Epistane (chemical name: 2α,3α-epithio-17α-methyl-5α-androstan-17β-ol; also called methylepitiostanol) is a synthetic oral anabolic–androgenic steroid (AAS) that was marketed for years as a “prohormone” or “dry” bulking agent. Despite supplement-style packaging, Epistane is a 17-alpha-alkylated steroid—an oral modification linked to liver stress—and not a benign muscle builder. In lab models, Epistane behaves like other AAS: it activates androgen receptors, shifts lipid markers, and can influence bile acid handling in the liver. In people, nonmedical AAS use is tied to a distinctive form of drug-induced liver injury, hormonal suppression, acne, hair loss, mood changes, and cardiovascular risk factors. No regulatory agency has approved Epistane for any medical indication, and dosing “cycles” promoted online are not evidence-based. If you’re researching Epistane for physique goals, this guide explains what it is, what is actually known, how risks arise, who should avoid it, and safer alternatives.
Key Insights
- Oral 17-α-alkylated steroid with androgenic and anabolic activity; human performance benefits come with significant medical risks.
- Major safety concern is cholestatic liver injury; lipid, blood pressure, and hormonal disturbances are common with AAS.
- No approved medical dose for Epistane; outside clinical care the only responsible intake is 0 mg/day.
- Avoid entirely if you have liver, kidney, or heart disease; if pregnant or breastfeeding; or if you are subject to anti-doping rules.
Table of Contents
- What is Epistane and how it works
- What benefits are supported by evidence
- How it is sold and legal context
- Healthier ways to reach your goals
- How much Epistane per day
- Side effects, interactions, and who should avoid
- Evidence gaps and what we still do not know
What is Epistane and how it works
Epistane is a lab-synthesized derivative of the anti-estrogenic steroid epitiostanol, modified with a 17-alpha-methyl group to survive first-pass metabolism. That methyl group makes it orally active—and also places stress on the liver. As an androgen receptor (AR) agonist, Epistane binds ARs in muscle and other tissues to promote protein synthesis and nitrogen retention. Like other 5α-reduced androgens, it can produce “dry” looking gains (lower water retention) compared with aromatizing steroids, which partly explains its gym-floor reputation.
Beyond muscle, two aspects of Epistane’s pharmacology shape risk:
- Bile acid and cholestasis signaling. 17-α-alkylated steroids can disrupt bile formation and flow, producing a characteristic bland cholestasis with deep jaundice but relatively modest enzyme elevations. In human hepatocyte models, Epistane specifically upregulates CYP8B1 (a bile-acid synthesis enzyme) and perturbs nuclear receptor cross-talk, a mechanistic path toward cholestasis.
- Endocrine feedback. Exogenous androgens suppress the hypothalamic–pituitary–gonadal (HPG) axis. Over weeks, endogenous testosterone production falls, testicular volume may decrease, sperm parameters can worsen, and estrogen-to-androgen balance shifts once exogenous steroid is withdrawn.
Other class-typical effects include lipid changes (HDL drop, LDL rise), blood pressure increases, acne/alopecia, and mood variability (irritability, low mood, aggression in susceptible users). None of these are unique to Epistane—but the oral methylation makes liver safety a central concern.
Key practical points if you’re simply learning the science:
- Labels calling Epistane a “prohormone” are misleading; it’s an active steroid.
- “Dry gains” reflect pharmacology (low aromatization and diuretic routines), not a safety advantage.
- The same structural features that make Epistane convenient to swallow also make it more hepatotoxic than many injectable androgens.
What benefits are supported by evidence
Body composition and strength (inference from AAS class). Anabolic–androgenic steroids increase lean mass and strength in controlled trials; users often report faster training progression, better gym performance, and short-term physique changes. Epistane is expected to share these class effects given its AR activity. However, there are no high-quality randomized trials in healthy adults demonstrating Epistane’s net clinical benefits or long-term safety. Reports in the fitness community are anecdotal and confounded by training, diet, and polypharmacy (stacking with other agents).
Anti-estrogen reputation vs reality. Because epitiostanol was studied as an anti-estrogen, Epistane is often marketed as “estrogen-controlling.” In practice, any anti-estrogen action is unreliable at real-world doses and does not neutralize the androgen’s own adverse effects. Users sometimes mistake a lack of water retention for “estrogen control,” but that is not the same as proven receptor antagonism in vivo. Relying on this reputation invites complacency about gynecomastia risk from other stacked hormones and about HPG axis suppression during and after use.
Liver-specific data. The most concrete mechanistic evidence around Epistane is negative: in human hepatocytes, Epistane triggered cholestatic changes and increased cholic-acid conjugates. Clinically, oral 17-α-alkylated AAS are the subtype most associated with prolonged cholestatic jaundice, sometimes requiring hospitalization. This is the opposite of a benefit profile; it is a risk signal users often underestimate.
Bottom line. If the question is “Does Epistane build muscle?” the best available inference is “yes, as a potent oral AAS.” If the question is “Does Epistane offer a favorable risk–benefit ratio for nonmedical users?” the evidence points clearly to no—particularly given credible liver, lipid, endocrine, and blood-pressure risks and the absence of approved medical indications.
How it is sold and legal context
Epistane circulated for years as an over-the-counter “prohormone” despite being a true synthetic steroid. Some vendors still sell look-alikes labeled as research chemicals or multi-ingredient “muscle builders.” These products often arrive with dosing scoops, cycle “guides,” and post-cycle therapy (PCT) recommendations—none of which are standardized, evidence-based, or safe substitutes for medical oversight.
In many jurisdictions, anabolic steroids are controlled substances; they are not legal to sell or possess without a valid prescription for an approved medical use. Even where the letter of the law is ambiguous for specific analogs, anti-doping rules are not: anabolic agents are prohibited in sport at all times. Athletes are strictly liable for what they ingest, and “not listed by name” is not a defense when a compound clearly falls within a prohibited class.
Regulatory agencies also warn that bodybuilding products marketed as supplements may hide drugs—including undisclosed AAS. Such products can be misbranded, contaminated, or dosed inconsistently. When FDA or other authorities test these items, they frequently find active ingredients not listed on the label, a setup for unexpected side effects and positive doping tests.
Practical implications if you are weighing legal and ethical aspects:
- Purchasing Epistane products exposes you to legal risk (controlled-substance laws), career risk (anti-doping violations), and health risk (unknown identity/purity).
- “For research use only” labels do not shield buyers from regulatory enforcement or medical liability.
- If you compete, even in smaller federations, assume any AAS analog can trigger sanctions.
Healthier ways to reach your goals
Most people look at Epistane for three reasons: visible muscularity, strength progress, and “dry” appearance. You can move the needle on each—without steroids—by tightening controllable levers and, if needed, using legal, lower-risk tools.
Training levers
- Progressive overload with intelligent periodization. Rotate rep ranges and stress types (volume blocks into intensity blocks) to keep hypertrophy signals high while managing fatigue.
- Exercise selection and range of motion. Favor multi-joint lifts for efficiency and sprinkle isolation movements to bring up lagging muscles; train near full ROM for hypertrophy.
- Deloads on schedule. Short deloads prevent the “two steps forward, two steps back” cycle of overreaching and injury.
Nutrition levers
- Protein 1.6–2.2 g/kg/day distributed over 3–5 meals; include leucine-rich sources.
- Consistent energy balance. Gain phases run at a small surplus (≈+5–10% calories); cut phases at a modest deficit (≈−10–20%).
- Hydration and fiber. “Dry” look comes more from lower subcutaneous fat and smart sodium/carbohydrate timing than from risky diuretics or steroids.
Evidence-supported, legal supplements (if appropriate and tolerated)
- Creatine monohydrate (3–5 g/day). Improves strength, power, and training volume in hundreds of studies.
- Caffeine (≈3 mg/kg pre-workout). Acute performance aid; mind your sleep.
- Beta-alanine (3–6 g/day). Helps with high-rep sets and interval work after a loading period.
- Protein powders. Convenience, not magic—whole foods first.
Medical and recovery foundations
- Sleep regularity. Aim for 7–9 hours; chronically short sleep blunts hypertrophy signals and elevates injury risk.
- Cardiometabolic screening. If you have dyslipidemia, hypertension, or prediabetes, prioritize treatment; steroids worsen each.
- Injury prevention. Technique coaching and sensible load progression outcompete “chemical solutions” for long-term progress.
If aesthetic or performance goals are driving you toward risky compounds, consider a coach or sports physician who can design a structured program that fits your physiology and timeline—without crossing into AAS territory.
How much Epistane per day
There is no approved medical dose for Epistane. No regulator has established a safe or effective regimen for any indication. Online “cycles” (for example, fixed milligram schedules with or without PCT) are not grounded in peer-reviewed clinical research, and they ignore known risks of oral 17-α-alkylated steroids—especially cholestatic liver injury.
What the evidence actually allows us to say:
- Human pharmacokinetics are not defined. We do not have validated data on absorption, distribution, half-life, or metabolism in people. Without these, any numeric plan is guesswork.
- Class effects predict harm. Oral 17-α-alkylated AAS have the highest association with prolonged cholestatic jaundice, with some cases requiring prolonged recovery even after stopping the drug.
- “Post-cycle therapy” is not a safety net. Over-the-counter SERMs or aromatase inhibitors are often counterfeit or misdosed; even when real, they cannot reverse liver injury that has already developed.
Responsible takeaway: outside clinical trials and legitimate medical indications, the only evidence-based dose is 0 mg/day. If you are already using Epistane, seek medical care for baseline labs (comprehensive metabolic panel, bilirubin, GGT, lipid profile, CBC, blood pressure). Stop immediately and see a clinician if you develop itching, dark urine, yellowing of the eyes/skin, right-upper-quadrant pain, severe fatigue, or pale stools—classic cholestasis signs.
Side effects, interactions, and who should avoid
Common class-typical effects (AAS)
- Liver: risk of bland cholestasis with deep jaundice, sometimes protracted recovery; rare but serious tumors reported with long-term AAS exposure.
- Lipids and cardiovascular: HDL tends to fall, LDL to rise; blood pressure may climb; endothelial function can worsen. These changes increase long-term cardiovascular risk when stacked with smoking, sleep apnea, or family history.
- Endocrine and reproductive: suppression of endogenous testosterone, testicular atrophy, decreased sperm count/quality, menstrual irregularities in women; sexual dysfunction during and after use.
- Dermatologic and hair: acne, oily skin, androgenic alopecia acceleration in genetically susceptible individuals.
- Neuropsychiatric: irritability, low mood, anxiety, and aggression are reported in some users; susceptibility varies.
Serious warning signs—seek urgent care
- Jaundice, generalized itching, dark urine, pale stools.
- Severe abdominal pain, vomiting, or unexplained fever.
- Chest pain, shortness of breath, or leg swelling (possible thrombotic events).
- Sudden severe headache or neurological deficits.
Interactions and compounding risks
- Alcohol and hepatotoxic drugs (for example, high-dose acetaminophen, certain antibiotics): additive liver stress.
- Other AAS, SERMs, aromatase inhibitors, or “liver support” blends: stacking increases unpredictability; “support” products do not prevent cholestasis.
- Statins and other lipid-active drugs: AAS-driven dyslipidemia can complicate management; medical supervision is essential.
- Anticoagulants/antiplatelets: AAS may influence clotting factors and blood pressure; clinician oversight is needed.
Who should avoid Epistane entirely
- Anyone with liver disease (past or present), cholestasis, kidney disease, heart disease, or uncontrolled hypertension.
- Pregnant or breastfeeding individuals; those trying to conceive.
- Adolescents and young adults (still developing endocrine and skeletal systems).
- Athletes under anti-doping codes—AAS are prohibited at all times.
- People with psychiatric conditions (depression, anxiety, bipolar disorder) or substance use disorders; mood destabilization risk is higher.
Monitoring if exposed
If a clinician is caring for someone who has already taken Epistane, reasonable labs include bilirubin (total/direct), ALT/AST, ALP, GGT, lipid panel, CBC, testosterone/LH/FSH at appropriate intervals, plus blood pressure monitoring and symptom review. Prolonged cholestasis is managed supportively; stopping the agent is fundamental.
Evidence gaps and what we still do not know
- No modern randomized trials of Epistane in humans for any clinical endpoint. Most claims come from general AAS data or uncontrolled, confounded anecdotes.
- Mechanistic liver data are stronger than benefit data. In vitro work with human hepatocytes shows cholestatic signatures specific to Epistane; this tilts the evidence–risk balance away from use.
- Pharmacokinetics and dose–response unknowns. Without human PK data, all popular “cycles” are speculative and may overshoot risk thresholds.
- Long-term outcomes unquantified. We lack prospective cohort data tracking cardiovascular events, fertility, mood, or cancer risk in Epistane users specifically; AAS-wide literature raises concern on each dimension.
- Product identity and purity issues persist. Analyses repeatedly find mislabeling and undisclosed drugs in bodybuilding “supplements,” making even self-reported user experiences unreliable.
Practical takeaway. If you are aiming for lasting physique or strength changes, the highest-yield path remains structured training, evidence-based nutrition, sleep, and legal ergogenics. From a health and regulatory standpoint, Epistane is best viewed as high-risk with no approved use, not as a shortcut.
References
- Epistane, an anabolic steroid used for recreational purposes, causes cholestasis with elevated levels of cholic acid conjugates, by upregulating bile acid synthesis (CYP8B1) and cross-talking with nuclear receptors in human hepatocytes 2020 (Mechanistic Study)
- Androgenic Steroids – LiverTox – NCBI Bookshelf 2020 (Safety Overview)
- Anabolic androgenic steroid-induced liver injury: An update – PMC 2022 (Systematic Review)
- Anabolic steroid-associated liver injury – PMC 2024 (Review)
- Caution: Bodybuilding Products Can Be Risky 2024 (Regulatory Consumer Update)
Disclaimer
This guide is for educational purposes and is not a substitute for professional medical advice, diagnosis, or treatment. Epistane (methylepitiostanol) is not approved for any medical indication. Nonmedical use of anabolic steroids carries significant risks, including serious liver injury, hormonal suppression, and cardiovascular complications, and may violate laws and anti-doping rules. Do not start, continue, or stop any drug or supplement without consulting a qualified healthcare professional. If you have symptoms of liver injury (itching, dark urine, yellowing of eyes/skin), seek medical care immediately.
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