Compound profile

Methasterone

Also known as Superdrol, Methyldrostanolone

Not approved
  • Anabolic steroids
  • Oral (tablet)
  • DHT derivative

Last reviewed October 2026

Educational only. A summary of published research, not medical advice or a recommendation. No doses are listed.

Quick take

A potent oral “designer” steroid once sold as a supplement, and linked to serious liver injury.

Class
Anabolic steroids
Status
Not approved
Evidence
Mostly animal & lab studies
Half-life
Not well documented

Mechanism fingerprint

What it acts on, and how. Each chip links to that pathway on the map.

A 17α-methylated form of drostanolone, so it works as a tablet and is hard on the liver.

What makes it different

A 17α-methylated form of drostanolone once sold as a “supplement”, and linked to serious liver injury.

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Mechanism & pathways

Methasterone
  • Agonist Androgen receptor

    Receptor for testosterone and DHT. Activating it builds muscle and drives male traits such as body hair and a deeper voice. Every anabolic steroid binds it.

See Methasterone on the pathway map

Evidence overview

Mostly animal & lab studies

Never tested in proper human trials; human information comes from case reports, many describing severe liver injury.

A breakdown into human, animal and cell studies hasn't been added for this compound yet.

Why it's used

Sold as a supplement for fast gains in size and strength, before it became a controlled substance.

Side effects & risks

Reported side effects

  • Lower HDL (“good”) cholesterol
  • Raised blood pressure
  • Fatigue and loss of appetite
  • Lower libido

Risks and warnings

  • Case reports of severe cholestatic liver injury with jaundice, some needing hospital care
  • Oral 17α-alkylated steroid: can injure the liver, including cholestatic jaundice, blood-filled cysts (peliosis hepatis) and liver tumors.
  • Lowers HDL (“good”) cholesterol and raises LDL, adding to heart disease risk.
  • Shuts down the body's own testosterone production: testicles shrink and sperm counts fall, and recovery after stopping can take months or be incomplete.
  • In women: masculinizing effects (deeper voice, facial and body hair, clitoral enlargement) that can be permanent.
  • Schedule III controlled substance in the US: illegal to possess without a prescription.
  • Prohibited in sport by the World Anti-Doping Agency (WADA).

FAQ

Short answers taken from this profile.

What is Methasterone?

A potent oral “designer” steroid once sold as a supplement, and linked to serious liver injury.

How does Methasterone work?

A 17α-methylated form of drostanolone, so it works as a tablet and is hard on the liver.

What receptors or pathways does Methasterone act on?

androgen receptor (agonist).

How is Methasterone different from similar compounds?

A 17α-methylated form of drostanolone once sold as a “supplement”, and linked to serious liver injury.

Is Methasterone approved?

Never approved as a medicine. Sold in the mid-2000s as a “prohormone” supplement; the DEA made it a Schedule III controlled substance in 2012.

What has Methasterone been studied for?

Sold as a supplement for fast gains in size and strength, before it became a controlled substance.

How strong is the evidence?

Mostly animal & lab studies. Never tested in proper human trials; human information comes from case reports, many describing severe liver injury.

What are the main risks?

Case reports of severe cholestatic liver injury with jaundice, some needing hospital care. Oral 17α-alkylated steroid: can injure the liver, including cholestatic jaundice, blood-filled cysts (peliosis hepatis) and liver tumors. Lowers HDL (“good”) cholesterol and raises LDL, adding to heart disease risk. More are listed under risks and warnings.

Sources

  • Shah NL et al. Methasteron-associated cholestatic liver injury: clinicopathologic findings in 5 cases. Clin Gastroenterol Hepatol 2008.
  • DEA, 2012: placement of methasterone and prostanozol into Schedule III.
  • LiverTox (NIH): Androgenic steroids.