Methasterone

updated

Methasterone (Superdrol) is an oral anabolic steroid with no approved medical use, classified as a Schedule III controlled substance in the US since 2012. No controlled human trial of its effects was found, and the published record is case reports of cholestatic liver injury and kidney injury, including a 52-case review of anabolic steroid liver injury. Its potency claim traces to castrated rat and in vitro assays, and it has turned up undeclared in vitamin capsules.

17-alpha-alkylated oral anabolic-androgenic steroid

  • DEA classified methasterone as a Schedule III anabolic steroid in a final rule published 30 July 2012 (77 FR 44456), effective 29 August 2012; it is listed at 21 CFR 1308.13(f)(48).
  • A Drugs@FDA query and a DailyMed search on 9 October 2026 returned no application and no label, so there is no approved medical product in the US record.
  • A PubMed search on 9 October 2026 for controlled-trial terms returned 1 record, an antidoping urine study in 2 volunteers; ClinicalTrials.gov searches returned no studies.
  • In a review of 52 cases of anabolic steroid liver injury, the most common steroid was methyldrostanolone, median peak bilirubin was 705 micromol/L and 43% developed kidney injury; no patient died or needed a liver transplant.
  • Every potency figure comes from castrated rat and in vitro assays, not from people.
  • Methasterone appeared undeclared in B-50 vitamin and multimineral capsules from one supplier, with one resident hospitalized for liver damage.

What is methasterone, and what is its legal status?

Methasterone (Superdrol) is a 17-alpha-alkylated oral anabolic steroid that DEA classified as a Schedule III controlled substance in 2012. There is no approved medical product and no label in the US record.

Methasterone is controlled in the United States. DEA classified it as an anabolic steroid under 21 U.S.C. 802(41)(A) in a final rule published 30 July 2012 (77 FR 44456), effective 29 August 2012, making it, with its salts, esters and ethers, a Schedule III controlled substance. 21 CFR 1308.13(f)(48) lists it among the Schedule III anabolic steroids in the text for the 2026-10-01 edition, and possession and distribution are controlled accordingly.

A Drugs@FDA query on 9 October 2026 for products with methasterone as an active ingredient returned no matching application, and a DailyMed search returned no labels. There is no approved medical product and no label anywhere in the US record. Status outside the United States is not covered here.

Methasterone is PubChem CID 237186, C21H34O2, molecular weight 318.5 g/mol, CAS 3381-88-2. Listed synonyms include Superdrol, methyldrostanolone, 17-methyldrostanolone, methasteron and NSC 40490. Chemically it is 2alpha,17alpha-dimethyl-5alpha-androstan-17beta-ol-3-one, a 17-alpha-alkylated oral derivative of drostanolone.

DEA final rule, 30 July 2012 (77 FR 44456): Schedule III

Regulatory record

Drug Enforcement Administration. Classification of Two Steroids, Prostanozol and Methasterone, as Schedule III Anabolic Steroids Under the Controlled Substances Act. Final rule, 77 FR 44456, published 30 July 2012, effective 29 August 2012.

DEA classified methasterone as an anabolic steroid under 21 U.S.C. 802(41)(A), making it, with its salts, esters and ethers, a Schedule III controlled substance. The rule records that methasterone synthesis was reported in 1956 and anabolic activity in 1959; that it was described as a potent anabolic agent with weak androgenic activity in the castrated male rat; that Zaffaroni and coworkers reported one fifth the androgenic and four times the anabolic activity of methyltestosterone given orally to the experimental animal; that in castrated male rats, by subcutaneous and oral routes, it prevented atrophy of ventral prostate, seminal vesicles, and levator ani muscle to a degree comparable to testosterone and methyltestosterone; and that it bound the androgen receptor comparably to testosterone and showed increased activity relative to testosterone in a transactivation assay. The rule also states that a review of the scientific literature finds adverse health effects including liver toxicity with renal failure reported in conjunction with methasterone abuse, and that FDA issued a Warning Letter in March 2006 in response to adverse health effects associated with the product Superdrol.

Participants / model
Castrated male rats and receptor assays; US legal status
Treatment
Subcutaneous and oral dosing in rats
Follow-up
Rule effective 29 August 2012
Study design
Official Federal Register final rule
Funding
not stated in the source

Every potency figure in this record is from castrated rat and in vitro assays, not from people.

Read the original source
21 CFR 1308.13(f)(48): methasterone listed in Schedule III

Regulatory record

Electronic Code of Federal Regulations. 21 CFR 1308.13, Schedule III, paragraph (f)(48), text for the 2026-10-01 edition.

21 CFR 1308.13(f)(48) lists methasterone (2alpha,17alpha-dimethyl-5alpha-androstan-17beta-ol-3-one, or 2alpha,17alpha-dimethyl-17beta-hydroxy-5alpha-androstan-3-one) among the Schedule III anabolic steroids. Possession and distribution in the US are controlled accordingly. A Drugs@FDA query on 9 October 2026 for products with methasterone as an active ingredient returned no matching application, and a DailyMed search returned no labels, so there is no approved medical product and no label anywhere in the US record.

Participants / model
US legal status, not a clinical population
Treatment
Any form
Follow-up
Text for the 2026-10-01 edition
Study design
Official CFR text
Funding
not stated in the source

The scheduling entry is a legal classification. The Drugs@FDA and DailyMed searches are dated and US-scoped.

Read the original source
PubChem: methasterone (Superdrol) identity

Chemical identity record

National Library of Medicine. PubChem compound record CID 237186 (methasterone).

Methasterone: PubChem CID 237186, C21H34O2, molecular weight 318.5 g/mol, CAS 3381-88-2. Listed synonyms include Superdrol, methyldrostanolone, 17-methyldrostanolone, methasteron, and NSC 40490. Chemically it is 2alpha,17alpha-dimethyl-5alpha-androstan-17beta-ol-3-one, a 17-alpha-alkylated oral derivative of drostanolone. The 17-alpha methyl group is what makes it orally active and is the chemical feature shared by the oral androgens associated with cholestatic liver injury.

Participants / model
Chemical identity, not a clinical population
Treatment
Defined molecule
Follow-up
Not applicable
Study design
NLM chemical record
Funding
not stated in the source

Identity record only; it says nothing about efficacy or safety.

Read the original source

Have any controlled human trials of methasterone been done?

None were found. A PubMed search on 9 October 2026 returned 1 record, an antidoping urine study in 2 volunteers that measured detection windows only, and ClinicalTrials.gov searches returned no studies.

A PubMed search on 9 October 2026 for methasterone, methyldrostanolone or Superdrol combined with randomized, randomised, placebo, clinical trial as a publication type, healthy volunteers, lean body mass or strength returned 1 record. ClinicalTrials.gov searches for methasterone and for Superdrol on the same date returned no studies.

That one record is an antidoping excretion study in which healthy volunteers each ingested one tablet of the drug and urine was collected over 50 days. Two new methasterone metabolites were identified, and a named metabolite was detectable as a glucuronide in urine from both volunteers up to 50 days after administration. The study measured detection windows only. It reports no efficacy, body composition, lipid, blood pressure or safety outcome.

No controlled trial of methasterone in humans exists in the records found: there is no measured gain in lean mass, no measured strength result, no lipid panel, no blood pressure measurement and no systematic adverse event collection. Everything known about its effects in people comes from case reports of harm and from analytical chemistry.

PubMed search, 9 October 2026: 1 record, an antidoping urine study

PubMed search record

PubMed search run on 9 October 2026: (methasterone OR methyldrostanolone OR superdrol) AND (randomized OR randomised OR placebo OR clinical trial[pt] OR healthy volunteers OR lean body mass OR strength). 1 record returned.

The search returned 1 record, the antidoping urinary excretion study. ClinicalTrials.gov searches for methasterone and for Superdrol on the same date returned no studies. No controlled trial of methasterone in humans exists in the records found: there is no measured gain in lean mass, no measured strength result, no lipid panel, no blood pressure measurement, and no systematic adverse event collection. Everything known about its effects in people comes from case reports of harm and from analytical chemistry.

Participants / model
Records returned, not a population
Treatment
Not applicable
Follow-up
Search run on 9 October 2026
Study design
Literature and registry search
Funding
not stated in the source

A search result shows what PubMed and ClinicalTrials.gov returned on that date. It is not proof that no unindexed study exists.

Read the original source
Antidoping study: 2 volunteers, metabolite detectable up to 50 days

Human study

Zheng S et al. Anal Chem. 2025;97(5):3009-3018. PMID 39883123.

Healthy volunteers each ingested one tablet of the drug and urine was collected over 50 days. Two new methasterone metabolites were identified, and the metabolite 18-nor-17beta-hydroxymethyl-2alpha,17alpha-dimethyl-5alpha-androst-13-en-3-one was detectable as a glucuronide in urine from both volunteers up to 50 days after administration.

Participants / model
Healthy volunteers, 2 for the methasterone arm
Treatment
Single oral tablet
Follow-up
Urine collected over 50 days
Study design
Analytical human excretion study
Funding
not stated in the source

The study measured detection windows only. It reports no efficacy, body composition, lipid, blood pressure, or safety outcome.

Read the original source

Is methasterone an extremely potent oral for dry gains?

Its potency figures come from castrated rat and in vitro assays, and no human study measured gains. Of the supplier's warnings, liver injury is supported, lipid effects only by class evidence, and no source was found for blood pressure or lethargy.

Sellers describe methasterone as an extremely potent oral for dry gains, with severe liver, lipid, blood pressure and lethargy concerns.

The potency claim traces to animal and cell assays. The DEA rule records that methasterone was described as a potent anabolic agent with weak androgenic activity in the castrated male rat, and that Zaffaroni and coworkers reported one fifth the androgenic and four times the anabolic activity of methyltestosterone given orally to the experimental animal. Anabolic activity was reported in 1959. Every potency figure in that record is from castrated rat and in vitro assays, not from people, and no human measurement of lean mass or strength exists.

On the warnings, the liver concern is the best-supported statement in the records and is covered below. The lipid concern is supported only by class evidence from a different oral steroid. The records contain no source for the blood pressure or lethargy warnings, so this page does not state them as findings.

DEA final rule, 30 July 2012 (77 FR 44456): Schedule III

Regulatory record

Drug Enforcement Administration. Classification of Two Steroids, Prostanozol and Methasterone, as Schedule III Anabolic Steroids Under the Controlled Substances Act. Final rule, 77 FR 44456, published 30 July 2012, effective 29 August 2012.

DEA classified methasterone as an anabolic steroid under 21 U.S.C. 802(41)(A), making it, with its salts, esters and ethers, a Schedule III controlled substance. The rule records that methasterone synthesis was reported in 1956 and anabolic activity in 1959; that it was described as a potent anabolic agent with weak androgenic activity in the castrated male rat; that Zaffaroni and coworkers reported one fifth the androgenic and four times the anabolic activity of methyltestosterone given orally to the experimental animal; that in castrated male rats, by subcutaneous and oral routes, it prevented atrophy of ventral prostate, seminal vesicles, and levator ani muscle to a degree comparable to testosterone and methyltestosterone; and that it bound the androgen receptor comparably to testosterone and showed increased activity relative to testosterone in a transactivation assay. The rule also states that a review of the scientific literature finds adverse health effects including liver toxicity with renal failure reported in conjunction with methasterone abuse, and that FDA issued a Warning Letter in March 2006 in response to adverse health effects associated with the product Superdrol.

Participants / model
Castrated male rats and receptor assays; US legal status
Treatment
Subcutaneous and oral dosing in rats
Follow-up
Rule effective 29 August 2012
Study design
Official Federal Register final rule
Funding
not stated in the source

Every potency figure in this record is from castrated rat and in vitro assays, not from people.

Read the original source
PubMed search, 9 October 2026: 1 record, an antidoping urine study

PubMed search record

PubMed search run on 9 October 2026: (methasterone OR methyldrostanolone OR superdrol) AND (randomized OR randomised OR placebo OR clinical trial[pt] OR healthy volunteers OR lean body mass OR strength). 1 record returned.

The search returned 1 record, the antidoping urinary excretion study. ClinicalTrials.gov searches for methasterone and for Superdrol on the same date returned no studies. No controlled trial of methasterone in humans exists in the records found: there is no measured gain in lean mass, no measured strength result, no lipid panel, no blood pressure measurement, and no systematic adverse event collection. Everything known about its effects in people comes from case reports of harm and from analytical chemistry.

Participants / model
Records returned, not a population
Treatment
Not applicable
Follow-up
Search run on 9 October 2026
Study design
Literature and registry search
Funding
not stated in the source

A search result shows what PubMed and ClinicalTrials.gov returned on that date. It is not proof that no unindexed study exists.

Read the original source
52 cases of steroid liver injury: methyldrostanolone most common, bilirubin 705

Human study

Abeles RD et al. BMJ Open Gastroenterol. 2020;7(1). PMID 33214235.

Two new cases plus a comprehensive review identifying 50 further cases of anabolic androgenic steroid drug-induced liver injury were assessed with the updated RUCAM score. The most common steroid taken was methyldrostanolone. Patients presented a median 56 days after starting, and bilirubin peaked a median 28 days after stopping. Causality was unlikely in 1 (2%), possible in 31 (60%) and probable in 20 (38%). Median peak values were bilirubin 705 micromol/L, ALT 125 U/L, AST 71 U/L, ALP 262 U/L, GGT 52 U/L and INR 1.1. Liver biopsies showed bland canalicular cholestasis. 43% developed kidney injury with a peak creatinine of 225 micromol/L. Therapies included antipruritics, ursodeoxycholic acid, and corticosteroids. No patient died or required liver transplantation.

Participants / model
52 cases of anabolic androgenic steroid liver injury
Treatment
Oral anabolic androgenic steroids, most commonly methyldrostanolone
Follow-up
Median 56 days to presentation; bilirubin peak a median 28 days after stopping
Study design
Case reports plus systematic literature review, assessed with the updated RUCAM score
Funding
not stated in the source

The authors state that defining indications and proving efficacy for any of the therapies remains challenging. The cases are not all methasterone, though methyldrostanolone was the most common steroid.

Read the original source
Class evidence: stanozolol in 11 weight lifters, HDL cholesterol down 33%

Randomized controlled trial

Thompson PD et al. JAMA. 1989;261(8):1165-8. PMID 2915439.

Oral stanozolol, also a 17-alpha-alkylated androgen, reduced HDL cholesterol by 33% and the HDL2 subfraction by 71%, reduced apolipoprotein A-I by 40%, increased LDL cholesterol by 29%, and increased postheparin hepatic triglyceride lipase activity by 123%. Intramuscular testosterone reduced HDL cholesterol by only 9% and LDL cholesterol fell 16%. Weight gain was similar with both. The authors attribute the difference to the oral 17-alpha-alkylated route rather than androgenic potency.

Participants / model
11 male weight lifters
Treatment
Oral stanozolol versus intramuscular testosterone enanthate
Follow-up
Six weeks, crossover design
Study design
Randomized crossover trial
Funding
not stated in the source

This is stanozolol in 11 men, not methasterone, and it supports only the class pattern for oral 17-alpha-alkylated androgens.

Read the original source

How does methasterone work, and what does the body do with it?

Methasterone is a 17-alpha-alkylated androgen that bound the androgen receptor comparably to testosterone in a receptor assay. No human pharmacokinetic data exist beyond urinary metabolite detection windows.

Methasterone is a 17-alpha-alkylated oral derivative of drostanolone. The 17-alpha methyl group is what makes it orally active, and it is the chemical feature shared by the oral androgens associated with cholestatic liver injury.

In castrated male rats, by subcutaneous and oral routes, methasterone prevented atrophy of ventral prostate, seminal vesicles and levator ani muscle to a degree comparable to testosterone and methyltestosterone. It bound the androgen receptor comparably to testosterone and showed increased activity relative to testosterone in a transactivation assay. These are rat and in vitro findings, not human ones.

No human half-life, Tmax or bioavailability is available in the records found. The only human administration study measured urinary metabolites after a single tablet in 2 volunteers: a named metabolite was detectable as a glucuronide in urine from both volunteers up to 50 days after administration.

PubChem: methasterone (Superdrol) identity

Chemical identity record

National Library of Medicine. PubChem compound record CID 237186 (methasterone).

Methasterone: PubChem CID 237186, C21H34O2, molecular weight 318.5 g/mol, CAS 3381-88-2. Listed synonyms include Superdrol, methyldrostanolone, 17-methyldrostanolone, methasteron, and NSC 40490. Chemically it is 2alpha,17alpha-dimethyl-5alpha-androstan-17beta-ol-3-one, a 17-alpha-alkylated oral derivative of drostanolone. The 17-alpha methyl group is what makes it orally active and is the chemical feature shared by the oral androgens associated with cholestatic liver injury.

Participants / model
Chemical identity, not a clinical population
Treatment
Defined molecule
Follow-up
Not applicable
Study design
NLM chemical record
Funding
not stated in the source

Identity record only; it says nothing about efficacy or safety.

Read the original source
DEA final rule, 30 July 2012 (77 FR 44456): Schedule III

Regulatory record

Drug Enforcement Administration. Classification of Two Steroids, Prostanozol and Methasterone, as Schedule III Anabolic Steroids Under the Controlled Substances Act. Final rule, 77 FR 44456, published 30 July 2012, effective 29 August 2012.

DEA classified methasterone as an anabolic steroid under 21 U.S.C. 802(41)(A), making it, with its salts, esters and ethers, a Schedule III controlled substance. The rule records that methasterone synthesis was reported in 1956 and anabolic activity in 1959; that it was described as a potent anabolic agent with weak androgenic activity in the castrated male rat; that Zaffaroni and coworkers reported one fifth the androgenic and four times the anabolic activity of methyltestosterone given orally to the experimental animal; that in castrated male rats, by subcutaneous and oral routes, it prevented atrophy of ventral prostate, seminal vesicles, and levator ani muscle to a degree comparable to testosterone and methyltestosterone; and that it bound the androgen receptor comparably to testosterone and showed increased activity relative to testosterone in a transactivation assay. The rule also states that a review of the scientific literature finds adverse health effects including liver toxicity with renal failure reported in conjunction with methasterone abuse, and that FDA issued a Warning Letter in March 2006 in response to adverse health effects associated with the product Superdrol.

Participants / model
Castrated male rats and receptor assays; US legal status
Treatment
Subcutaneous and oral dosing in rats
Follow-up
Rule effective 29 August 2012
Study design
Official Federal Register final rule
Funding
not stated in the source

Every potency figure in this record is from castrated rat and in vitro assays, not from people.

Read the original source
Antidoping study: 2 volunteers, metabolite detectable up to 50 days

Human study

Zheng S et al. Anal Chem. 2025;97(5):3009-3018. PMID 39883123.

Healthy volunteers each ingested one tablet of the drug and urine was collected over 50 days. Two new methasterone metabolites were identified, and the metabolite 18-nor-17beta-hydroxymethyl-2alpha,17alpha-dimethyl-5alpha-androst-13-en-3-one was detectable as a glucuronide in urine from both volunteers up to 50 days after administration.

Participants / model
Healthy volunteers, 2 for the methasterone arm
Treatment
Single oral tablet
Follow-up
Urine collected over 50 days
Study design
Analytical human excretion study
Funding
not stated in the source

The study measured detection windows only. It reports no efficacy, body composition, lipid, blood pressure, or safety outcome.

Read the original source

What risks do the case reports show?

Case reports and a 52-case review describe severe cholestatic liver injury and kidney injury with methasterone and related oral steroids. In the review, median peak bilirubin was 705 micromol/L and 43% had kidney injury, and no patient died or needed a liver transplant.

The DEA rule states that a review of the scientific literature finds adverse health effects including liver toxicity with renal failure reported in conjunction with methasterone abuse, and that FDA issued a Warning Letter in March 2006 in response to adverse health effects associated with the product Superdrol.

In the largest case series, 5 previously healthy patients who used methasteron developed jaundice 2 weeks after discontinuation and presented to tertiary care 2 weeks later. Bilirubin peaked a further 2 to 3 weeks after presentation, and about 12 weeks after initial presentation all cases had resolved with no identifiable residual hepatic dysfunction. The authors note that liver failure can worsen after initial presentation, especially within 2 weeks.

One case report describes cholestatic jaundice and IgA nephropathy after an over-the-counter supplement sold as Superdrol and advertised as having no hormonal activity. The authors state that IgA nephropathy had not previously been described in association with testosterone. A 2009 case report and literature review is titled severe cholestasis and renal failure associated with the designer steroid Superdrol (methasteron); the PubMed record has no abstract, so only that title-level association is used here. A further report presented 3 cases of anabolic androgenic steroid-enriched supplement hepatotoxicity and 1 case of renal failure, with prolonged intrahepatic cholestasis.

The most quantitative synthesis is a report of 2 new cases plus a review of 50 further cases of anabolic androgenic steroid drug-induced liver injury, assessed with the updated RUCAM score. The most common steroid taken was methyldrostanolone. Patients presented a median 56 days after starting, and bilirubin peaked a median 28 days after stopping. Causality was unlikely in 1 (2%), possible in 31 (60%) and probable in 20 (38%). Median peak values were bilirubin 705 micromol/L, ALT 125 U/L, AST 71 U/L, ALP 262 U/L, GGT 52 U/L and INR 1.1. Biopsies showed bland canalicular cholestasis, and 43% developed kidney injury with a peak creatinine of 225 micromol/L. No patient died or required liver transplantation.

Therapies in those cases included antipruritics, ursodeoxycholic acid and corticosteroids. The authors state that defining indications and proving efficacy for any of them remains challenging, and no controlled evidence in the records found supports any therapy in this setting.

DEA final rule, 30 July 2012 (77 FR 44456): Schedule III

Regulatory record

Drug Enforcement Administration. Classification of Two Steroids, Prostanozol and Methasterone, as Schedule III Anabolic Steroids Under the Controlled Substances Act. Final rule, 77 FR 44456, published 30 July 2012, effective 29 August 2012.

DEA classified methasterone as an anabolic steroid under 21 U.S.C. 802(41)(A), making it, with its salts, esters and ethers, a Schedule III controlled substance. The rule records that methasterone synthesis was reported in 1956 and anabolic activity in 1959; that it was described as a potent anabolic agent with weak androgenic activity in the castrated male rat; that Zaffaroni and coworkers reported one fifth the androgenic and four times the anabolic activity of methyltestosterone given orally to the experimental animal; that in castrated male rats, by subcutaneous and oral routes, it prevented atrophy of ventral prostate, seminal vesicles, and levator ani muscle to a degree comparable to testosterone and methyltestosterone; and that it bound the androgen receptor comparably to testosterone and showed increased activity relative to testosterone in a transactivation assay. The rule also states that a review of the scientific literature finds adverse health effects including liver toxicity with renal failure reported in conjunction with methasterone abuse, and that FDA issued a Warning Letter in March 2006 in response to adverse health effects associated with the product Superdrol.

Participants / model
Castrated male rats and receptor assays; US legal status
Treatment
Subcutaneous and oral dosing in rats
Follow-up
Rule effective 29 August 2012
Study design
Official Federal Register final rule
Funding
not stated in the source

Every potency figure in this record is from castrated rat and in vitro assays, not from people.

Read the original source
Case series: 5 healthy adults with jaundice, resolved by about 12 weeks

Case report

Shah NL et al. Clin Gastroenterol Hepatol. 2008;6(2):255-8. PMID 18187367.

5 previously healthy patients who used methasteron developed jaundice 2 weeks after discontinuation and presented to tertiary care 2 weeks later. Bilirubin peaked a further 2 to 3 weeks after presentation. About 12 weeks after initial presentation all cases had resolved with no identifiable residual hepatic dysfunction. The authors note that liver failure can worsen after initial presentation, especially within 2 weeks.

Participants / model
5 previously healthy adults using methasterone
Treatment
Oral methasterone supplement products
Follow-up
About 12 weeks from presentation to resolution
Study design
Case series
Funding
not stated in the source

The largest case series of methasterone use in the records found. It reports harm and no benefit measure.

Read the original source
Case report: cholestatic jaundice and IgA nephropathy

Case report

Jasiurkowski B et al. Am J Gastroenterol. 2006;101(11):2659-62. PMID 16952289.

A case of cholestatic jaundice and IgA nephropathy following use of an over-the-counter muscle building supplement sold as Superdrol and advertised as having no hormonal activity. The authors state that IgA nephropathy had not previously been described in association with testosterone and that misrepresentation of the chemicals present in such products creates a false sense of security.

Participants / model
One adult patient
Treatment
Oral over-the-counter supplement containing methasterone
Follow-up
not stated in the source
Study design
Case report with a renal biopsy finding
Funding
not stated in the source

A single case. It shows an association in one patient, not an incidence.

Read the original source
2009 case report and literature review, title-level record only

Case report

Nasr J et al. Dig Dis Sci. 2009;54(5):1144-6. PMID 18720005.

A 2009 report titled severe cholestasis and renal failure associated with the use of the designer steroid Superdrol (methasteron), described as a case report and literature review. The PubMed record carries no abstract, so only the title-level association of this product with severe cholestasis and renal failure is supported here.

Participants / model
One adult patient
Treatment
Oral methasterone product
Follow-up
not stated in the source
Study design
Case report and literature review; abstract not available
Funding
not stated in the source

No figures from this paper are used because the abstract is not available.

Read the original source
Case series: 3 hepatotoxicity cases and 1 renal failure

Case report

Krishnan PV et al. J Clin Gastroenterol. 2009;43(7):672-5. PMID 19238093.

A report presenting 3 cases of anabolic androgenic steroid-enriched dietary supplement-induced hepatotoxicity and 1 case of renal failure, with the authors noting that three recent reports had already documented cholestatic jaundice and nephropathy from these compounds. The pattern described is prolonged intrahepatic cholestasis.

Participants / model
4 adult patients
Treatment
Oral dietary supplements enriched with anabolic androgenic steroids
Follow-up
not stated in the source
Study design
Case series
Funding
not stated in the source

The supplements are described as steroid-enriched; the abstract is not specific to methasterone alone.

Read the original source
52 cases of steroid liver injury: methyldrostanolone most common, bilirubin 705

Human study

Abeles RD et al. BMJ Open Gastroenterol. 2020;7(1). PMID 33214235.

Two new cases plus a comprehensive review identifying 50 further cases of anabolic androgenic steroid drug-induced liver injury were assessed with the updated RUCAM score. The most common steroid taken was methyldrostanolone. Patients presented a median 56 days after starting, and bilirubin peaked a median 28 days after stopping. Causality was unlikely in 1 (2%), possible in 31 (60%) and probable in 20 (38%). Median peak values were bilirubin 705 micromol/L, ALT 125 U/L, AST 71 U/L, ALP 262 U/L, GGT 52 U/L and INR 1.1. Liver biopsies showed bland canalicular cholestasis. 43% developed kidney injury with a peak creatinine of 225 micromol/L. Therapies included antipruritics, ursodeoxycholic acid, and corticosteroids. No patient died or required liver transplantation.

Participants / model
52 cases of anabolic androgenic steroid liver injury
Treatment
Oral anabolic androgenic steroids, most commonly methyldrostanolone
Follow-up
Median 56 days to presentation; bilirubin peak a median 28 days after stopping
Study design
Case reports plus systematic literature review, assessed with the updated RUCAM score
Funding
not stated in the source

The authors state that defining indications and proving efficacy for any of the therapies remains challenging. The cases are not all methasterone, though methyldrostanolone was the most common steroid.

Read the original source

Is there evidence on cholesterol effects?

Not for methasterone. The only controlled lipid data are for stanozolol, another oral 17-alpha-alkylated steroid: in 11 weight lifters, HDL cholesterol fell 33% and LDL cholesterol rose 29%.

The lipid concern has no methasterone study behind it, but the class mechanism has a controlled one. Eleven male weight lifters took oral stanozolol or intramuscular testosterone enanthate in a six-week crossover design. Oral stanozolol, also a 17-alpha-alkylated androgen, reduced HDL cholesterol by 33% and the HDL2 subfraction by 71%, reduced apolipoprotein A-I by 40%, increased LDL cholesterol by 29% and increased postheparin hepatic triglyceride lipase activity by 123%.

Intramuscular testosterone reduced HDL cholesterol by only 9%, and LDL cholesterol fell 16%. Weight gain was similar with both. The authors attribute the difference to the oral 17-alpha-alkylated route rather than androgenic potency. This is stanozolol in 11 men, not methasterone, and it supports only the class pattern.

Class evidence: stanozolol in 11 weight lifters, HDL cholesterol down 33%

Randomized controlled trial

Thompson PD et al. JAMA. 1989;261(8):1165-8. PMID 2915439.

Oral stanozolol, also a 17-alpha-alkylated androgen, reduced HDL cholesterol by 33% and the HDL2 subfraction by 71%, reduced apolipoprotein A-I by 40%, increased LDL cholesterol by 29%, and increased postheparin hepatic triglyceride lipase activity by 123%. Intramuscular testosterone reduced HDL cholesterol by only 9% and LDL cholesterol fell 16%. Weight gain was similar with both. The authors attribute the difference to the oral 17-alpha-alkylated route rather than androgenic potency.

Participants / model
11 male weight lifters
Treatment
Oral stanozolol versus intramuscular testosterone enanthate
Follow-up
Six weeks, crossover design
Study design
Randomized crossover trial
Funding
not stated in the source

This is stanozolol in 11 men, not methasterone, and it supports only the class pattern for oral 17-alpha-alkylated androgens.

Read the original source

Has methasterone turned up in products that did not declare it?

Yes. A New York State health department investigation of about 16 residents traced symptoms, including one hospitalization for liver damage, to B-50 vitamin capsules that contained methasterone, dimethazine and methylstenbolone.

A New York State Department of Health investigation of about 16 residents reporting fatigue, scalp hair loss and muscle aches, one hospitalized for liver damage, traced a common factor to B-50 vitamin and multimineral supplements from one supplier. Chemical analysis by GC-MS, LC-MS/MS, LC-HRMS and NMR found significant levels of methasterone, dimethazine (an azine-linked dimer of methasterone) and methylstenbolone.

Methasterone and extracts of certain capsules were highly androgenic in androgen receptor luciferase assays, with androgenicity persisting for several days after cell exposure. The implicated lots were associated with the hospitalization and with symptoms of severe virilization in a child. Because the capsules contained three compounds, these reports cannot be assigned to methasterone alone.

Product identity is not reliable for this compound. A case report of an over-the-counter supplement sold as Superdrol also describes it as advertised as having no hormonal activity.

Undeclared steroids in B-50 vitamin capsules: about 16 residents, 1 hospitalized

Human study

Tran BN et al. Steroids. 2023;193:109199. PMID 36796473.

A New York State Department of Health investigation of about 16 residents reporting fatigue, scalp hair loss, and muscle aches, one hospitalized for liver damage, traced a common factor to B-50 vitamin and multimineral supplements from one supplier. Chemical analysis by GC-MS, LC-MS/MS, LC-HRMS, and NMR found significant levels of methasterone, dimethazine (an azine-linked dimer of methasterone), and methylstenbolone. Methasterone and extracts of certain capsules were highly androgenic in androgen receptor luciferase assays, with androgenicity persisting for several days after cell exposure. The implicated lots were associated with the hospitalization and with symptoms of severe virilization in a child.

Participants / model
About 16 adults and one child; cell-based androgen receptor assays
Treatment
Oral vitamin and multimineral supplement capsules
Follow-up
not stated in the source
Study design
Analytical and epidemiological investigation
Funding
not stated in the source

The capsules contained three androgens, so the reports cannot be assigned to methasterone alone. The product did not declare these ingredients.

Read the original source
Case report: cholestatic jaundice and IgA nephropathy

Case report

Jasiurkowski B et al. Am J Gastroenterol. 2006;101(11):2659-62. PMID 16952289.

A case of cholestatic jaundice and IgA nephropathy following use of an over-the-counter muscle building supplement sold as Superdrol and advertised as having no hormonal activity. The authors state that IgA nephropathy had not previously been described in association with testosterone and that misrepresentation of the chemicals present in such products creates a false sense of security.

Participants / model
One adult patient
Treatment
Oral over-the-counter supplement containing methasterone
Follow-up
not stated in the source
Study design
Case report with a renal biopsy finding
Funding
not stated in the source

A single case. It shows an association in one patient, not an incidence.

Read the original source

Why does methasterone sit in F tier?

The published record is almost entirely harm, with cholestatic liver and kidney injury in case reports and a 52-case review, and nothing measured on the benefit side. It is also a Schedule III controlled substance in the US with no approved product or label.

The published record for methasterone is almost entirely a record of harm: five previously healthy people with jaundice in one series, a case with IgA nephropathy, a case of severe cholestasis with renal failure, further cases of cholestasis and renal failure, and a 52-case review in which methyldrostanolone was the most common steroid, median peak bilirubin was 705 micromol/L, biopsy showed bland canalicular cholestasis and 43% had kidney injury.

Nothing is measured on the benefit side. One search for any controlled human trial returned a single record, an antidoping urine study in two volunteers that measured detection windows. The potency claim traces back to castrated rat and in vitro assays recorded in the DEA rule, with no human measurement of anything.

It is a Schedule III controlled substance in the US under 21 CFR 1308.13(f)(48), with no approved product and no label, and the one documented supply-side incident involved it turning up undeclared in vitamin capsules.

Case series: 5 healthy adults with jaundice, resolved by about 12 weeks

Case report

Shah NL et al. Clin Gastroenterol Hepatol. 2008;6(2):255-8. PMID 18187367.

5 previously healthy patients who used methasteron developed jaundice 2 weeks after discontinuation and presented to tertiary care 2 weeks later. Bilirubin peaked a further 2 to 3 weeks after presentation. About 12 weeks after initial presentation all cases had resolved with no identifiable residual hepatic dysfunction. The authors note that liver failure can worsen after initial presentation, especially within 2 weeks.

Participants / model
5 previously healthy adults using methasterone
Treatment
Oral methasterone supplement products
Follow-up
About 12 weeks from presentation to resolution
Study design
Case series
Funding
not stated in the source

The largest case series of methasterone use in the records found. It reports harm and no benefit measure.

Read the original source
52 cases of steroid liver injury: methyldrostanolone most common, bilirubin 705

Human study

Abeles RD et al. BMJ Open Gastroenterol. 2020;7(1). PMID 33214235.

Two new cases plus a comprehensive review identifying 50 further cases of anabolic androgenic steroid drug-induced liver injury were assessed with the updated RUCAM score. The most common steroid taken was methyldrostanolone. Patients presented a median 56 days after starting, and bilirubin peaked a median 28 days after stopping. Causality was unlikely in 1 (2%), possible in 31 (60%) and probable in 20 (38%). Median peak values were bilirubin 705 micromol/L, ALT 125 U/L, AST 71 U/L, ALP 262 U/L, GGT 52 U/L and INR 1.1. Liver biopsies showed bland canalicular cholestasis. 43% developed kidney injury with a peak creatinine of 225 micromol/L. Therapies included antipruritics, ursodeoxycholic acid, and corticosteroids. No patient died or required liver transplantation.

Participants / model
52 cases of anabolic androgenic steroid liver injury
Treatment
Oral anabolic androgenic steroids, most commonly methyldrostanolone
Follow-up
Median 56 days to presentation; bilirubin peak a median 28 days after stopping
Study design
Case reports plus systematic literature review, assessed with the updated RUCAM score
Funding
not stated in the source

The authors state that defining indications and proving efficacy for any of the therapies remains challenging. The cases are not all methasterone, though methyldrostanolone was the most common steroid.

Read the original source
Antidoping study: 2 volunteers, metabolite detectable up to 50 days

Human study

Zheng S et al. Anal Chem. 2025;97(5):3009-3018. PMID 39883123.

Healthy volunteers each ingested one tablet of the drug and urine was collected over 50 days. Two new methasterone metabolites were identified, and the metabolite 18-nor-17beta-hydroxymethyl-2alpha,17alpha-dimethyl-5alpha-androst-13-en-3-one was detectable as a glucuronide in urine from both volunteers up to 50 days after administration.

Participants / model
Healthy volunteers, 2 for the methasterone arm
Treatment
Single oral tablet
Follow-up
Urine collected over 50 days
Study design
Analytical human excretion study
Funding
not stated in the source

The study measured detection windows only. It reports no efficacy, body composition, lipid, blood pressure, or safety outcome.

Read the original source
PubMed search, 9 October 2026: 1 record, an antidoping urine study

PubMed search record

PubMed search run on 9 October 2026: (methasterone OR methyldrostanolone OR superdrol) AND (randomized OR randomised OR placebo OR clinical trial[pt] OR healthy volunteers OR lean body mass OR strength). 1 record returned.

The search returned 1 record, the antidoping urinary excretion study. ClinicalTrials.gov searches for methasterone and for Superdrol on the same date returned no studies. No controlled trial of methasterone in humans exists in the records found: there is no measured gain in lean mass, no measured strength result, no lipid panel, no blood pressure measurement, and no systematic adverse event collection. Everything known about its effects in people comes from case reports of harm and from analytical chemistry.

Participants / model
Records returned, not a population
Treatment
Not applicable
Follow-up
Search run on 9 October 2026
Study design
Literature and registry search
Funding
not stated in the source

A search result shows what PubMed and ClinicalTrials.gov returned on that date. It is not proof that no unindexed study exists.

Read the original source
DEA final rule, 30 July 2012 (77 FR 44456): Schedule III

Regulatory record

Drug Enforcement Administration. Classification of Two Steroids, Prostanozol and Methasterone, as Schedule III Anabolic Steroids Under the Controlled Substances Act. Final rule, 77 FR 44456, published 30 July 2012, effective 29 August 2012.

DEA classified methasterone as an anabolic steroid under 21 U.S.C. 802(41)(A), making it, with its salts, esters and ethers, a Schedule III controlled substance. The rule records that methasterone synthesis was reported in 1956 and anabolic activity in 1959; that it was described as a potent anabolic agent with weak androgenic activity in the castrated male rat; that Zaffaroni and coworkers reported one fifth the androgenic and four times the anabolic activity of methyltestosterone given orally to the experimental animal; that in castrated male rats, by subcutaneous and oral routes, it prevented atrophy of ventral prostate, seminal vesicles, and levator ani muscle to a degree comparable to testosterone and methyltestosterone; and that it bound the androgen receptor comparably to testosterone and showed increased activity relative to testosterone in a transactivation assay. The rule also states that a review of the scientific literature finds adverse health effects including liver toxicity with renal failure reported in conjunction with methasterone abuse, and that FDA issued a Warning Letter in March 2006 in response to adverse health effects associated with the product Superdrol.

Participants / model
Castrated male rats and receptor assays; US legal status
Treatment
Subcutaneous and oral dosing in rats
Follow-up
Rule effective 29 August 2012
Study design
Official Federal Register final rule
Funding
not stated in the source

Every potency figure in this record is from castrated rat and in vitro assays, not from people.

Read the original source
21 CFR 1308.13(f)(48): methasterone listed in Schedule III

Regulatory record

Electronic Code of Federal Regulations. 21 CFR 1308.13, Schedule III, paragraph (f)(48), text for the 2026-10-01 edition.

21 CFR 1308.13(f)(48) lists methasterone (2alpha,17alpha-dimethyl-5alpha-androstan-17beta-ol-3-one, or 2alpha,17alpha-dimethyl-17beta-hydroxy-5alpha-androstan-3-one) among the Schedule III anabolic steroids. Possession and distribution in the US are controlled accordingly. A Drugs@FDA query on 9 October 2026 for products with methasterone as an active ingredient returned no matching application, and a DailyMed search returned no labels, so there is no approved medical product and no label anywhere in the US record.

Participants / model
US legal status, not a clinical population
Treatment
Any form
Follow-up
Text for the 2026-10-01 edition
Study design
Official CFR text
Funding
not stated in the source

The scheduling entry is a legal classification. The Drugs@FDA and DailyMed searches are dated and US-scoped.

Read the original source
Undeclared steroids in B-50 vitamin capsules: about 16 residents, 1 hospitalized

Human study

Tran BN et al. Steroids. 2023;193:109199. PMID 36796473.

A New York State Department of Health investigation of about 16 residents reporting fatigue, scalp hair loss, and muscle aches, one hospitalized for liver damage, traced a common factor to B-50 vitamin and multimineral supplements from one supplier. Chemical analysis by GC-MS, LC-MS/MS, LC-HRMS, and NMR found significant levels of methasterone, dimethazine (an azine-linked dimer of methasterone), and methylstenbolone. Methasterone and extracts of certain capsules were highly androgenic in androgen receptor luciferase assays, with androgenicity persisting for several days after cell exposure. The implicated lots were associated with the hospitalization and with symptoms of severe virilization in a child.

Participants / model
About 16 adults and one child; cell-based androgen receptor assays
Treatment
Oral vitamin and multimineral supplement capsules
Follow-up
not stated in the source
Study design
Analytical and epidemiological investigation
Funding
not stated in the source

The capsules contained three androgens, so the reports cannot be assigned to methasterone alone. The product did not declare these ingredients.

Read the original source

Studies and sources

PubChem: methasterone (Superdrol) identity

Chemical identity record

National Library of Medicine. PubChem compound record CID 237186 (methasterone).

Methasterone: PubChem CID 237186, C21H34O2, molecular weight 318.5 g/mol, CAS 3381-88-2. Listed synonyms include Superdrol, methyldrostanolone, 17-methyldrostanolone, methasteron, and NSC 40490. Chemically it is 2alpha,17alpha-dimethyl-5alpha-androstan-17beta-ol-3-one, a 17-alpha-alkylated oral derivative of drostanolone. The 17-alpha methyl group is what makes it orally active and is the chemical feature shared by the oral androgens associated with cholestatic liver injury.

Participants / model
Chemical identity, not a clinical population
Treatment
Defined molecule
Follow-up
Not applicable
Study design
NLM chemical record
Funding
not stated in the source

Identity record only; it says nothing about efficacy or safety.

Read the original source
DEA final rule, 30 July 2012 (77 FR 44456): Schedule III

Regulatory record

Drug Enforcement Administration. Classification of Two Steroids, Prostanozol and Methasterone, as Schedule III Anabolic Steroids Under the Controlled Substances Act. Final rule, 77 FR 44456, published 30 July 2012, effective 29 August 2012.

DEA classified methasterone as an anabolic steroid under 21 U.S.C. 802(41)(A), making it, with its salts, esters and ethers, a Schedule III controlled substance. The rule records that methasterone synthesis was reported in 1956 and anabolic activity in 1959; that it was described as a potent anabolic agent with weak androgenic activity in the castrated male rat; that Zaffaroni and coworkers reported one fifth the androgenic and four times the anabolic activity of methyltestosterone given orally to the experimental animal; that in castrated male rats, by subcutaneous and oral routes, it prevented atrophy of ventral prostate, seminal vesicles, and levator ani muscle to a degree comparable to testosterone and methyltestosterone; and that it bound the androgen receptor comparably to testosterone and showed increased activity relative to testosterone in a transactivation assay. The rule also states that a review of the scientific literature finds adverse health effects including liver toxicity with renal failure reported in conjunction with methasterone abuse, and that FDA issued a Warning Letter in March 2006 in response to adverse health effects associated with the product Superdrol.

Participants / model
Castrated male rats and receptor assays; US legal status
Treatment
Subcutaneous and oral dosing in rats
Follow-up
Rule effective 29 August 2012
Study design
Official Federal Register final rule
Funding
not stated in the source

Every potency figure in this record is from castrated rat and in vitro assays, not from people.

Read the original source
21 CFR 1308.13(f)(48): methasterone listed in Schedule III

Regulatory record

Electronic Code of Federal Regulations. 21 CFR 1308.13, Schedule III, paragraph (f)(48), text for the 2026-10-01 edition.

21 CFR 1308.13(f)(48) lists methasterone (2alpha,17alpha-dimethyl-5alpha-androstan-17beta-ol-3-one, or 2alpha,17alpha-dimethyl-17beta-hydroxy-5alpha-androstan-3-one) among the Schedule III anabolic steroids. Possession and distribution in the US are controlled accordingly. A Drugs@FDA query on 9 October 2026 for products with methasterone as an active ingredient returned no matching application, and a DailyMed search returned no labels, so there is no approved medical product and no label anywhere in the US record.

Participants / model
US legal status, not a clinical population
Treatment
Any form
Follow-up
Text for the 2026-10-01 edition
Study design
Official CFR text
Funding
not stated in the source

The scheduling entry is a legal classification. The Drugs@FDA and DailyMed searches are dated and US-scoped.

Read the original source
Case series: 5 healthy adults with jaundice, resolved by about 12 weeks

Case report

Shah NL et al. Clin Gastroenterol Hepatol. 2008;6(2):255-8. PMID 18187367.

5 previously healthy patients who used methasteron developed jaundice 2 weeks after discontinuation and presented to tertiary care 2 weeks later. Bilirubin peaked a further 2 to 3 weeks after presentation. About 12 weeks after initial presentation all cases had resolved with no identifiable residual hepatic dysfunction. The authors note that liver failure can worsen after initial presentation, especially within 2 weeks.

Participants / model
5 previously healthy adults using methasterone
Treatment
Oral methasterone supplement products
Follow-up
About 12 weeks from presentation to resolution
Study design
Case series
Funding
not stated in the source

The largest case series of methasterone use in the records found. It reports harm and no benefit measure.

Read the original source
Case report: cholestatic jaundice and IgA nephropathy

Case report

Jasiurkowski B et al. Am J Gastroenterol. 2006;101(11):2659-62. PMID 16952289.

A case of cholestatic jaundice and IgA nephropathy following use of an over-the-counter muscle building supplement sold as Superdrol and advertised as having no hormonal activity. The authors state that IgA nephropathy had not previously been described in association with testosterone and that misrepresentation of the chemicals present in such products creates a false sense of security.

Participants / model
One adult patient
Treatment
Oral over-the-counter supplement containing methasterone
Follow-up
not stated in the source
Study design
Case report with a renal biopsy finding
Funding
not stated in the source

A single case. It shows an association in one patient, not an incidence.

Read the original source
2009 case report and literature review, title-level record only

Case report

Nasr J et al. Dig Dis Sci. 2009;54(5):1144-6. PMID 18720005.

A 2009 report titled severe cholestasis and renal failure associated with the use of the designer steroid Superdrol (methasteron), described as a case report and literature review. The PubMed record carries no abstract, so only the title-level association of this product with severe cholestasis and renal failure is supported here.

Participants / model
One adult patient
Treatment
Oral methasterone product
Follow-up
not stated in the source
Study design
Case report and literature review; abstract not available
Funding
not stated in the source

No figures from this paper are used because the abstract is not available.

Read the original source
Case series: 3 hepatotoxicity cases and 1 renal failure

Case report

Krishnan PV et al. J Clin Gastroenterol. 2009;43(7):672-5. PMID 19238093.

A report presenting 3 cases of anabolic androgenic steroid-enriched dietary supplement-induced hepatotoxicity and 1 case of renal failure, with the authors noting that three recent reports had already documented cholestatic jaundice and nephropathy from these compounds. The pattern described is prolonged intrahepatic cholestasis.

Participants / model
4 adult patients
Treatment
Oral dietary supplements enriched with anabolic androgenic steroids
Follow-up
not stated in the source
Study design
Case series
Funding
not stated in the source

The supplements are described as steroid-enriched; the abstract is not specific to methasterone alone.

Read the original source
52 cases of steroid liver injury: methyldrostanolone most common, bilirubin 705

Human study

Abeles RD et al. BMJ Open Gastroenterol. 2020;7(1). PMID 33214235.

Two new cases plus a comprehensive review identifying 50 further cases of anabolic androgenic steroid drug-induced liver injury were assessed with the updated RUCAM score. The most common steroid taken was methyldrostanolone. Patients presented a median 56 days after starting, and bilirubin peaked a median 28 days after stopping. Causality was unlikely in 1 (2%), possible in 31 (60%) and probable in 20 (38%). Median peak values were bilirubin 705 micromol/L, ALT 125 U/L, AST 71 U/L, ALP 262 U/L, GGT 52 U/L and INR 1.1. Liver biopsies showed bland canalicular cholestasis. 43% developed kidney injury with a peak creatinine of 225 micromol/L. Therapies included antipruritics, ursodeoxycholic acid, and corticosteroids. No patient died or required liver transplantation.

Participants / model
52 cases of anabolic androgenic steroid liver injury
Treatment
Oral anabolic androgenic steroids, most commonly methyldrostanolone
Follow-up
Median 56 days to presentation; bilirubin peak a median 28 days after stopping
Study design
Case reports plus systematic literature review, assessed with the updated RUCAM score
Funding
not stated in the source

The authors state that defining indications and proving efficacy for any of the therapies remains challenging. The cases are not all methasterone, though methyldrostanolone was the most common steroid.

Read the original source
Undeclared steroids in B-50 vitamin capsules: about 16 residents, 1 hospitalized

Human study

Tran BN et al. Steroids. 2023;193:109199. PMID 36796473.

A New York State Department of Health investigation of about 16 residents reporting fatigue, scalp hair loss, and muscle aches, one hospitalized for liver damage, traced a common factor to B-50 vitamin and multimineral supplements from one supplier. Chemical analysis by GC-MS, LC-MS/MS, LC-HRMS, and NMR found significant levels of methasterone, dimethazine (an azine-linked dimer of methasterone), and methylstenbolone. Methasterone and extracts of certain capsules were highly androgenic in androgen receptor luciferase assays, with androgenicity persisting for several days after cell exposure. The implicated lots were associated with the hospitalization and with symptoms of severe virilization in a child.

Participants / model
About 16 adults and one child; cell-based androgen receptor assays
Treatment
Oral vitamin and multimineral supplement capsules
Follow-up
not stated in the source
Study design
Analytical and epidemiological investigation
Funding
not stated in the source

The capsules contained three androgens, so the reports cannot be assigned to methasterone alone. The product did not declare these ingredients.

Read the original source
Class evidence: stanozolol in 11 weight lifters, HDL cholesterol down 33%

Randomized controlled trial

Thompson PD et al. JAMA. 1989;261(8):1165-8. PMID 2915439.

Oral stanozolol, also a 17-alpha-alkylated androgen, reduced HDL cholesterol by 33% and the HDL2 subfraction by 71%, reduced apolipoprotein A-I by 40%, increased LDL cholesterol by 29%, and increased postheparin hepatic triglyceride lipase activity by 123%. Intramuscular testosterone reduced HDL cholesterol by only 9% and LDL cholesterol fell 16%. Weight gain was similar with both. The authors attribute the difference to the oral 17-alpha-alkylated route rather than androgenic potency.

Participants / model
11 male weight lifters
Treatment
Oral stanozolol versus intramuscular testosterone enanthate
Follow-up
Six weeks, crossover design
Study design
Randomized crossover trial
Funding
not stated in the source

This is stanozolol in 11 men, not methasterone, and it supports only the class pattern for oral 17-alpha-alkylated androgens.

Read the original source
Antidoping study: 2 volunteers, metabolite detectable up to 50 days

Human study

Zheng S et al. Anal Chem. 2025;97(5):3009-3018. PMID 39883123.

Healthy volunteers each ingested one tablet of the drug and urine was collected over 50 days. Two new methasterone metabolites were identified, and the metabolite 18-nor-17beta-hydroxymethyl-2alpha,17alpha-dimethyl-5alpha-androst-13-en-3-one was detectable as a glucuronide in urine from both volunteers up to 50 days after administration.

Participants / model
Healthy volunteers, 2 for the methasterone arm
Treatment
Single oral tablet
Follow-up
Urine collected over 50 days
Study design
Analytical human excretion study
Funding
not stated in the source

The study measured detection windows only. It reports no efficacy, body composition, lipid, blood pressure, or safety outcome.

Read the original source

Why is Methasterone in F tier?

F fits a compound whose published record is almost entirely harm and whose benefit has never been measured. Five previously healthy people developed jaundice in one series, a 52-case review reports bland canalicular cholestasis and kidney injury in 43%, no controlled human trial exists, and the potency claim rests on castrated rat and in vitro assays. It is also a Schedule III controlled substance in the US with no approved product or label.