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Superdrol, known generically as methasterone, is a synthetic, orally active anabolic-androgenic steroid derived from dihydrotestosterone. First prepared in the 1950s but never developed as a medicine, it later resurfaced as a designer steroid sold over the counter as a bodybuilding supplement. It is now a controlled substance and is noted chiefly for pronounced liver toxicity.
- Rapid strength gains
- Dry lean mass
- Extremely potent oral
- Non-aromatizing
- Hard on liver and lipids
- Liver injury, including cholestatic jaundice
- Unfavorable changes in blood cholesterol
- Suppression of natural testosterone production
- Raised blood pressure
- Isolated reports of kidney injury
Overview
Superdrol is a brand and street name for methasterone, a 17alpha-methylated anabolic-androgenic steroid with the molecular formula C21H34O2 [1]. Structurally it is a derivative of dihydrotestosterone that carries extra methyl groups at the 2alpha and 17alpha positions, formally named 2alpha,17alpha-dimethyl-5alpha-dihydrotestosterone [1]. The 17alpha-methyl group lets the molecule survive first-pass breakdown in the liver, which gives it useful oral activity but also contributes to its liver toxicity [1][4].
The compound was first synthesized by chemists at Syntex in the mid-1950s during a program exploring steroid analogs, and a 1959 report described it as a potent orally active anabolic agent with comparatively weak androgenic effects [1]. It then drew little attention until 2005, when it was introduced to the United States supplement market under the name Superdrol [2]. Sold as a dietary supplement rather than a drug, it was promoted as building muscle without hormonal activity, a claim that later clinical case reports directly contradicted [2].
Because it was available without a prescription, methasterone reached recreational users seeking rapid gains in muscle mass and strength, and much of the medical literature on it consists of case reports describing harm rather than trials of benefit [2][3]. Published cases document cholestatic jaundice, prolonged liver injury, and in one instance IgA nephropathy following use of products containing the steroid [2][3]. Anti-doping and analytical laboratories have separately characterized how it is metabolized and excreted so that it can be identified in urine testing [4].
Regulators responded as these products spread. Methasterone is now controlled as a Schedule III substance under United States law, and the World Anti-Doping Agency prohibits it in sport, where laboratories screen for its metabolites [4]. Despite these controls it has periodically reappeared in grey-market preparations, typically sold as oral tablets or capsules, and it has no recognized medical indication.
- Though first synthesized in the 1950s, methasterone was never approved as a medicine and only became widely known after being sold as the supplement Superdrol around 2005.
- The 17-alpha-methyl group that lets methasterone survive first-pass liver metabolism, and thus work as a pill, is also the feature most associated with its liver toxicity.
- Laboratory analyses have found methasterone hidden as an undeclared ingredient in products marketed as ordinary B-vitamin and mineral supplements.
Mechanism
As an anabolic-androgenic steroid, methasterone acts by binding the in muscle and other tissues, where it mimics endogenous androgens such as testosterone and dihydrotestosterone to drive protein synthesis and muscle growth [1]. Early characterization reported a high anabolic-to-androgenic ratio, meaning its tissue-building effects were strong relative to classic androgenic effects [1].
The same 17alpha-methyl substitution that allows it to survive liver metabolism, and therefore to work when swallowed, is also the feature most tied to its hepatotoxicity; oral 17alpha-alkylated steroids of this class are repeatedly linked to cholestatic liver injury, in which bile flow is impaired [2][3]. Beyond the liver, reported consequences of use include suppression of the body's own testosterone production, unfavorable shifts in blood lipids, and, in isolated reports, kidney injury [2][3].
receptor fingerprint
potent agonist
Muscle protein synthesisstrongly raises
Liver (17-alpha-alkylated)stresses
Safetyrisks and cautions, not medical advice
Superdrol (methasterone) is an oral 17-alpha-alkylated anabolic-androgenic steroid and is not a legitimate medicine. It is markedly hepatotoxic, with reported cases of cholestatic liver injury and liver failure, and it strongly suppresses the hypothalamic-pituitary-testicular axis, sharply lowers HDL cholesterol while raising blood pressure, and worsens cardiovascular risk. Additional harms include mood changes and aggression, and virilizing effects in women; its use carries serious, well-documented dangers.
Interactionsdocumented pairs only, not exhaustive
Superdrol (methasterone) is an unapproved oral 17-alpha-alkylated anabolic-androgenic steroid with no formal drug label, so its interactions are inferred from the well-documented anabolic-steroid class. Like other 17-alpha-alkylated oral steroids it potentiates the effect of warfarin and other coumarin anticoagulants, raising bleeding risk and requiring reduced anticoagulant dosing, a class interaction described for oxandrolone and methyltestosterone. Its marked hepatotoxicity, including cholestatic injury and peliosis, is additive with other hepatotoxic drugs and alcohol. Anabolic steroids can also increase sensitivity to insulin and oral hypoglycemics and may antagonize the fluid-balance effects of corticosteroids. This is research information, not medical advice.
Checking a whole stack? Run it through interactions + stacks.
History
Methasterone was first prepared in the 1950s during the intensive era of steroid chemistry, when companies such as Syntex synthesized and characterized large numbers of anabolic-androgenic derivatives of dihydrotestosterone. Early reports described it as having a high anabolic-to-androgenic ratio, yet unlike many of its contemporaries it was never developed or marketed as an approved medicine. The compound resurfaced decades later, around 2005, when it was sold over the counter as a designer steroid and bodybuilding supplement under the name Superdrol, marketed as a legal alternative to prescription anabolics.
Mounting reports of liver injury and its clearly androgenic nature drew regulatory attention, and it was ultimately brought under control as a scheduled anabolic steroid in the United States, a status reinforced by the Designer Anabolic Steroid Control Act of 2014. Analytical studies have since documented methasterone turning up as an undeclared ingredient in products sold as ordinary dietary supplements.
Reputation
Superdrol carries a reputation within bodybuilding circles as an unusually potent oral compound capable of producing rapid gains in muscle size and strength, and this potency is the basis of its notoriety. In the scientific and medical literature, however, it is far better known as a cautionary example: an orally active 17-alpha-alkylated steroid repeatedly linked to cholestatic liver injury, unfavorable shifts in blood lipids, and suppression of the body's own testosterone.
Its history as a covertly sold designer steroid, sometimes hidden in products labeled as vitamins, has made it a frequent subject of doping-control and public-health investigations. An honest account credits its strong androgen-receptor activity while emphasizing that the same chemical feature enabling oral use is the one most tied to its liver toxicity. It stands today as a controlled substance rather than a legitimate therapeutic agent.
Subjective profileweighing the evidence above
Hard pass. Cholestatic liver injury and liver failure are documented, HDL falls sharply, blood pressure rises and natural testosterone shuts down. The strength and dry mass are real; they are not worth a liver. It was never developed as a medicine and was only ever sold as a supplement because nobody was checking.
Resources
Don't even think about it.
Research
- 1956first citedSteroids. LXXXIII. Synthesis of 2-Methyl and 2,2-Dimethyl Hormone Analogs (Ringold and Rosenkra…
- 2023most recentAndrogen receptor blockade by flutamide down-regulates renal fibrosis, inflammation, and apopto…
- 1.Steroids. LXXXIII. Synthesis of 2-Methyl and 2,2-Dimethyl Hormone Analogs (Ringold and Rosenkranz, 1956)
- 2.Cholestatic jaundice and IgA nephropathy induced by OTC muscle building agent superdrol.
- 3.Methasteron-associated cholestatic liver injury: clinicopathologic findings in 5 cases.
- 4.Metabolism and excretion of anabolic steroids in doping control--new steroids and new insights.
- 5.Androgenic steroids in Over-the-Counter dietary Supplements: Analysis for association with adverse health effects
- 6.In vitro and in vivo metabolism studies of dimethazine
- 7.A comparative study of the effect of the dose and exposure duration of anabolic androgenic steroids on behavior, cholinergic regulation, and oxidative stress in rats
- 8.Human steroid biosynthesis, metabolism and excretion are differentially reflected by serum and urine steroid metabolomes: A comprehensive review
- 9.Human hydroxysteroid dehydrogenases and pre-receptor regulation: insights into inhibitor design and evaluation
- 10.The anabolic androgenic steroid fluoxymesterone inhibits 11β-hydroxysteroid dehydrogenase 2-dependent glucocorticoid inactivation
- 11.Influence of muscle mass and physical activity on serum and urinary creatinine and serum cystatin C
- 12.Androgen receptor blockade by flutamide down-regulates renal fibrosis, inflammation, and apoptosis pathways in male rats
13 listed here; entry last updated August 2026
Reviews
My notesprivate to this device
FAQ
What is Superdrol?
It is a very potent oral anabolic steroid (methasterone) known for rapid gains in strength and lean size. It is not an approved medicine.
Why is it considered harsh?
It is notably hard on the liver and can worsen cholesterol significantly. These risks are a major concern with oral steroids.
Does it suppress natural hormones?
Yes, it strongly suppresses the body's own testosterone. Recovery of natural production is a common concern afterward.
Is it legal in sport?
No, it is banned by anti-doping agencies and is a controlled substance in many places. It is not approved for human use.
Adverse effects
- Liver injury, including cholestatic jaundice
- Unfavorable changes in blood cholesterol
- Suppression of natural testosterone production
- Raised blood pressure
- Isolated reports of kidney injury