.
How to notice: Oily skin, spots on back, shoulders and face.
possible

What the levels mean

Lowbackground — just be aware
Moderatewatch for signs
Elevatedneeds regular control
Highcritical — can be life-threatening or permanent

Level: general category from the literature, not your personal risk

How often

common
reported often
possible
reported in some people
rare
reported occasionally

How to lower the risks

For 3 of 5 possible side effects there are specific ways to lower the chance: everyday measures, supplements and options a doctor may consider. For the rest — general advice. No measure removes a risk completely.

ModerateUnknown long-term safety (little human data)

What is unknown cannot be lowered, only avoided; tell your doctor what you have taken.

ModerateBlack-market quality risk (fakes, contamination)

Products obtained without a prescription are often fake, mislabeled or non-sterile, and there is no way to check at home. For legal supplements, look for third-party testing (Informed Sport, NSF).

ModerateToo-low estrogen (joints, libido, mood, lipids)

Avoid controlling estrogen blindly; adjust only by blood tests with a doctor.

Measure
Regular blood tests
How each option helps (1)
  • Regular blood tests — Testing ends guesswork use of aromatase inhibitors — prescription drugs that can push estrogen too low and harm joints, libido, mood and lipids.
MenLow
WomenElevated
Virilization in women (often irreversible)

Stop at the first voice change and see a doctor — early stopping matters.

Measure
Working with a doctor
How each option helps (1)
  • Working with a doctor — Steroid labels say to stop at the first mild signs (hoarse voice, facial hair, clitoral growth) to prevent permanent change; checks catch them early but do not make use safe.
MenLow
WomenModerate
Acne, oily skin

Gentle skin care, cleansing after training, a dermatologist if it spreads.

Supplement or OTC product
How each option helps (3)
  • Adapalene — Reduces spots in many users. Redness, scaling, dryness and stinging are common early and usually ease; acne may look worse at first. Rarely, allergic swelling.
  • Benzoyl peroxide — A first-line acne option. Dryness, redness and peeling are common at first; it bleaches hair and fabric; rarely, serious allergic reactions. Severe steroid acne needs a dermatologist.
  • Zinc — Trials show a modest drop in inflamed spots, weaker than antibiotics; steroid acne is driven by androgens.

Check-ups and blood tests

Which tests and check-ups to do and when. This is a guide — agree the exact schedule with your doctor.

Baseline tests
your own starting values — every later result is compared with them
Lipid panel (HDL, LDL, triglycerides, ApoB)low estrogen
Testosterone (total, free), LH, FSH, SHBG
Estradiol (sensitive assay)low estrogen
While taking
about 4–6 weeks in, then every 6–8 weeks — agree the exact schedule with your doctor
Lipid panel (HDL, LDL, triglycerides, ApoB)low estrogen
Estradiol (sensitive assay)low estrogen
After stopping
4–8 weeks after stopping (later after long-acting injections), then until values return to baseline
Lipid panel (HDL, LDL, triglycerides, ApoB)low estrogen
Testosterone (total, free), LH, FSH, SHBG

Which doctors can help

Sports physiciancoordinates everything
Endocrinologistlow estrogen
Gynecologistvirilization (women)
Dermatologistacne (women)

Get medical help at once if

  • Deepening voice, new facial hair, clitoral enlargement — stop and see a doctor: changes can become permanent. (women)

In an emergency, call your local emergency number.

For women

Before menopause the ovaries answer an aromatase inhibitor by making more hormones, so the effect is unpredictable; its androgenic activity in lab tests is a further concern.

Myth & fact

Myth

“Formestane is natural because the body makes it, so a cream is harmless.”

Fact

Traces can form in the body, which is why anti-doping labs use isotope tests, but the products deliver a withdrawn breast-cancer drug in unknown amounts. Positive tests were confirmed at the Rio 2016 Games.

Combinations

No specific combination notes for this substance yet. The stack check still adds up side effects that several substances share.

Check combinations →

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