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Lexicon

Cardarine (GW-501516)

Not a SARM but a PPAR-delta agonist with an endurance profile, famous from exercise-mimetic research and infamous for the rodent cancer data.

2 min read 8 sources

White tablet bottle with a black TPD label for GW-501516 (Cardarine) on a white podium, next to a blue 3D molecule model in a bright lab
Phase 2 · not approved

Summary

At a glance

Sources checked on 26 Oct 2026

Running time of trained mice
+68 %

only together with training, no change without training1

Triglycerides in 2 weeks
-30 %

6 overweight men per group, liver fat -20%2

HDL cholesterol in 12 weeks
+16.9 %

268 people with low HDL, highest dose level3

Phase 3 trials in the registry
0 trials

development stopped after tumours in rodent studies7

  • Cardarine (GW501516) is not a SARM but an agonist at the PPAR-delta receptor. It does not act on the androgen receptor.8
  • In mice it raised endurance only together with training: running time +68 percent and running distance +70 percent compared with training alone. Without training endurance did not change.1
  • In humans there are short studies over 2 to 12 weeks. They showed better blood lipids, less liver fat and more fat burning in muscle.234
  • According to a review GlaxoSmithKline stopped development after rodent studies showed tumours in many organs. GW501516 never got past phase 2.58
  • Long-term human safety data are missing. Everything here is research status, not a recommendation.7
Profile

Updated May 2026

How long does it stay in the body?

Share left after one dose, calculated with a half-life of ~20 hours

Half-life ~20 hours
After 40 hours: 25 %
Hour 20 · 50 %Hour 24, next dose · 44 %Hour 40 · 25 %Hour 60 · 12.5 %Hour 100 · 3.1 %

Simplified model without an absorption phase, half-life from the TPD lexicon. The lexicon gives 16 to 24 hours, we calculate with the middle.

Class
PPAR-delta agonist

not a SARM

Use
Oral

daily

Half-life
approx. 16 to 24 hours
WADA
Banned

hormone and metabolic modulators

Sizes
10 mg

1 size in the shop

Contents 14 sections
  1. At a glance
  2. What is Cardarine?
  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 Cardarine?

Cardarine, also GW-501516, is often mentioned in the same breath as SARMs but is not one. It is an agonist at the PPAR-delta receptor, a switch in energy metabolism. It was originally developed by GlaxoSmithKline for metabolic disease.

In the community Cardarine is known mainly for its endurance and fat-burning profile. Equally important is an honest read of the animal data, see below.

Comparison

Exercise mimetics in the lexicon

Which switch each entry targets, as stated in the TPD lexicon. Tap a card to open its entry.

Simplified. In the mouse study AICAR (AMPK) worked even without training, GW1516 (PPAR-delta) only together with training. Ostarine is a SARM and is shown for comparison. 1

How it works

Through the PPAR-delta receptor Cardarine switches on programs in muscle cells tied to fat burning and oxidative metabolism. In animal models this shifted energy use toward fat and increased endurance performance.

Cardarine does not act on the androgen receptor, so it does not suppress the testosterone axis. It is hormonally neutral, which fundamentally separates it from the SARMs.

Where it acts

Where Cardarine acted in studies

Tap a point or a card. Colour = PPAR-delta, grey = observed.

  1. Skeletal muscle

    More fat burning, gene for fat transport into mitochondria (CPT1b) more active2

    PPARδ
  2. Liver

    Liver fat 20% lower after 2 weeks2

    Observed in trials
  3. Blood lipids

    HDL up to +16.9%, triglycerides -16.9%, LDL -7.3%3

    Observed in trials

Targets in the ChEMBL database8

Compound ChEMBL CHEMBL38943: one recorded mechanism, Agonist.

Peroxisome proliferator-activated receptor delta
Gene
PPARD
UniProt
Q03181
ChEMBL
CHEMBL3979
Action
Agonist
Translucent muscle fibres with glowing blue mitochondria, blue 3D molecules above and golden light points streaming into the fibres
PPAR-delta switches on fat-burning programmes in muscle. Symbolic image.

How to take it

Oral, usually once daily.

  • One dose per day is generally enough, some split because of the half-life.
  • Often taken before training.
  • With some water, with or without food.
Tablet bottle with a black TPD label for GW-501516 (Cardarine) next to a glass of water and a few white tablets
Taken orally, according to the entry usually once daily. 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 best-known study (Narkar, 2008) showed in mice that GW1516 together with training markedly increased the number of oxidative muscle fibers and endurance performance, a classic exercise-mimetic result.

The other side: GlaxoSmithKline stopped development after long-term animal studies at high doses showed increased tumors in several organs. That is the central reason Cardarine never reached approval. Human long-term safety data are missing. Anyone using Cardarine should know these animal data and not talk them away.

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.

Blood lipids after 12 weeks3

268 people with low HDL, largest reported change from baseline

HDL cholesterol3 highest dose level
GW501516 +16.9%
Apolipoprotein A-I3
GW501516 +6.6%
LDL cholesterol3
GW501516 -7.3%
Triglycerides3
GW501516 -16.9%
Apolipoprotein B3
GW501516 -14.9%
Free fatty acids3
GW501516 -19.4%

Values from the abstract, three dose levels against placebo. The abstract gives the largest change per value but no placebo values.

Metabolism after 2 weeks2

Overweight men, 6 per group, change from baseline

Triglycerides2
GW501516 -30%
Comparator: PPAR-alpha agonist -30%
Apolipoprotein B2
GW501516 -26%
LDL cholesterol2
GW501516 -23%
Liver fat2
GW501516 -20%
Fasting insulin2
GW501516 -11%
Oxidative stress2 urinary isoprostanes
GW501516 -30%

Values from the abstract. HDL stayed unchanged. The PPAR-alpha comparator only lowered triglycerides. Very small groups over a short time.

Endurance and muscle fibres in mice1

4 weeks, treadmill test, 9 animals each

Running time1 compared with training alone
Training with GW1516 (mice) +68%
Running distance1 compared with training alone
Training with GW1516 (mice) +70%
Type I fibres (share)1 compared with untrained mice
Training with GW1516 (mice) +38%
Endurance without training1 separate experiment with AICAR
AICAR without training (mice) +44%

Values from the full text. GW1516 alone did not raise endurance in untrained mice, not even after up to 5 months. Only AICAR worked without training.

Glass muscle model with red fibres and a glass running shoe on a lab bench, racks of blue tubes beside them
More endurance in mice only together with training. Symbolic image.

Research status

Where the research stands

ClinicalTrials.gov lists three trials with GW501516, all from 2003 to 2006 and completed. The phase 2 trial is counted here. A metabolic study with 13 men is entered as phase 4 although GW501516 was never approved. Another trial has neither a phase nor an end date. As of 26 Oct 2026. 7

  1. Preclinical Mice: more endurance only together with training
  2. Phase 1 no registered trial
  3. Phase 2 1 trial, 1 completed
  4. Phase 3 no registered trial
  5. Approval not yet
Not approved. ChEMBL lists GW501516 with phase 2 as the highest phase. According to a review GlaxoSmithKline stopped development because of tumours in rodent studies.8
Show all 1 phase 2 trial on a timelineHide timeline 1 completed 0 running 0 with results
Phase 2

Bar: start to primary endpoint (planned for running trials). Green = completed, blue = progress until 26 Oct 2026.

Side effects

  • Central point: increased tumor rate in long-term animal studies at high doses, the reason for the development stop.
  • Short term, users report few acute effects, which is exactly what hides the real risk.
  • No solid long-term human safety data.

Practice

  1. The animal tumor data are real, take them seriously rather than ignoring them.

  2. If at all, then low and not over long periods.

  3. Banned and detectable in official competition.

White running shoes, a light blue water bottle, a sports watch and a light blue towel on a wooden bench by the window

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 and a folded light blue towel on a white shelf
Dry, cool and protected from light in the closed original container. Symbolic image.
Level · Cardarine (GW-501516)

How the level builds up

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

Lexicon: Oral (daily)
Peak 1.77×Trough 0.77×
Day 3 · 4. dose
1.71× of the first dose
Plateau
from Day 3

96 % of the plateau after dose 4

Peak
1.77×

of the first dose

Trough
0.77×

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

A different path: all in the TPD lexicon.

FAQ

Common questions about Cardarine (GW-501516)

Short answers, each backed by the sources below.

Is Cardarine a SARM?

No. Cardarine (GW501516) is an agonist at the PPAR-delta receptor, a switch in fat metabolism. It does not act on the androgen receptor.8

Is Cardarine approved?

No. ChEMBL lists GW501516 with phase 2 as the highest phase. The registry lists three trials from 2003 to 2006, none of them in phase 3 (as of 26 October 2026).87

Why was development stopped?

According to a 2013 review GlaxoSmithKline stopped research because preclinical studies in rodents linked the drug to tumours in many organs. The human studies only ran for a few weeks, long-term data are missing.5

Does Cardarine alone raise endurance?

Not in the well-known mouse study. Untrained mice did not run longer with GW1516, not even after up to 5 months. Only together with 4 weeks of training did running time rise by 68 and running distance by 70 percent compared with training alone.1

What do human studies show?

After 2 weeks triglycerides fell by 30, LDL by 23 and liver fat by 20 percent in overweight men. In a 12-week study with 268 people HDL rose by up to 16.9 percent. A study with 13 men showed that the liver cleared more fat-rich particles from the blood.234

Which side effects are known?

There are no solid figures, the human studies were short. A case report describes a man with strongly raised liver values and muscle breakdown after Cardarine together with Ostarine, he recovered fully. The central risk remains the tumours in rodent studies.65

Glossary

Terms explained briefly

Dotted words in the text open these explanations directly.

Agonist
Substance that activates a receptor and so triggers a signal.
Androgen receptor
Binding site for testosterone and SARMs. Cardarine does not use it.
Exercise mimetic
Substance meant to mimic effects of endurance training in muscle.
Half-life
Time until half of a compound in the blood has been broken down.
HDL cholesterol
Cholesterol in particles that carry fat from the vessels to the liver. Often called good cholesterol.
Oxidative muscle fibres
Endurance fibres (type I) with many mitochondria. They draw energy mainly from fat and oxygen.
PPAR-delta
Receptor in the cell nucleus that controls genes for fat burning and energy metabolism, mainly in muscle.
SARM
Selective androgen receptor modulator. Acts on the androgen receptor, unlike Cardarine.
Testosterone axis
Control loop of brain and testes that steers the body's own testosterone production.
Triglycerides
Most common form of fat in the blood and in fat tissue.

Evidence

Sources

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

Studies

  1. AMPK and PPAR-delta agonists as exercise mimetics in mice

    Narkar et al., Cell, 2008

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed, PubMed Central
  2. PPAR-delta activation in overweight men over 2 weeks

    Risérus et al., Diabetes, 2008

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  3. Blood lipids on GW501516 in low HDL, 12 weeks

    Olson et al., Arteriosclerosis Thrombosis and Vascular Biology, 2012

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  4. How GW501516 changes fat transport in the blood

    Ooi et al., Journal of Clinical Endocrinology and Metabolism, 2011

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  5. Review of PPAR-delta agonists and the development stop

    Mackenzie et al., Life Sciences, 2013

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  6. Case report: poisoning after Cardarine and Ostarine

    Kintz et al., Toxics, 2021

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

Trial registry

  1. GW501516 on ClinicalTrials.gov

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

    Checked 26 Oct 2026 via ClinicalTrials.gov API v2

Database

  1. GW501516 in ChEMBL (phase and target)

    ChEMBL, EMBL-EBI (CHEMBL38943)

    Checked 26 Oct 2026 via ChEMBL API

In the shop

Cardarine (GW-501516) in the catalog

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