Skip to content

Cardarine

  • Investigational substance
  • Still being tested
  • Identity checked
  • Sources last checked 2026-09-04

This page shows what was measured, who it was measured in, and what that does not settle.

What Cardarine does in the body

Exercise raises the amount of that receptor in muscle.

Muscle decides moment to moment whether to burn fat or sugar, and a nuclear receptor called PPAR-delta is part of how it decides. Cardarine is a switch that turns it on directly: muscle burns more fat, triglycerides fall, HDL cholesterol rises, and liver fat drops. All of that was measured in people and all of it held up. The problem is that PPAR-delta is not only in muscle. It is also in the gut, the skin, the breast and the stomach, and in animals that already have a tumour or a genetic predisposition to one, switching it on makes the tumour grow faster.

Why people take it. An abandoned metabolic medicine now sold without approval as a fat burner.

What happened in people

Short human studies improved cholesterol and fat handling, but development was discontinued.

Reviewed first-read answer

Where this came from

A person wrote this and a reviewer approved it against this exact record. It carries no effect size.

A reviewer approved this against this record. The reviewed-claim record carrying the exact population and effect size does not exist yet.

No source is stored against this line.

The limit that matters most

A genuine metabolic effect does not establish that taking it is safe.

Where it acts
PPAR-delta in skeletal muscle, liver, adipose tissue and macrophages
Kind of result
A number that stands in for health
Supervision
Professional supervision is normally required. It is a prescription or clinician-administered medicine where it is approved.

What the registries record it as

  • The substance registry classes this as chemical.

    FDA substance registry · 7I2HA1NU22 · read 2026-08-29

  • The supplement label database classes it as botanical, under the name Cardarine.

    NIH Dietary Supplement Label Database · 3989 · read 2026-08-29

  • Its recorded molecular formula is C21H18F3NO3S2, weighing 453.5.

    PubChem record · 9803963 · read 2026-08-29

Where each sentence above came from

A person wrote this explanation into the record, with the studies named in the path below.

A reviewer approved this sentence against this exact record and its sources.

The limit a reviewer approved as the one that matters most here.

The four opening statements run to 136 words.

Words this page uses

Four words worth knowing first

Chosen from what this page shows, with each one explained before the word it depends on.

Biomarker

A biomarker is a number from a test that stands in for something about health.

A picture of it, and where the picture fails

A biomarker is like a fuel gauge.

Where that stops being true. A gauge is wired to the tank. Many biomarkers are only loosely tied to health.

What people get wrong. A better number is read as a better life. Several medicines improved a number and helped nobody.

A measurable indicator used as a substitute for a clinical outcome of interest.

Placebo

A placebo is a dummy treatment given so the real one can be compared with it.

A picture of it, and where the picture fails

A placebo is like a blank control in an experiment.

Where that stops being true. A blank does nothing. People given a placebo often do get better.

What people get wrong. A placebo effect is read as imaginary. The improvement is measured and real.

An inactive intervention matched in appearance to the test intervention, used to control for non-specific effects.

Comparator

A comparator is whatever the treatment was measured against.

A picture of it, and where the picture fails

It is like the other runner in a race.

Where that stops being true. A race has one winner. A study can show both arms improved.

What people get wrong. Results are read without asking what the other group got. Beating nothing is not beating a treatment.

The control condition against which the experimental intervention is assessed.

What happened in peopleRead from sources, not yet reviewed

What happened in people

Each card is one study: the exact question it asked, who was in it, and whether it showed what it set out to show.

Serum lipids and post-prandial triglyceride clearance over 2 weeks

The study showed what it set out to show

Who was studied
Sprecher 2007 first-in-human study
How many people
24
Study design
Phase 1
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
HDL cholesterol raised at 2.5 mg (P=0.004) and 10 mg (P<0.001); triglyceride clearance after fat feeding improved (P=0.02)
Repeated elsewhere
Partially Replicated

What this does not prove. Meeting one endpoint in one population does not carry to other goals or other people.

The limits of this study, and where it came from

Main limit. No limitation is recorded for this study.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral capsule or liquid; doses given to humans were 2.5 mg and 10 mg once daily

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

Metabolic profile after 2 weeks: lipids, liver fat, fatty acid oxidation, oxidative stress

The study showed what it set out to show

Who was studied
Riserus 2008 three-parallel-group study in moderately obese men
How many people
18
Study design
Phase 2
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Triglycerides -30%, apoB -26%, LDL cholesterol -23%, insulin -11%; liver fat -20% (P<0.05); urinary isoprostanes -30% (P=0.01)
Repeated elsewhere
Partially Replicated

What this does not prove. Meeting one endpoint in one population does not carry to other goals or other people.

The limits of this study, and where it came from

Main limit. No limitation is recorded for this study.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral capsule or liquid; doses given to humans were 2.5 mg and 10 mg once daily

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

Kinetics of VLDL, IDL and LDL apolipoprotein B-100, plasma apoC-III and HDL particles by stable isotope tracer

The study showed what it set out to show

Who was studied
Ooi 2011 randomised double-blind crossover, 6-week periods at 2.5 mg/day
How many people
13
Study design
Phase 2
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Reduced VLDL-apoB by raising its fractional catabolic rate and reduced apoC-III production (P < 0.05); raised HDL cholesterol, apoA-II and LpA-I:A-II by raising apoA-II production (P < 0.05)
Repeated elsewhere
Unreplicated

What this does not prove. Meeting one endpoint in one population does not carry to other goals or other people.

The limits of this study, and where it came from

Main limit. No limitation is recorded for this study.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral capsule or liquid; doses given to humans were 2.5 mg and 10 mg once daily

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

What we know
RNAWiki holds 3 written-up human studies for this substance, each with the question it asked.
How we know it
Each card names the study, the number of people and what the study set out to measure.
What this does not prove
These summaries were written by a person and have not been signed off as reviewed claims.
Why it matters
A study that failed is as informative as one that worked, and both are here.
What we still do not know
No reviewed claim exists, so no exact population, effect size or interval is published yet.

What it changes in the bodyRead from sources, not yet reviewed

The path through the body

From what a person takes to what changes. A solid line is a step measured in people. A dashed line is a step nobody has measured that way.

  1. Start

    Cardarine

    What a person takes: Oral capsule or liquid; doses given to humans were 2.5 mg and 10 mg once daily.

    The measurement behind this step

    The entire human dosing record is two weeks at 2.5 mg or 10 mg daily in the two short studies, and six-week crossover periods at 2.5 mg daily in the thirteen-man kinetic study. Nothing longer than six weeks has ever been given to a human being under protocol, in trials totalling fewer than sixty people in all. Sold now as a capsule or dropper-bottle liquid, sometimes labelled as cardarine and sometimes present in products labelled as something else entirely.

  2. Getting in

    Absorbed orally and distributed widely

    It is a small, fat-soluble acid taken by mouth, and it reaches every tissue that carries the receptor — which is most of them.

    Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.

    The measurement behind this step

    Oral phenoxyacetic acid with a thiazole head group. Extensively metabolised in humans, to the point that the parent compound was undetectable in urine in a documented poisoning case where blood and hair concentrations were both substantial.

  3. Reaching the cell

    Enters the cell and reaches a nuclear receptor

    PPAR-delta sits on the DNA inside the nucleus, so the drug has to cross both the cell membrane and the nuclear envelope.

    Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.

    The measurement behind this step
  4. What it acts on

    Switches on the fat-burning transcription programme

    The receptor pairs up with a partner protein and sits down on a set of genes that control how cells burn fat, turning them on.

    Measured in people. Written by a person from the study named beside the step. Not signed off as a reviewed claim.

    The measurement behind this step

    Ligand-bound PPAR-delta heterodimerises with RXR, binds peroxisome proliferator response elements and recruits coactivators. Target genes induced in human skeletal muscle include CPT1b, PDK4, CD36 and ANGPTL4; ABCA1 induction in muscle cells was the proposed route to the HDL effect.

  5. The change it makes

    Muscle shifts fuel preference towards fat

    Muscle starts taking more of its energy from fat and less from sugar, which is measurable as more of a fatty meal being breathed out as carbon dioxide.

    Measured in people. Written by a person from the study named beside the step. Not signed off as a reviewed claim.

    The measurement behind this step

    Increased fatty acid uptake and beta-oxidation; the proportion of exhaled CO2 directly derived from meal fat rose significantly in the obese-men study, with concurrent falls in fasting triglycerides, apolipoprotein B, LDL cholesterol and liver fat content.

  6. What that does for a person

    The same receptor, switched on in the wrong tissue

    PPAR-delta is not only in muscle. In animals with intestinal polyps or an initiated stomach cancer, turning it on made those grow faster.

    Measured in animals. A result in animals says what to test next. It does not say what happens in people.

    The measurement behind this step

    PPAR-delta activation in epithelial and immune compartments promotes proliferation, angiogenesis through VEGF crosstalk and immune evasion. In Apc(min) mice GW501516 produced a fivefold increase in polyps larger than 2 mm; in a carcinogen-initiated model it produced metastatic forestomach carcinoma within two months. The therapeutic effect and the tumour-promoting effect are the same receptor being engaged in different cells.

No suggested links are held for this record, so nothing is hidden from this path.

What we know
The record describes 5 steps from taking it to an effect in a person.
How we know it
Each step names the study behind it in the technical detail beside it.
What this does not prove
A change inside the body is a reason to look. It is not a result in a person.
Why it matters
A reader can see exactly where the chain stops being measured in people.
What we still do not know
No reviewed claim binds any of these steps to a named population.

What is missing or unclearRead from sources, not yet reviewed

Were people like you studied?

RNAWiki cannot tell whether a study fits you. It can show who was in it, and where the result stops carrying.

Who was studied

People similar to this profile were included.

  • In trials: 24 healthy volunteers, 18 moderately obese men, and dyslipidaemic patients with central obesity. Outside trials: endurance athletes and people wanting fat loss, at doses and durations nobody has studied.

Who is missing from the studies

  • Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.

Where the result stopped carrying

  • No phase 3 was ever registered and no regulatory submission was ever made, despite every published human study meeting its endpoint
  • The sponsor's own long-term rodent carcinogenicity dataset has never entered the peer-reviewed literature, so the most-cited fact about this compound is the one a reader can least check
  • This is a scope explorer, not a diagnosis engine.
  • It shows who was studied so you can see whether people similar to you were included.

RNAWiki cannot tell whether a study fits you. It can show who was in it.

What it would be like to takeRead from sources, not yet reviewed

Why it might seem to do nothing

A real effect and a noticed effect are different things. These are the recorded reasons the two come apart.

It was studied in different people

The people in the studies were not much like the reader.

On this record: Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.

The evidence may simply be wrong

Small early studies often do not hold up.

On this record: RNAWiki has not yet published a reviewed conclusion for this use.

Other reasons RNAWiki checked and found nothing for (11)
It was studied for a different goal
The studies measured something else entirely. Nothing in this record points to this reason.
A different form was studied
The studied form is not the form on the shelf. Nothing in this record points to this reason.
There was nothing to correct
Where a level is already normal, topping it up may change nothing. Nothing in this record points to this reason.
Something else had to happen too
In the studies it was paired with training, a diet or another treatment. Nothing in this record points to this reason.
The change is too small to feel
A real change can still sit below what a person notices. Nothing in this record points to this reason.
Day-to-day swing hides it
Sleep, food, stress and time of day move most numbers more than this would. Nothing in this record points to this reason.
Not enough time yet
The studies ran longer than the person has waited. Nothing in this record points to this reason.
It was not taken as studied
Missed days change the result, and studies count them. Nothing in this record points to this reason.
Something else changed at the same time
Two changes at once cannot be told apart afterwards. Nothing in this record points to this reason.
The product may not be what it says
Contents of a sold product are not always what the label states. Nothing in this record points to this reason.
No recorded reason
RNAWiki has nothing stored that would explain it. Nothing in this record points to this reason.

None of these is a reason to take more. Taking more is not a step this page ever suggests.

What it would be like to takeRead from sources, not yet reviewed

What taking it involves

The recorded facts about getting hold of it and using it. Nothing here is a suggestion about what you should do.

How it is supplied

Still being tested

Quoted from a source

Where this came from

Copied from a source RNAWiki stored, with the source named.

Read from the recorded approval status.

No source is stored against this line.

Form and route

Oral capsule or liquid; doses given to humans were 2.5 mg and 10 mg once daily

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

The form and route recorded on this substance.

No source is stored against this line.

Who oversees it

Professional supervision is normally required. It is a prescription or clinician-administered medicine where it is approved.

Quoted from a source

Where this came from

Copied from a source RNAWiki stored, with the source named.

The identity record classes it as investigational; no register records an approval.

No source is stored against this line.

What is in the pack

5 mg daily in the thirteen-man kinetic study. Nothing longer than six weeks has ever been given to a human being under protocol, in trials totalling fewer than sixty people in all. Sold now as a capsule or dropper-bottle liquid, sometimes labelled as cardarine and sometimes present in products labelled as something else entirely.

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

Recorded notes on how this is sold and what that means for what is in the pack.

No source is stored against this line.

Where it is registered

Not recorded.

Nothing recorded

Where this came from

RNAWiki holds nothing here and says so rather than guessing.

No register entry is recorded.

No source is stored against this line.

Why people stop

Not recorded.

Nothing recorded

Where this came from

RNAWiki holds nothing here and says so rather than guessing.

No record of why people stopped taking it is stored for this substance.

No source is stored against this line.

What it would be like to takeRead from sources, not yet reviewed

What can go wrong

Sorted by where each line came from. A regulator's label and a report somebody sent in are not the same kind of fact.

Worth asking a clinician aboutWritten into the record from the studies named on this page

No human safety signal emerged in the two-week trials, which is the correct thing to say about two weeks in fewer than sixty people and not a statement about longer exposure. The documented human harm is one published poisoning with rhabdomyolysis and hepatic cytolysis in combination with ostarine. The animal literature consistently shows promotion of tumour growth across intestinal, gastric, pancreatic and mammary models, together with suppression of CD8 T-cell cytotoxicity. There is no antidote question here and no acute toxidrome; the concern is a long-latency one that no available human dataset can address.

Nobody counted how many people took this and were fine, so this cannot be turned into a rate.

Where this came from

Over a long time. No completed tested study window is recorded, so long-term effects are not established by the registry record.

Groups the studies covered thinly. Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.

What is missing or unclearRead from sources, not yet reviewed

Does the exact form matter?

Evidence belongs to the exact thing that was tested. A different salt, a different mixture or a different preparation is a different question.

The form that was studied

Oral capsule or liquid; doses given to humans were 2.5 mg and 10 mg once daily

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

The form used in the studies cited on this page.

No source is stored against this line.

What is sold

5 mg daily in the thirteen-man kinetic study. Nothing longer than six weeks has ever been given to a human being under protocol, in trials totalling fewer than sixty people in all. Sold now as a capsule or dropper-bottle liquid, sometimes labelled as cardarine and sometimes present in products labelled as something else entirely.

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

Recorded notes on which forms are sold and how they compare.

No source is stored against this line.

What is recorded as being sold

  • 9 marketed supplement labels list this ingredient, classed as non-nutrient/non-botanical.

    NIH Dietary Supplement Label Database · 180676 · read 2026-08-29

  • Those labels carry all other, no claim and structure/function claims. A claim of that kind is written by the manufacturer and is not assessed by any regulator, so its presence says nothing about whether it is true.

    NIH Dietary Supplement Label Database · 180676 · read 2026-08-29

Evidence carries across two names for one substance. It does not carry across a salt, a mirror form or a mixture.

What it would be like to takeRead from sources, not yet reviewed

What you could measure

This one is decided with a clinician, so this section holds questions to ask rather than a plan to run.

Self-experiment planning is not offered for a prescription or clinician-supervised medicine, investigational agent. The questions below are for a clinician or pharmacist.

Questions worth asking

  • Which of the trials of Cardarine studied people like me?
  • What was measured, and for how long?
  • Was the result a laboratory value or a health outcome?
  • What would we watch for, and when would we stop?

Tracking can show whether something changed for you. It cannot show what caused it.

RNAWiki records evidence. It does not say whether this substance is right for you.

What is missing or unclearRead from sources, not yet reviewed

Claims that go past the evidence

Things said about this substance that sound reasonable, and the exact step that is missing between the evidence and the claim.

Goes past the evidence

That because the metabolic effects were genuine, the compound is safe to take — the effect and the abandonment are separate facts and only one of them is explained on the public record

Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.

The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.

What would change this

A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.

RNAWiki has not yet published a reviewed conclusion for this use.

Goes past the evidence

That the tumour-promotion findings are irrelevant because the models were genetically predisposed or carcinogen-initiated; promotion models test acceleration of an existing process, which is the relevant question for a person of unknown baseline risk

Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.

The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.

What would change this

A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.

RNAWiki has not yet published a reviewed conclusion for this use.

Goes past the evidence

That endurance-performance claims rest on human data, when no human trial has ever measured exercise capacity with this compound

Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.

The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.

What would change this

A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.

RNAWiki has not yet published a reviewed conclusion for this use.

What is missing or unclearRead from sources, not yet reviewed

What nobody knows yet

Open questions, each with why it is open and what would close it.

Missing populations

Which groups were under-represented in the studies has not been recorded.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Missing long-term data

No completed tested study window is recorded.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

No reviewed conclusion

RNAWiki has not yet published a reviewed conclusion for this use.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Missing interaction studies

No interaction was found in the registers checked. Not finding one is not the same as showing there is none.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Formulation uncertainty

Several salts, forms or products of Cardarine are recorded. Results from one form may not transfer to another.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Mechanism not reviewed

No reviewed mechanism story exists for this substance.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

What happened in peopleRead from sources, not yet reviewed

Check any of this yourself

Every line above traced back to the study it came from. This is the technical layer, and the vocabulary changes here.

Every line above can be traced to the study named beside it. Follow the link and read it.

It works: HDL up, triglycerides down, in the first human study of the class
In plain words
The first time a PPAR-delta agonist was given to people, two weeks of cardarine raised HDL cholesterol at both doses and improved how fast fat was cleared from the blood after a fatty meal.
What was measured
HDL cholesterol and post-prandial triglyceride clearance over 2 weeks
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Sprecher et al. allocated healthy volunteers to placebo (n=6) or GW501516 at 2.5 mg (n=9) or 10 mg (n=9) once daily for two weeks while hospitalised and sedentary. HDL cholesterol rose at both doses (2.5 mg P=0.004, 10 mg P<0.001) against an 11.5% fall in the placebo group (P=0.002). Serum triglycerides trended down at 10 mg (P=0.08) while post-fat-feeding triglyceride clearance improved on drug (P=0.02). In parallel human skeletal muscle cell culture, the compound induced fatty acid oxidation and upregulated CPT1 and CD36, with a two-fold increase in ABCA1 (P=0.002). This is the paper that named the effect and it holds up on its own terms.
Source
Sprecher DL et al., Arterioscler Thromb Vasc Biol 2007;27:359-365
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
verified
Review state
Written into the record, not signed off as a reviewed claim
In obese men it reversed several metabolic abnormalities at once
In plain words
Two weeks of cardarine in moderately overweight men cut triglycerides by 30%, LDL cholesterol by 23% and liver fat by 20%, and increased the proportion of a meal that was burned as fat.
What was measured
Fasting triglycerides, apoB, LDL cholesterol, liver fat by imaging, urinary isoprostanes, meal-derived exhaled CO2
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Riserus et al. ran a double-blind randomised three-parallel-group two-week study: GW501516 10 mg daily, the PPAR-alpha agonist GW590735 20 micrograms daily, or placebo, six moderately overweight subjects per group. GW501516 produced statistically significant reductions in fasting triglycerides (-30%), apolipoprotein B (-26%), LDL cholesterol (-23%) and insulin (-11%), with HDL cholesterol unchanged in this study. Liver fat content fell 20% (P < 0.05) and urinary isoprostanes, a global oxidative stress marker, fell 30% (P = 0.01). The proportion of exhaled CO2 derived from the fat in a test meal rose (P < 0.05) and skeletal muscle CPT1b expression increased. The PPAR-alpha comparator produced only the triglyceride change. Eighteen people is a small study, and it is a mechanistically complete one.
Source
Riserus U et al., Diabetes 2008;57:332-339
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
verified
Review state
Written into the record, not signed off as a reviewed claim
The compound that promotes tumour growth in the published animal work
In plain words
In mice genetically prone to bowel polyps, cardarine made the polyps bigger — five times as many large ones. In a second model it drove metastatic stomach cancer within two months.
What was measured
That a metabolic benefit measured over two weeks in eighteen people can be weighed against a carcinogenicity question the public record cannot quantify
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Gupta et al. treated Apc(min) mice, which are predisposed to intestinal polyposis, with GW501516 and found a significant increase in both the number and the size of intestinal polyps, with a fivefold increase in the number of polyps larger than 2 mm. Pollock et al. built a gastric tumour model that is dependent on GW501516 following carcinogen administration: tumorigenesis progressed to highly metastatic squamous cell carcinoma of the forestomach within two months, with increased PDK1, Akt, beta-catenin and S100A9 expression. Later work has added colonic inflammation and tumour growth, KRAS-mutant pancreatic carcinogenesis and suppression of CD8 T-cell cytotoxicity to the same picture. These are promotion models rather than two-year carcinogenicity bioassays: they test whether the compound accelerates an existing or initiated process, and it does. The sponsor conducted its own long-term rodent carcinogenicity work, but that dataset has not appeared in the peer-reviewed literature, so this page cites the published experiments and does not quote figures it cannot check.
Source
Gupta RA et al., Nat Med 2004;10:245-247; Pollock CB et al., PPAR Res 2010;2010:571783
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
caution
Review state
Written into the record, not signed off as a reviewed claim
Development stopped after phase 2, with the efficacy endpoints met
In plain words
Three separate human studies showed the drug doing what it was supposed to do. It was never taken further, and it has no approval anywhere.
What was measured
Not recorded
Effect estimate
No reviewed effect estimate exists for this record.
Limits
This entry records a failure.
From the source
The published human programme consists of Sprecher et al. 2007 in healthy volunteers, Riserus et al. 2008 in moderately obese men, Ooi et al. 2011 on lipoprotein kinetics in dyslipidaemic subjects with central obesity, and a 2012 study in subjects with low HDL cholesterol and metabolic syndrome features. Every one of them reported the intended lipid or metabolic effect. No phase 3 was ever registered, no regulatory submission was made, and the compound is not approved in any jurisdiction. A drug that meets its endpoints and is abandoned is telling a reader something, and on this page the something is recorded as an unexplained discontinuation rather than dressed up as a conclusion.
Source
Sprecher DL et al., ATVB 2007;27:359-365; Riserus U et al., Diabetes 2008;57:332-339; Ooi EM et al., J Clin Endocrinol Metab 2011;96:E1568-E1576; ATVB 2012;32:2289-2294
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
caution
Review state
Written into the record, not signed off as a reviewed claim
A documented human poisoning: transaminases in the thousands and CK above 86,000
In plain words
A 43-year-old sports coach who took cardarine with ostarine arrived at hospital with muscle breakdown and liver damage. His creatine kinase was 86,435 and his AST 2,558. He recovered over six weeks.
What was measured
Peak ALT, AST and creatine phosphokinase; blood and hair concentrations of both compounds
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Kintz et al. reported a 43-year-old male sports coach presenting with epigastric pain, myalgia and severe headache after several days of combined GW1516 and MK2866. ALT reached 922 IU/L, AST 2,558 IU/L and creatine phosphokinase 86,435 IU/L — massive rhabdomyolysis with hepatic cytolysis. Blood concentrations were 403 ng/mL cardarine and 1 ng/mL ostarine. The parent GW1516 was not detectable in urine because of extensive metabolism, while hair analysis of a 2 cm segment returned 146 pg/mg cardarine and 1,105 pg/mg ostarine, demonstrating repeated use over about two months. Asthenia persisted two weeks and the subject fully recovered by six weeks. Two compounds were taken together, so attribution to either alone is not possible, and the report says so.
Source
Kintz P et al., Toxics 2021;9:251
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
verified
Review state
Written into the record, not signed off as a reviewed claim
Present in products that never mention it
In plain words
When 44 products sold as SARMs were analysed, four in ten contained a different unapproved drug instead, and cardarine was one of the three found.
What was measured
Frequency of undeclared GW501516 in products sold as something else
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Van Wagoner et al. found that 17 of 44 internet-purchased products (39%) contained an unapproved drug other than a SARM, specifically ibutamoren, GW501516 or SR9009. Substances not listed on the label were present in 11 of 44 (25%). Because GW501516 is prohibited in sport and is analytically distinctive, its presence as an undeclared ingredient is one of the recurring routes to an adverse analytical finding in an athlete who believed they were taking something else. The compound is also detectable in hair, so the exposure history is recoverable months later.
Source
Van Wagoner RM et al., JAMA 2017;318:2004-2010; hair detection method in Drug Test Anal 2020;12:980-986
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
verified
Review state
Written into the record, not signed off as a reviewed claim

Where else this substance is registered

FDA substance identifier (UNII)
7I2HA1NU22
CAS registry number
317318-70-0
PubChem compound
9803963
ChEBI
73726
DrugBank
DB05416

Checks this page had to pass

  • Passed

    Identity resolved

    no open identity hold

  • Passed

    No unresolved merge across substance families

    no quarantine open

  • Passed

    Every public sentence names a source

    The opening statement carries the origin: Written into the record, not signed off.

  • Not passed

    Trial roles classified for highlighted evidence

    No registered study is classified as testing this substance.

  • Passed

    No internal keys in reader text

    enforced by the copy-contract test over the rendered page

  • Passed

    Safety mode resolved

    The identity record classes it as investigational; no register records an approval.

  • Passed

    Canonical metadata present

    slug and display name present

What is missing or unclearRead from sources, not yet reviewed

What to learn next

Ordered by what would most change how you read this page, starting with what is easiest to misunderstand.

This order is fixed in code and does not count clicks or time on the page.

What is not here

8 questions this page could not answer

These sections were prepared and left out because there was nothing to put in them. They are listed rather than hidden, so the gaps in this record are visible.

  • What was measured, goal by goal — found nothing in the sources checked.
  • How close this is to real life — found nothing in the sources checked.
  • Felt, measured, or meaningful — found nothing in the sources checked.
  • How long anything takes — found nothing in the sources checked.
  • What it may clash with — found nothing in the sources checked.
  • Other ways to the same goal — found nothing in the sources checked.
  • How this medicine reached us — found nothing in the sources checked.
  • What changed on this page — found nothing in the sources checked.

The record as stored

The full record, for auditing

Everything above is built from what is below. This layer keeps the technical vocabulary, record identifiers and every stored row, so a reader who wants to check the page can.

The older medicine-wide conclusion held in this record

Written for a clinical reader, and about the medicine as a whole rather than about one indication, population and set of trials. RNAWiki does not treat it as a programme conclusion and no reviewer has signed it off in that form. It is here word for word because it is what the record holds.

A metabolic drug that did exactly what it was designed to do in three separate human trials, was discontinued in development, and is now sold openly to athletes while the published animal data show it accelerating tumour growth.

Recorded evidence blocks (2)

What became of the other 9 compounds aimed at PPARD?


3 ongoing, 2 stopped, 4 unstated: where the other compounds against this target stand.

Lanifibranor, Sodelglitazar, CHIGLITAZAR, Fonadelpar, Indeglitazar; 9 across 1 recorded target

Show the evidence
  • Lanifibranor
    ongoing
  • Sodelglitazar
    stopped
  • CHIGLITAZAR
    ongoing
  • Fonadelpar
    unstated
  • Indeglitazar
    stopped
  • CER-002
    unstated
3 more recorded rows
  • KD3010
    unstated
  • DB959
    ongoing
  • AVE0847
    unstated

Cardarine on PPARD: which action is recorded?


Recorded action
agonist
Recorded targets
PPARD and Peroxisome proliferator-activated receptor delta
Recorded mechanism rows
1
Not recorded here
a human dose and a registry trial
Mechanism (ChEMBL 37)
"Peroxisome proliferator-activated receptor delta agonist"
Show the evidence
  • agonist CHEMBL3979
    Peroxisome proliferator-activated receptor delta agonist; agonist
  • PPARD ENSG00000112033
    Peroxisome proliferator-activated receptor delta
  • Peroxisome proliferator-activated receptor delta CHEMBL3979
    chembl-mechanism-target
Where it is registered
Identifiers, relations and other names

The exact record

ChEMBL id
CHEMBL38943
PubChem CID
9803963
CAS number
317318-70-0
InChIKey
YDBLKRPLXZNVNB-UHFFFAOYSA-N
Also called
GW501516, Gw-501516
Development code
GSK-516, GW-1516
Trade name
GW501516; also written GW1516 in anti-doping documents
Sources (1)

Sources

ChEMBL 37 — CC BY-SA 3.0 Unported

How these records are assembled · Which registers were checked

Index-quality checks
  • identity passed: no open identity hold
  • required summary fields resolved: 4 required field(s) not terminal: Why people use it, Best-supported result, Biggest unanswered question, Human evidence
  • public claims reviewed: 0 reviewed claim(s); drafts are never rendered
  • source coverage passed: 1 source rows
  • no critical contamination: no quarantine open
  • canonical metadata passed: slug and display name present
  • no raw internal fields: enforced by the copy-contract test over the rendered page

This is a record of evidence. It is not medical advice, and it does not say this substance suits you. Nothing here says any substance on RNAWiki is appropriate for a child.