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Lexicon

RAD-140 (Testolone)

One of the most potent non-steroidal SARMs in the research record, with a strong anabolic profile and a correspondingly dense liver case literature.

3 min read 8 sources

White tablet bottle with a dark The Peptide Desk label for RAD-140 on a white podium, next to it a large molecule model of blue, light blue and white spheres with one green sphere in a bright lab
Phase 1 · not approved

Summary

At a glance

Sources checked on 26 Oct 2026

Only study in humans
22 patients

phase 1 in women with advanced breast cancer, not in healthy people3

Liver value AST raised
59.1 %

most common side effect of the phase 1 study, ALT in 45.5 percent3

Binding to the androgen receptor (Ki)
7 nM

the smaller, the tighter the binding, measured in the lab8

Clinical benefit at 24 weeks
18.2 %

in heavily pretreated breast cancer, one partial response3

  • RAD-140 is a non-steroidal SARM. It binds tightly to the androgen receptor and activated it in muscle cells in the lab.81
  • It was developed against breast cancer: in animal models RAD-140 inhibited the growth of tumours with androgen and oestrogen receptors.2
  • The only study in humans was a phase 1 study in 22 women with advanced breast cancer. Liver values rose most often, 72.7 percent had a severe side effect.3
  • Outside of studies, liver injury and myocarditis in young men are described as case reports.456
  • RAD-140 is not approved. There is no study on muscle gain in healthy people. Everything here is the state of research, not a recommendation.73
Profile

Updated May 2026

How long does it stay in the body?

Share left after one dose, calculated with a half-life of ~1.9 days

Half-life ~1.9 days
After 3.7 days: 25 %
Day 1, next dose · 69 %Day 1.9 · 49 %Day 3.7 · 25 %Day 5.6 · 12.4 %Day 9.3 · 3.1 %

Simplified model without an absorption phase, half-life from the TPD lexicon.

Class
SARM

non-steroidal

Use
Oral

daily

Half-life
44.7 hours

measured in humans

WADA
Banned

category S1.2

Sizes
10 to 15 mg

2 sizes in the shop

Contents 14 sections
  1. At a glance
  2. What is RAD-140?
  3. How it works
  4. How to take it
  5. Dosing
  6. What the research shows
  7. Research status
  8. Side effects
  9. Practice
  10. Storage
  11. Related compounds
  12. FAQ
  13. Glossary
  14. Sources

What is RAD-140?

RAD-140, also called Testolone, is a selective androgen receptor modulator (SARM). It was developed by Radius Health, originally with a focus on neuroprotective properties and oncology questions. In performance research it is regarded as one of the strongest members of its class.

It is not a steroid but a small, orally available molecule. The appeal: hit the androgen receptor in muscle and bone without acting broadly where classic steroids cause trouble. How well that selectivity holds up across every endpoint is an open research question.

Comparison

At the androgen receptor in the lexicon

SARMs and testosterone use the same receptor, as stated in the TPD lexicon. Tap a card to open its entry.

Simplified: SARMs are meant to act tissue-preferentially, testosterone acts broadly and is also converted to oestrogen and DHT. 8

How it works

RAD-140 binds the androgen receptor and activates it with tissue preference: strong in muscle and bone, weaker in tissues like prostate or sebaceous glands. In preclinical models it showed a very high anabolic-to-androgenic ratio (over 90:1 in the original characterization).

Unlike testosterone, RAD-140 does not aromatize to estrogen and is not reduced to DHT. That changes the side-effect pattern but does not remove it, in particular the suppression of the body's own testosterone production remains.

Where it acts

Where RAD-140 acted in studies

Tap a point or a card. Colour = androgen receptor, grey = observed.

  1. Muscle

    Activates the androgen receptor in muscle cells, measured in the lab8

    AR
  2. Liver

    AST raised in 59.1 percent, plus case reports of liver injury3

    Observed in trials
  3. Blood values

    SHBG fell in all 18 women measured3

    Observed in trials
  4. Heart

    Case report of myocarditis in a young man6

    Observed in trials

Targets in the ChEMBL database8

Compound CHEMBL1672635: one recorded mechanism, Agonist, Ki 7 nM, EC50 0.1 nM in muscle cells.

Androgen receptor
Gene
AR
UniProt
P10275
ChEMBL
CHEMBL1871
Action
Agonist, Ki 7 nM, EC50 0.1 nM in muscle cells
Glassy light blue and violet muscle fibres on the left, a transparent honeycomb bone structure on the right, glowing blue molecule models dock onto both, another floats between them
SARMs target the androgen receptor in muscle and bone. Symbolic image.

How to take it

RAD-140 is taken orally, no mixing, no injecting.

  • Once daily, the roughly 45-hour half-life means one dose is enough.
  • With some water, with or without food.
  • Research cycles typically run over 8 weeks, followed by a break and axis recovery.
White tablet bottle with a dark The Peptide Desk label for RAD-140 next to a glass of water, six white tablets in front on a bright table
Oral, no dissolving, no injecting. Symbolic image.

Dosing

Dosing

Dosing, titration and syringe

Loading the dosing information …

  • Getting started and stepping up, drawn as a staircase
  • Units on the U-100 syringe for every step
  • How long one vial lasts

What the research shows

The original characterization (Miller, 2011) described RAD-140 as a potent, orally available SARM with a very high anabolic-to-androgenic ratio. A preclinical study (Yu, 2017) showed RAD-140 inhibits the growth of certain androgen-receptor-positive breast cancer models, the original oncology development track. The first study in humans (LoRusso, 2022, phase 1, 22 women with breast cancer) measured a half-life of 44.7 hours; the most common side effects were raised liver values.

On the risk side, RAD-140 is the SARM with the densest case literature on liver injury. A cleanly documented case of liver injury under RAD-140 was published in 2023 (Ladna). There are no human efficacy studies for muscle building in healthy people. No approval exists either.

Study results

What the trials measured

Interactive: switch tabs, tap points, show or hide arms. Arms are named relative to each other, no dosing advice.

Signs that RAD-140 reaches the receptor3

22 women with advanced breast cancer, no comparison group

SHBG fell3 18 of 18
RAD-140 100.0%
PSA rose3 16 of 20
RAD-140 80.0%
Clinical benefit at 24 weeks3
RAD-140 18.2%

SHBG and PSA respond to androgens and served as signs that the receptor is activated. Median progression-free survival was 2.3 months.

Lab cabinet with metal shelves, stacked petri dishes on top, a glass muscle bundle in the middle, a glass brain below
The data come mainly from the lab and animal models. Symbolic image.

Research status

Where the research stands

On ClinicalTrials.gov there is exactly one study for RAD140: the completed phase 1 study in breast cancer. There are no studies in healthy people or on muscle gain. As of 26 Oct 2026. 7

  1. Preclinical Preclinical: slows breast cancer models with androgen and oestrogen receptors
  2. Phase 1 1 trial, 1 completed
  3. Phase 2 no registered trial
  4. Phase 3 no registered trial
  5. Approval not yet
Not approved. The registry lists only one phase 1 study, there is no approval anywhere.7

Apart from 1 phase 1 trial there is no registered trial in phase 2 or later. 7

Side effects

Documented in studies and case reports:

  • Suppression of the body's own testosterone axis, dose-dependent, with recovery times of weeks.
  • Falling HDL values, shifts in the lipid profile.
  • Liver values: RAD-140 has the densest liver-injury case literature among SARMs, monitoring here is not optional.
  • Anecdotally: irritability, aggression, sleep issues at higher doses.

Tolerability

Side effects in the phase 1 study

Share of women with the side effect during treatment. Without a placebo group, the disease itself contributes to some values.

73 of 100 RAD-140
Event RAD-140
Severe side effect (grade 3 or 4)3 73%
AST raised3 59%
ALT raised3 46%
Bilirubin raised3 27%
Vomiting3 27%
Decreased appetite3 27%

Side effects were attributed to RAD-140 itself in 77.3 percent, severe ones in 31.8 percent. Raised liver values and low phosphate were the most common severe findings (22.7 percent each).3

Practice

  1. Start low, 10mg is usually enough, do not chase the upper end.

  2. Limit cycles (often 8 weeks) and plan a real break afterwards.

  3. In official competition RAD-140 is banned and detectable in urine for weeks (WADA S1.2).

  4. Liver and blood values before and after a cycle make sense.

Two light blue dumbbells, a folded white towel and a water bottle on a wooden bench in a bright training room, a blue exercise ball behind

Storage

Store dry, cool and protected from light, out of reach of children. Keep the original container closed and mind the expiry date.

Three white tablet bottles on a bright shelf next to a folded light blue towel
Dry, cool and away from light. Symbolic image.
Level · RAD-140 (Testolone)

How the level builds up

One dose per day: each dose adds to what is left of the previous one.

Lexicon: Oral (daily)
Peak 3.22×Trough 2.22×
Day 8 · 9. dose
3.1× of the first dose
Plateau
from Day 8

96 % of the plateau after dose 9

Peak
3.22×

of the first dose

Trough
2.22×

before the next dose

Simplified model, values relative to the first dose, no dosing information. Dashed: the first dose alone, green: the plateau.

Related

Related compounds

Same receptors or a different path: all in the TPD lexicon.

FAQ

Common questions about RAD-140 (Testolone)

Short answers, each backed by the sources below.

How does RAD-140 work?

According to ChEMBL RAD-140 binds to the androgen receptor with a Ki of 7 nM and activated it in muscle cells in the lab. Yu and colleagues found that it activates the receptor in breast cancer cells but not in prostate cancer cells. That is the tissue preference SARMs aim for.82

Is RAD-140 approved?

No. On ClinicalTrials.gov there is a single study for RAD140, the completed phase 1 study in breast cancer (as of 26 October 2026). There are no studies in healthy people. Everything here is the state of research, not a recommendation.7

What did the phase 1 study show?

22 heavily pretreated women with breast cancer took RAD-140 daily. SHBG fell in all 18 women measured, PSA rose in 16 of 20, a sign of action at the receptor. After 24 weeks 18.2 percent had a benefit, one woman a partial response. Liver values rose often.3

What about the liver?

In the phase 1 study AST rose in 59.1 percent, ALT in 45.5 percent. In addition there are case reports. A 26-year-old had acute liver injury, his values normalised two months after stopping. A 24-year-old developed cholestatic liver injury after five weeks of use.345

Are there reports on the heart?

Yes, as a case report: Padappayil and colleagues describe a young man with possible acute myocarditis after self-use of RAD-140 for bodybuilding. A case report does not prove a link, but it shows what to watch for.6

Is muscle gain proven in humans?

No. The first description by Miller and colleagues shows anabolic effects in animal models. In humans there is only the phase 1 study in women with breast cancer, which did not measure muscle mass.13

Glossary

Terms explained briefly

Dotted words in the text open these explanations directly.

Androgen receptor
Docking site in the cell through which testosterone and related substances act.
AST and ALT
Liver values in the blood. When they rise, liver cells are being damaged.
Cholestasis
Bile congestion in the liver, often with jaundice and itching.
Ki
Measure of binding strength in the lab. The smaller the value, the tighter the substance binds.
Myocarditis
Inflammation of the heart muscle that can lead to rhythm disorders and heart failure.
Partial response
A tumour shrinks clearly but does not disappear completely.
Phase 1 study
First study in humans. It mainly tests safety, tolerability and blood levels.
PSA
Prostate-specific antigen. Made via the androgen receptor, in small amounts also in women.
SARM
Selective androgen receptor modulator: meant to activate the receptor mainly in muscle and bone.
SHBG
Protein in the blood that binds sex hormones. Androgens lower it.

Evidence

Sources

Show all 8 sourcesHide sources 6 Studies1 Trial registry1 Database checked 26 Oct 2026

Studies

  1. Discovery and preclinical characterization of RAD140

    Miller et al., ACS Medicinal Chemistry Letters, 2011

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  2. RAD140 slows breast cancer models with androgen and oestrogen receptors

    Yu et al., Clinical Cancer Research, 2017

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  3. First-in-human phase 1 study in breast cancer

    LoRusso et al., Clinical Breast Cancer, 2022

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  4. Case report: liver injury on RAD140

    Ladna et al., Journal of Medical Case Reports, 2023

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  5. Case report: cholestatic liver injury on RAD-140

    Leung et al., Ochsner Journal, 2022

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  6. Case report: myocarditis on RAD-140

    Padappayil et al., Cureus, 2022

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed

Trial registry

  1. Trials on RAD140 on ClinicalTrials.gov

    ClinicalTrials.gov, U.S. National Library of Medicine

    Checked 26 Oct 2026 via ClinicalTrials.gov API v2

Database

  1. Binding to the androgen receptor in ChEMBL

    ChEMBL, EMBL-EBI (CHEMBL1672635, Androgen-Rezeptor CHEMBL1871)

    Checked 26 Oct 2026 via ChEMBL

In the shop

RAD-140 (Testolone) in the catalog

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