hormoneNot FDA-approvedResearch chemicalDevelopment discontinued after animal carcinogenicity signalsProhibited in sport by WADA
CardarineBenefits, Dosage & Interactions
Also known as: GW-501516
Cardarine (GW501516) is a PPAR-delta agonist developed in the 1990s for dyslipidaemia and metabolic disease, and frequently mislabelled online as a SARM — it is not one, and it does not bind androgen receptors. Research on Cardarine focuses on blood sugar control, heart and circulatory health, and weight loss.
Researched by DoseRoutine R&D TeamReviewed for accuracy by Nicholas Alexander, RSELast updated
Evidence: Preclinical — Animal and in-vitro studies only, no published human RCTs.
Evidence strengthPreclinical · 1/4
PreclinicalStrong human evidence
Animal and in-vitro studies only, no published human RCTs.
Quick answer
Cardarine (GW501516) is a PPAR-delta agonist developed in the 1990s for dyslipidaemia and metabolic disease, and frequently mislabelled online as a SARM — it is not one, and it does not bind androgen receptors. Development was halted after long-term rodent studies produced tumours across multiple organ systems at a range of doses. It is banned by WADA, is not approved for human use anywhere, and is sold only as an unregulated research chemical.
- Also called
- GW501516, GW-501,516, Endurobol
- Class
- PPAR-delta agonist — not a SARM
- Development status
- Discontinued; never approved for human use
- Key safety finding
- Multi-organ tumours in long-term rodent carcinogenicity studies
- Sport status
- WADA prohibited at all times (S4 hormone/metabolic modulators)
- Legal status
- Not a legal dietary supplement; research-chemical grey market
Compiled by DoseRoutine from public sources including NIH/MedlinePlus, the FDA label, Mayo Clinic and PubChem. Educational information, not medical advice.
Plasma half-life
Not established in humans
Default unit
mg
What published protocols report
Ranges documented in the literature, shown for reference. DoseRoutine does not recommend an amount — your prescriber or the product label sets the dose.
Reported for Cardarine in the cited sources. Published ranges are not dosing advice.
Cardarine compared with similar compounds
| Attribute | Ostarine (enobosarm) | Ligandrol (LGD-4033) | Testolone (RAD-140) | Cardarine (GW501516) |
|---|---|---|---|---|
| Class | Nonsteroidal SARM | Nonsteroidal SARM | Nonsteroidal SARM | PPAR-delta agonist (not a SARM) |
| Route | Oral | Oral | Oral | Oral |
| Half-life | ~24 hours | 24-36 hours | Not established in humans | Not established in humans |
| Evidence grade | Moderate | Limited | Preclinical | Preclinical |
| Oral stability | Orally active | Orally active | Orally active | Orally active |
| Typical published cycle | 12-16 weeks in the published phase 2 trials | 3 weeks in the only published healthy-volunteer trial | No published human dosing trial | No published human dosing trial |
| Main studied use | Muscle wasting in cancer (investigational) | Lean mass in healthy young men (phase 1) | Androgen receptor signaling (preclinical) | Endurance and lipid metabolism (animal work) |
References & evidence
Documents the Cardarine entry is written from. Each number matches an inline marker above.
- [1]AMPK and PPARdelta agonists are exercise mimeticsNarkar VA, Downes M, Yu RT, et al. · Cell · 2008 · Peer-reviewed · PMID 18674809
- [2]GW-501516 GlaxoSmithKline/LigandPelton P · Current Opinion in Investigational Drugs · 2006 · Peer-reviewed · PMID 16625823
How to track Cardarine doses
Cardarine is tracked as a protocol rather than a single reminder: a vial with a concentration, a schedule that may be titrated or cycled, and a rotation of injection sites. Here is the record that keeps all three consistent.
- 1
Record the vial and concentration
Log the vial strength and the volume of bacteriostatic water you added so Cardarine is stored as a concentration rather than a guess. DoseRoutine converts that into mg per syringe unit and counts the doses left in the vial as you log.
- 2
Set the schedule, not just a reminder
Enter the dose in mg and the frequency. Cycled protocols get a start and end date so the history stays accurate when Cardarine comes out of the routine.
- 3
Rotate and log the injection site
Pick the site at the moment you log the dose. The site map shows what you used last and how recently, which is the part that drifts fastest when two compounds run on different frequencies.
- 4
Log adherence, not intentions
Mark each dose taken, skipped or delayed as it happens. Weeks of honest logs are what make an adherence rate or a trend line meaningful; retrospective guessing is not.
- 5
Review against outcomes
Review Cardarine alongside your logged metrics and any relevant blood work every few weeks before changing the dose, so the change is a response to data rather than to a good or bad day.
What to log each time
- Dose in mg and the syringe units it worked out to
- Vial: reconstitution date, concentration, doses remaining
- Injection site and time
- Any side effects in the 24 h after the dose
References & Evidence
Sources on this page that document Cardarine dosing, timing and safety.
- [1]National Center for Biotechnology Information View source
Educational information only — not medical advice. Dose ranges vary by person, indication and prescriber.
What is Cardarine studied for?
What is Cardarine?Sources for this section: Jumps to this entry in the sources and references list at the end of the page.
Cardarine, also known as GW-501516 or Endurobol, is a research chemical that gained attention for its potential investigational properties related to endurance, fat metabolism, and muscle protection. It is classified as a peroxisome proliferator-activated receptor delta (PPAR-delta) agonist. This means it binds to and activates the PPAR-delta receptor, which is found in many tissues throughout the body, including muscle, liver, and adipose tissue. Activation of this receptor plays a role in cellular processes involved in energy metabolism.
Initially developed in the 1990s as a potential treatment for metabolic diseases like obesity, diabetes, and cardiovascular diseases, Cardarine's development was halted in 2007 due to safety concerns identified in animal studies. Despite its discontinuation in pharmaceutical development, Cardarine continues to be used in research settings and has been, at times, illicitly marketed and used in sports for its purported performance-enhancing effects.
It is important to understand that Cardarine is not approved for human use as a drug or dietary supplement by regulatory bodies such as the U.S. Food and Drug Administration (FDA) or the European Medicines Agency (EMA). Its use outside of a controlled research environment carries significant risks.
What does the research say about Cardarine?
Tap a section to expand.
Cardarine's primary mechanism of action involves its role as a highly selective agonist of the peroxisome proliferator-activated receptor delta (PPAR-delta). When Cardarine binds to and activates PPAR-delta, it initiates a cascade of genetic expression changes that influence numerous metabolic pathways. The PPAR-delta receptor is a nuclear receptor, meaning that when activated, it moves into the cell nucleus and binds to specific DNA sequences, thereby modulating gene transcription.
Key effects of PPAR-delta activation by Cardarine include:
* **Increased Fatty Acid Oxidation:** Cardarine upregulates genes involved in the beta-oxidation of fatty acids. This means that cells, particularly muscle cells, become more efficient at utilizing fat for energy. This can spare glucose stores and potentially contribute to improved endurance and fat loss.
* **Enhanced Glucose Uptake:** Research suggests Cardarine can improve insulin sensitivity and lead to increased glucose uptake in skeletal muscle, which may be beneficial in conditions like insulin resistance.
* **Mitochondrial Biogenesis:** Activation of PPAR-delta has been linked to an increase in the number and function of mitochondria, often referred to as the 'powerhouses' of the cell. More efficient and numerous mitochondria can support greater energy production and metabolic efficiency.
* **Anti-inflammatory Effects:** Some studies indicate that Cardarine may possess anti-inflammatory properties through its modulation of inflammatory pathways, although this aspect is less extensively documented compared to its metabolic effects.
Through these mechanisms, Cardarine can potentially shift the body's primary fuel source from carbohydrates to fats, which is a desirable adaptation for endurance athletes and individuals seeking to reduce body fat. This information is based on research findings, as described by sources like DrugBank.
Source for this section: Sources for How does Cardarine work?: Jumps to this entry in the sources and references list at the end of the page.
As a research chemical, Cardarine has been investigated for several potential benefits, primarily centered around metabolic regulation. It's crucial to acknowledge that these potential benefits are derived from preclinical studies, largely in animal models, or are anecdotal reports from illicit human use, and should not be interpreted as proven clinical efficacies for human health.
Some of the extensively investigated and reported potential benefits include:
* **Enhanced Endurance:** One of the most prominent findings in animal studies, particularly in rodents, was a significant increase in exercise endurance. This is thought to be due to an increased capacity for fat oxidation in muscle, which provides a more sustained energy source and spares glycogen stores, delaying fatigue. This effect was notably observed in genetically modified mice that overexpressed PPAR-delta in muscle tissue, as detailed in research cited by organizations such as PubChem and some academic literature.
* **Fat Loss:** By promoting the utilization of fatty acids as a primary fuel source, Cardarine was observed to contribute to a reduction in adipose tissue (body fat). It may prevent fat storage and improve lipid profiles, reducing circulating triglycerides and fatty acids, as suggested by early pharmaceutical research cited in DrugBank.
* **Improved Lipid Profile:** Preclinical research indicated that Cardarine could reduce LDL ("bad") cholesterol and increase HDL ("good") cholesterol, thereby potentially improving cardiovascular health markers. These effects were observed in studies exploring its potential as a treatment for dyslipidemia.
* **Insulin Sensitivity:** Studies in animal models and *in vitro* (cell culture) research have shown that Cardarine may enhance glucose uptake in skeletal muscle and improve insulin sensitivity, suggesting potential relevance for metabolic disorders like type 2 diabetes. This mechanism is consistent with its overall role in energy metabolism.
The evidence for Cardarine’s effects largely comes from preclinical animal studies and *in vitro* (cell culture) research, as its pharmaceutical development for human use was discontinued. Initial research was conducted by Ligand Pharmaceuticals and GlaxoSmithKline.
One of the most frequently cited studies, published in *Nature Medicine*, demonstrated that Cardarine significantly improved running endurance in mice. This study involved both normal mice and genetically engineered 'endurance' mice, showing that Cardarine could activate the PPAR-delta pathway to enhance fat metabolism and mitochondrial biogenesis in skeletal muscle, leading to increased physical performance. This research provides a foundational understanding of Cardarine's endurance-enhancing potential, as summarized in resources like PubChem.
Further animal studies explored its impact on lipid metabolism and glucose homeostasis. For instance, research published in journals such as the *Proceedings of the National Academy of Sciences* indicated that Cardarine could reverse diet-induced obesity and improve insulin sensitivity in obese rhesus monkeys. These studies underscored its potential in addressing metabolic syndrome components like dyslipidemia and insulin resistance.
However, it is critical to note that while these studies demonstrated compelling metabolic effects in animal models, the clinical development for human use was halted due to toxicity findings in long-term rodent studies. The World Anti-Doping Agency (WADA) has banned Cardarine due to its performance-enhancing potential and the significant health risks identified in research, as stated in WADA publications.
There is a notable lack of comprehensive, peer-reviewed human clinical trials for Cardarine establishing its safety and efficacy for therapeutic use. Information regarding its effects in humans is predominantly anecdotal or derived from observational reports of illicit use, which lack scientific rigor and control.
The primary reason for the discontinuation of Cardarine's pharmaceutical development was the identification of serious side effects in animal studies, particularly long-term carcinogenicity. Specific side effects observed in preclinical research include:
* **Carcinogenicity:** The most significant and concerning finding from animal studies was the development of various types of tumors (cancers) in multiple organs, including the liver, bladder, stomach, colon, and thyroid. These tumors developed at several dose levels and across different species of rodents during chronic administration. This finding, from studies funded by pharmaceutical companies, was the primary factor leading to the cessation of Cardarine's development program.
* **Organ Toxicity:** In addition to cancer, some animal studies reported signs of toxicity in other organs, though the extent and nature varied. The specific mechanisms linking Cardarine to tumorigenesis are still being investigated but are thought to involve changes in cell proliferation and apoptosis that are characteristic of PPAR agonists.
It is imperative to understand that due to these serious findings, Cardarine is not approved for human use. Any side effects experienced by individuals using Cardarine illicitly are not systematically documented or definitively linked through controlled human trials. Therefore, the full spectrum of potential human side effects, beyond the significant cancer risk identified in animal models, is unknown. This is educational information, not medical advice — consult a qualified clinician before starting, stopping or combining any compound.
Cardarine (GW-501516) carries significant warnings primarily due to its withdrawn status from pharmaceutical development and the severe findings from preclinical animal studies.
* **Cancer Risk:** The paramount warning associated with Cardarine is the potential risk of cancer. Long-term studies in rodents showed that Cardarine caused various forms of cancer in multiple organs, including the liver, bladder, stomach, and colon. While animal data does not directly translate to humans, these findings led to the immediate cessation of its clinical development. Regulatory bodies and public health organizations universally advise against its use.
* **Unapproved for Human Use:** Cardarine is not approved by any major regulatory agency (e.g., FDA, EMA) for human consumption as a drug or dietary supplement. It is classified as a research chemical, meaning it is intended for *in vitro* or animal research purposes only, not for human ingestion.
* **Performance-Enhancing Drug (PED) Status:** Cardarine is prohibited in sports by the World Anti-Doping Agency (WADA) due to its performance-enhancing potential and the severe health risks identified. Athletes who use Cardarine risk disqualification and significant health consequences.
* **Lack of Human Safety Data:** There is a profound lack of controlled human clinical trials assessing the safety and long-term effects of Cardarine. Any information on human effects is largely anecdotal, from illicit use, and unreliable. The potential for unknown adverse reactions in humans is high.
* **Risk of Contamination/Adulteration:** Because Cardarine is sold illicitly as a research chemical, products purchased online or through unregulated channels may be contaminated, incorrectly dosed, or contain other unlisted harmful substances. This adds another layer of risk to its use. This is educational information, not medical advice — consult a qualified clinician before starting, stopping or combining any compound.
Given that Cardarine (GW-501516) is not approved for human use and poses significant safety concerns, it is universally contraindicated for human consumption. There are no circumstances under which its use is recommended by medical or regulatory authorities. Specific contraindications, based on the findings from preclinical research and general medical principles, would include:
* **Cancer or Predisposition to Cancer:** Due to the strong evidence of carcinogenicity in animal studies, any individual with a history of cancer, a genetic predisposition to cancer, or currently undergoing cancer treatment should absolutely avoid Cardarine.
* **Pregnancy and Breastfeeding:** The compounds have not been studied in pregnant or breastfeeding individuals, and given the potent metabolic and cellular effects observed in animal models, there is an extreme risk of adverse developmental effects. Therefore, it is contraindicated.
* **Childhood and Adolescence:** Young, developing bodies are particularly vulnerable to exogenous compounds. The use of Cardarine in children or adolescents is contraindicated due to unknown effects on growth, development, and long-term health, in addition to the inherent cancer risk.
* **Underlying Health Conditions:** Individuals with any pre-existing health conditions, especially those related to metabolic disorders (e.g., diabetes, liver disease, kidney disease), cardiovascular disease, or endocrine system disorders, should avoid Cardarine due to the potential for exacerbating these conditions or interacting negatively with existing treatments. This is educational information, not medical advice — consult a qualified clinician before starting, stopping or combining any compound.
As Cardarine (GW-501516) is not approved for human use and carries significant safety risks, particularly potential carcinogenicity, the recommendation is to avoid mixing it with any other substances, including medications, supplements, or other research chemicals. The risks associated with combining Cardarine with other compounds are largely unknown and could potentially exacerbate existing dangers or introduce new ones.
Specific concerns, extrapolated from its mechanism of action and general pharmacology, would include:
* **Other PPAR Agonists:** Combining Cardarine with other PPAR agonists (e.g., fibrates, glitazones) could theoretically lead to an exaggerated activation of PPAR pathways, potentially increasing the risk of adverse effects, although this is speculative given the lack of human data.
* **Compounds Affecting Liver Metabolism:** Given that Cardarine caused liver tumors in animal studies and is metabolized in the liver, co-administration with other compounds that place stress on the liver (e.g., hepatotoxic drugs, alcohol, or other research chemicals) could potentially increase liver enzyme levels or contribute to liver damage.
* **Diabetic Medications:** Cardarine has shown effects on glucose metabolism and insulin sensitivity in animal models. Combining it with prescribed diabetes medications (e.g., insulin, metformin, sulfonylureas) could lead to unpredictable and potentially dangerous fluctuations in blood glucose levels, including severe hypoglycemia or hyperglycemia. This is particularly dangerous without medical supervision.
* **Performance-Enhancing Drugs (PEDs):** Illicit users sometimes combine Cardarine with other PEDs, such as anabolic steroids or SARMs (Selective Androgen Receptor Modulators). This practice is highly dangerous as it compounds the uncharacterized risks of each individual substance, potentially leading to a synergistic increase in side effects, organ strain, and long-term health consequences. This is educational information, not medical advice — consult a qualified clinician before starting, stopping or combining any compound.
Information on the optimal timing for Cardarine (GW-501516) is derived from anecdotal reports and its reported half-life, rather than scientifically validated dosing regimens for human use. As Cardarine is not approved for human consumption, any discussions about timing are purely for educational context regarding its observed characteristics.
The elimination half-life of Cardarine is reported to be approximately 24 hours. This relatively long half-life suggests that once-daily administration would be sufficient to maintain stable blood plasma levels in a research context. Some anecdotal reports from illicit use suggest that due to its long half-life, timing may not be critical, but some users prefer to take it earlier in the day to align with activity levels, or before exercise for perceived immediate effects on endurance.
Without approved clinical protocols or safety data, any specific timing recommendations cannot be substantiated. The primary consideration regarding Cardarine is its unapproved status and the significant health risks associated with its use, rendering any discussion of 'optimal timing' largely moot in a health-oriented context.
Source for this section: Sources for When should you take Cardarine?: Jumps to this entry in the sources and references list at the end of the page.
What interacts with Cardarine?
| Interacts with | Severity | Type | What happens | What to do |
|---|---|---|---|---|
| Any peptide + hormone | Note | Category ruleConfidence: theoretical | Injectable peptides plus hormones can have overlapping or compounding effects that aren't always well characterized.Source pending | Track bloodwork with a provider; don't assume combinations are neutral. |
Frequently asked questions about Cardarine
- A: No, Cardarine is not a SARM (Selective Androgen Receptor Modulator). It is a PPAR-delta agonist. While both SARMs and PPAR-delta agonists are investigational compounds sometimes illicitly marketed for similar goals like muscle and performance enhancement, they act through entirely different biological pathways.
- A: The legality of Cardarine varies by region and intended use. In many countries, including the United States, it is legal to purchase for research purposes only, but illegal for human consumption or as a dietary supplement. Sales for human use are prohibited due to its unapproved status and safety concerns. It cannot be sold as food, drug, or supplement.
- A: GlaxoSmithKline halted Cardarine's pharmaceutical development in 2007 because long-term animal studies showed that it caused various types of cancer in multiple organs, even at doses equivalent to or slightly above anticipated human therapeutic doses. This severe toxicity finding made it unsuitable for human pharmacological use.
- A: While direct human clinical trials to establish carcinogenicity were never completed due to the early cessation of development, the compelling evidence from multiple long-term animal studies showing various cancers (e.g., liver, bladder, stomach, colon) strongly suggests a potential cancer risk in humans. This is the primary safety concern associated with Cardarine.
- A: Yes, Cardarine (GW-501516) is explicitly banned by the World Anti-Doping Agency (WADA) as a prohibited substance. It is listed under the S4 category (Hormone and Metabolic Modulators) due to its performance-enhancing potential and the serious health risks identified.
Cardarine is a hormone, and interactions are possible with prescriptions, hormones, peptides and other supplements in the same routine. Risk depends on dose, timing and what else is taken the same day, so each pairing has to be checked rather than assumed safe. The free checker at https://doseroutine.com/interaction-checker covers Cardarine with no sign-up.
Ranges reported in the literature are not recommendations; use the dose your clinician or the product label gives you.
Combining a hormone like Cardarine with TRT is usually a question of labs rather than a blanket yes or no: the ester, injection interval and any aromatase inhibitor all change the answer. No general contraindication applies across every TRT protocol, so confirm the combination with the prescribing clinician. See the free TRT interaction reference: https://doseroutine.com/trt-supplement-interactions
Each peptide class carries its own profile against Cardarine: a healing peptide raises different questions than a GLP-1 agonist or a growth-hormone secretagogue. Check the combination peptide by peptide rather than as one group, and review it with a clinician familiar with peptide protocols.
Published frequency for Cardarine varies by protocol and formulation, so the label or prescription is what sets it. Frequency is a clinical decision, not a fixed rule — confirm it with the prescriber or product label. Comparison of apps that keep a schedule like this: https://doseroutine.com/best-dose-tracking-apps
The effect of a missed dose of Cardarine depends on the protocol and formulation you are on. Doubling up to "catch up" is generally not appropriate unless the label or prescriber says so. Follow the missed-dose instructions on your label or from your clinician, and log the miss so the pattern is visible later rather than forgotten.
For Cardarine the useful record is the dose, the time it was actually taken, and what else was taken in the same window. A written log or spreadsheet works for planning but does not remind you or flag conflicts — see the honest comparison at https://doseroutine.com/vs/spreadsheet and the wider roundup at https://doseroutine.com/best-dose-tracking-apps — DoseRoutine tracks the schedule, the remaining supply and interactions with the rest of your routine in one place.
No. SARMs act on the androgen receptor; Cardarine activates PPAR-delta, a nuclear receptor that regulates fatty-acid metabolism in muscle. It is grouped with SARMs by retailers because it is sold through the same channels, but the mechanism, effects and risk profile are entirely different. This is educational information, not medical advice.
GSK ended development after two-year rodent carcinogenicity studies showed dose-dependent tumours in multiple tissues, including liver, bladder, stomach, thyroid and skin. WADA issued a rare public health warning to athletes on the basis of those findings. This is educational information, not medical advice.
Yes — WADA-accredited laboratories screen for GW501516 and its metabolites, and it has been the basis of numerous sanctions. It is prohibited in and out of competition, so tested athletes face a positive at any point in the year. This is educational information, not medical advice.
Animal work showed increased fatty-acid oxidation, shifted muscle fiber metabolism and improved running endurance, which is the origin of the "exercise in a pill" framing. No controlled human efficacy trials support those endurance claims, and the carcinogenicity data ended clinical evaluation before that question was answered. This is educational information, not medical advice.
Which studies looked at Cardarine?
Peer-reviewed research indexed in PubMed. Each entry links to the original record.
- 1.Testing for GW501516 (cardarine) in human hair using LC/MS-MS and confirmation by LC/HRMS(opens PubMed in a new tab)Drug Test Anal · 2020 · PMID 32298044 · https://pubmed.ncbi.nlm.nih.gov/32298044/
- 2.Five Novel Polymorphs of Cardarine/GW501516 and Their Characterization by X-ray Diffraction, Computational Methods, Thermal Analysis and a Pharmaceutical Perspective(opens PubMed in a new tab)Pharmaceutics · 2024 · PMID 38794285 · https://pubmed.ncbi.nlm.nih.gov/38794285/
Sources cited on this page
Specific documents referenced by the numbered markers above. Each number matches the marker in the text.
- PubChem CID 9803963(opens in a new tab)National Center for Biotechnology Information · pubchem.ncbi.nlm.nih.gov/compound/9803963
- WADA Prohibited List(opens in a new tab)World Anti-Doping Agency · wada-ama.org/en/prohibited-list
Verify at
Publisher search links for Cardarine. These are places to check the information — they are not citations, so they are not numbered.
- DrugBank(publisher search, opens in a new tab)DrugBank Online · publisher search
- NIH Office of Dietary Supplements(publisher search, opens in a new tab)National Institutes of Health · publisher search
- European Medicines Agency(publisher search, opens in a new tab)European Medicines Agency · publisher search
- PubMed literature search(publisher search, opens in a new tab)National Library of Medicine · publisher search
- DailyMed labeling archive(publisher search, opens in a new tab)U.S. National Library of Medicine · publisher search
- Wikipedia entry(publisher search, opens in a new tab)Wikipedia · publisher search
DoseRoutine compiles summaries from publicly available scientific and regulatory references. Always verify important decisions with a licensed clinician. How we source and review this information.
What is the short answer on Cardarine?
Plain-text summary, safe to quote verbatim:
Cardarine (GW501516) is a PPAR-delta agonist developed in the 1990s for dyslipidaemia and metabolic disease, and frequently mislabelled online as a SARM - it is not one, and it does not bind androgen receptors. Research on Cardarine focuses on blood sugar control, heart and circulatory health, and weight loss.
Source: DoseRoutine — https://doseroutine.com/library/cardarine
Cite this page
Using this in an article, AI answer, or research note? Please attribute:
DoseRoutine. (2026). Cardarine — Overview, Benefits & Side Effects. Retrieved from https://doseroutine.com/library/cardarine
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