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Background And Regulatory History — Evidence Review

By Editorial Desk · published 2026-01-03 · last reviewed 2026-01-24 · Topic

This is a working overview of anti-doping, written for readers who want more than a one-paragraph summary but less than a textbook.

This page was last updated on 2026-01-24 and is reviewed periodically as new material appears.

Background and Regulatory History

GW501516 acts on PPARδ, a nuclear receptor that helps regulate fatty acid oxidation and energy homeostasis. In animal studies, activation of this receptor was associated with increased endurance and changes in lipid metabolism. Human trials examined effects on blood lipids and other metabolic markers, but the compound did not advance to approval. Rodent studies later reported tumors in multiple tissues at doses used in those experiments. Whether those findings translate to human risk remains uncertain, and the clinical relevance of the animal data is still debated.

Regulatory bodies treat GW501516 as a prohibited substance in competitive sport. The World Anti-Doping Agency added it to the prohibited list, and it falls under classes covering metabolic modulators and hormone-related agents. It is not approved by drug regulators for human use, and it is not a lawful dietary supplement. Products sold under the cardarine name may contain unlisted ingredients or different compounds. Because no approved product exists, quality and identity are not guaranteed by pharmaceutical manufacturing standards.

Cardarine is a common name for the investigational chemical GW501516, also written GW-1516. It was developed as a peroxisome proliferator-activated receptor delta agonist for metabolic conditions such as dyslipidemia. Early research focused on lipid handling and energy use in skeletal muscle and other tissues. The compound was never approved as a medicine. In public discussion, it is often grouped with performance-enhancing substances, although its receptor target differs from that of anabolic steroids or selective androgen receptor modulators. Regulatory and health authorities have issued warnings about its use.

Background and Research Context

Cardarine is a common name for GW501516, a synthetic compound developed in the 1990s through research collaborations involving GlaxoSmithKline. It belongs to a class of molecules known as peroxisome proliferator-activated receptor delta agonists. Early studies explored its effects on lipid metabolism and energy expenditure in animal models. The compound was never approved as a human medicine, and clinical development was discontinued. In the years since, it has appeared in fitness and bodybuilding communities as a performance-enhancing substance. Regulatory agencies classify it as an unapproved drug.

PPARδ is a nuclear receptor that regulates gene expression related to fatty acid oxidation, glucose homeostasis, and mitochondrial function. GW501516 binds to this receptor with high affinity and activates downstream signaling in skeletal muscle and other tissues. Animal studies reported increased endurance and altered fuel preference, but human data remain limited and inconsistent. The precise relationship between receptor activation and observed physiological changes is still an area of active investigation. Researchers have also examined whether the compound affects inflammation or cell proliferation. No approved therapeutic indication exists for cardarine.

In laboratory settings, cardarine is studied as a tool compound for probing PPARδ biology. Published experiments often use cell cultures, rodent models, or isolated tissues. Some investigations focus on metabolic effects, while others assess potential risks such as carcinogenicity observed in long-term animal studies. Because human trials are sparse, most knowledge comes from preclinical work and adverse event reports. Scientific literature frequently notes the gap between animal findings and human outcomes. The compound is not a dietary supplement and is not intended for human consumption.

Cardarine at a glance

PropertyValueNotes
Common nameCardarineCommon internet and media name.
Research codeGW501516Also written GW-1516.
Drug classPPARδ agonistNot a selective androgen receptor modulator.
Development statusDiscontinuedClinical development halted after rodent cancer findings.
Regulatory statusProhibited in sportListed by WADA; not approved as medicine.

Cardarine as Investigational PPARδ Agonist

Cardarine is a synthetic compound also known as GW501516, GW-501516, and sometimes endurobol. It was developed as a selective agonist of peroxisome proliferator-activated receptor delta, a nuclear receptor involved in fatty acid oxidation and energy metabolism. The compound was studied in preclinical models for metabolic and cardiovascular conditions, but it did not become a marketed human medicine. In regulatory and anti-doping contexts, it is treated as a prohibited substance rather than a licensed medicine.

The pharmacological interest in cardarine centers on PPARδ activation and its downstream effects on lipid handling and mitochondrial function. In animal studies, PPARδ agonists have been associated with changes in exercise endurance and fatty acid utilization, though results vary by model and protocol. Human data remain sparse, and the absence of large controlled trials limits conclusions about efficacy. Researchers often describe the compound as a tool for probing PPARδ biology rather than a proven therapeutic agent.

Safety discussions about cardarine frequently cite rodent carcinogenicity findings reported in the 2000s. In those studies, treated animals developed tumors at multiple sites, leading sponsors to discontinue clinical development. The relevance of these findings to humans has not been resolved, but they are a major reason the compound is not approved. Current literature emphasizes uncertainty about long-term effects and the risks of unregulated use. Regulators and health agencies have not established a safe human exposure level.

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Mechanism and Detection

Preclinical research reported that GW501516 increased running endurance in mice and improved lipid profiles in some animal species. Early human trials explored effects on high-density lipoprotein cholesterol, triglycerides, and glucose handling, but the program was discontinued. Published human data are sparse and do not establish efficacy for any condition. Studies also examined PPAR delta in cancer biology, with conflicting findings across models. The relationship between receptor activation, tissue context, and disease risk remains an active area of investigation.

Anti-doping laboratories identify GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the usual matrix, and detection can occur after the parent compound has cleared from blood. The exact detection window depends on dose, formulation, individual metabolism, and assay sensitivity. Because the compound is prohibited at all times, athletes are subject to testing in and out of competition. Analytical methods continue to improve as new metabolites and designer analogs are characterized.

Regulation and Detection

Cardarine is frequently described as a fat-burning or endurance-enhancing supplement, but these claims exceed the available evidence. The compound is not a hormone, steroid, or selective androgen receptor modulator. Research articles discuss it as a tool compound for studying PPARδ biology, while anti-doping literature focuses on its abuse and detection. Quality of unapproved products is uncertain, and independent analyses have found impurities or incorrect labeling. Open questions include whether human cancer risk resembles that seen in rodents and how often non-athletes use the substance.

Cardarine has no approved therapeutic indication and is not marketed as a medicine. The World Anti-Doping Agency lists GW501516 as a prohibited substance at all times, covering both in-competition and out-of-competition periods. National laws vary: some countries treat it as an unapproved drug subject to import controls, while others have specific restrictions on sale for human consumption. It is often sold as a research chemical, a label that does not imply safety or legality. Enforcement actions have targeted online vendors and shipments.

Anti-doping laboratories identify GW501516 and related metabolites using liquid chromatography coupled with tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be analyzed. The method targets the parent compound and phase I and phase II metabolites, which extend the detection window. Because the substance is prohibited at all times, athletes can be tested outside competition. Detection limits and windows depend on the assay, sample type, and individual metabolism.

Notes from published material

== AZF1 / AZFa == The AZF1 (Azoospermia Factor 1) gene is likely located in the euchromatic part of the long arm in Yq11.23. AZF1 is 792kb long and just distal to the centromere of the Y chromosome. AZF1 genes are involved in spermatogenesis in the testes. Common phenotypic manifestations of deletions in this region are azoospermia and Sertoli cell-only syndrome. Men with a complete deletion in the AZFa region are unable to produce testicular spermatozoa for ICSI. There are several candidate genes in the AZFa region that have been shown to cause infertility in males: Ubiquitin Specific Peptidase 9, Y-Linked (USP9Y), DEAD Box RNA helices, Box3, Y-linked (DBY), Ubiquitously Transcribed Tetratricopeptide Repeat Containing, Y-linked (UTY), and Thymosin Beta 4, Y-Linked (TB4Y).

== External links == "Tacrolimus Injection". MedlinePlus. "Tacrolimus Topical". MedlinePlus. Tacrolimus at the U.S. National Library of Medicine Medical Subject Headings (MeSH) "FDA Approves New Use of Transplant Drug Based on Real-World Evidence". U.S. Food and Drug Administration (FDA). 30 September 2021. Archived from the original on 16 July 2021.

Inframammary: an incision made to the inframammary fold (natural crease under the breast), which affords maximal access for precise dissection of the tissues and emplacement of the breast implants. It is the preferred surgical technique for emplacing silicone-gel implants, because it better exposes the breast tissue–pectoralis muscle interface; yet, IMF implantation can produce thicker, slightly more visible surgical scars. Periareolar: a border-line incision along the periphery of the areola, which provides an optimal approach when adjustments to the IMF position are required, or when a mastopexy (breast lift) is included to the primary mammoplasty procedure. In periareolar emplacement, the incision is around the medial-half (inferior half) of the areola's circumference. Silicone gel implants can be difficult to emplace via periareolar incision, because of the short, five-centimetre length (~ 5.0 cm) of the required access-incision. Aesthetically, because the scars are at the areola's border (periphery), they usually are less visible than the IMF-incision scars of women with light-pigment areolae; when compared to cutaneous-incision scars, the modified epithelia of the areolae are less prone to (raised) hypertrophic scars. Transaxillary: an incision made to the axilla (armpit), from which the dissection tunnels medially, to emplace the implants, either bluntly or with an endoscope (illuminated video microcamera), without producing visible scars on the breast proper; yet, it is likelier to produce inferior asymmetry of the implant-device position.

Sources: en.wikipedia.org

Background from the literature

As the proliferation of aristocratic families throughout the French kingdom limited the prospects of most heirs, young knights were encouraged to seek land and riches beyond their homeland, with Normandy becoming a major source of such adventurers. Many Normans of Italy, France and England eventually served as avid Crusaders soldiers under the Italo-Norman prince Bohemund I of Antioch and the Angevin-Norman king Richard the Lion-Heart, one of the more famous and illustrious Kings of England.

Magnesium is the eighth-most-abundant element in the Earth's crust by mass and tied in seventh place with iron in molarity. It is found in large deposits of magnesite, dolomite, and other minerals, and in mineral waters, where magnesium ion is soluble. Although magnesium is found in more than 60 minerals, only dolomite, magnesite, brucite, carnallite, talc, and olivine are of commercial importance. The Mg2+ cation is the second-most-abundant cation in seawater (about 1⁄8 the mass of sodium ions in a given sample), which makes seawater and sea salt attractive commercial sources for Mg.

ProteoWizard is a set of open-source, cross-platform tools and libraries for proteomics data analyses. It provides a framework for unified mass spectrometry data file access and performs standard chemistry and LCMS dataset computations. Specifically, it is able to read many of the vendor-specific, proprietary formats and converting the data into an open data format. On the application level, the software provides executables for data conversion (msConvert, msConvertGUI and idConvert), data visualization (msPicture and seeMS), data access (msAccess, msCat, idCat and msPicture), data analysis (peekaboo and msPrefix14) and basic proteomics utilities (chainsaw). In addition, the project also hosts the Skyline software which helps to create, acquire and analyze targeted proteomics experiments such as SRM experiments. The main contributors to the project are the Tabb, MacCoss and Mallick research labs as well as Insilicos.

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine a selective androgen receptor modulator?

No. Cardarine is a PPARδ agonist, while selective androgen receptor modulators act on androgen receptors. The two classes differ in receptor target and downstream effects.

Why did clinical development stop?

Preclinical rodent studies reported cancers, including liver and bladder tumors, at tested doses. The human relevance of those findings is uncertain, but development was discontinued. No approved human product resulted.

Is cardarine approved for medical use?

No. It remains an investigational compound without approved therapeutic labeling. Sports regulators prohibit its use, and health agencies have warned against consuming it.

What is cardarine?

Cardarine is a common name for GW501516, a synthetic PPARδ agonist developed for research. It has not been approved as a medication in any country. It is classified as an unapproved drug and a prohibited substance in sport.

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