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Background And Regulatory History — Reference Sheet

By Editorial Desk · published 2026-05-21 · last reviewed 2026-06-08 · Data

The short version of anti-doping fits in a sentence. The long version — which is the one that helps — is below.

This page was last updated on 2026-06-08 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.

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.

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 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.

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.

Further detail

=== Cardiovascular === Heat shock proteins appear to serve a significant cardiovascular role. Hsp90, hsp84, hsp70, hsp27, hsp20, and alpha B crystallin all have been reported as having roles in the cardiovasculature. Hsp90 binds both endothelial nitric oxide synthase and soluble guanylate cyclase, which in turn are involved in vascular relaxation. The subset of hsp70, extracellular hsp70 (ehsp70) and intracellular hsp70 (ihsp70), has been shown to have a pivotal role in managing oxidative stress and other physiological factors. Krief et al. referred hspb7 (cvHSP - cardiovascular Heat shock protein) as cardiac heat shock protein. Gata4 is an essential gene responsible for cardiac morphogenesis. It also regulates the gene expression of hspb7 and hspb12. Gata4 depletion can result in reduced transcript levels of hspb7 and hspb12 and this could result in cardiac myopathies in zebrafish embryos as observed by Gabriel et al. hspb7 also acts in the downregulation of Kupffer vesicles which is responsible for regulation of left-right asymmetry of heart in zebrafish. Along with hspb7, hspb12 is involved in cardiac laterality determination. A kinase of the nitric oxide cell signalling pathway, protein kinase G, phosphorylates a small heat shock protein, hsp20. Hsp20 phosphorylation correlates well with smooth muscle relaxation and is one significant phosphoprotein involved in the process. Hsp20 appears significant in development of the smooth muscle phenotype during development.

=== Regulatory approval === Lurasidone was approved in the United States for the treatment of schizophrenia in October 2010 and for the treatment of depressive episodes associated with bipolar I disorder in June 2013. In 2015, lurasidone was studied for major depressive disorder with mixed features in a randomized trial and had a positive result, however it did not receive an FDA indication for it. In 2017, the FDA approved lurasidone for schizophrenia in adolescents age 13-17. In 2018, lurasidone was approved for bipolar depression in children and adolescents age 10-17. It received regulatory approval in the United Kingdom in September 2014. In October 2014, NHS Scotland advised use of lurasidone for schizophrenic adults who have not seen improvements with previous antipsychotics due to problems that arise from weight gain or changes in metabolic pathways when taking other medications. The Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) issued a positive opinion for it in January 2014, and it was approved for medical use by the EMA in March 2014. It was launched in Canada for the treatment of schizophrenia in September 2012, Health Canada giving their Summary Basis of Decision (SBD) as favourable on 15 October 2012. The European Commission has granted a marketing authorization for once-daily oral lurasidone for the treatment of schizophrenia in adults. It is approved for use in the EU. Generic versions of lurasidone were approved for use in the United States in January 2019 and became available in 2023.

Ukrainian President Volodymyr Zelenskyy claimed that air defences had shot down some thirty six Shahed drones. In occupied Crimea, the regional governor said six Ukrainian drones were shot down. In an interview with Die Welt, Vadym Skibitsky, deputy head of Ukraine's military intelligence service, said the government intends to assassinate Putin "because he coordinates and decides what happens" in the war. Yevgeny Prigozhin announced the start of the turnover of Bakhmut from his Wagner mercenaries to the Russian military and his forces' withdrawal from the city. He also said they would repatriate the bodies of an American national, whom he identified as a former special forces soldier named Nicholas Maimer, and a Turkish citizen, which they claimed to have recovered from the remains of a building blown up by Ukrainian forces, adding that the body of another Turkish national, a woman, was also found but could not be retrieved. 106 Ukrainian POWs captured in Bakhmut were repatriated to Ukraine in a prisoner exchange with Russia. The FSB announced that it had arrested two members of a Ukrainian "sabotage group" and two Russian accomplices who were plotting to bomb power lines connected to the Leningrad and Kalinin Nuclear Power Plants, adding that 36.5 kilos of explosives and about 60 detonators were recovered from them. The Russian Defence Ministry said it had scrambled Su-27 and Su-35 fighter jets to intercept two US Air Force B-1B strategic bombers near the country's airspace boundary over the Baltic Sea.

Sources: en.wikipedia.org

Background from the literature

Over 13,000 Plautdietsch-speaking Mennonites live in Belize, farming the land and living according to their religious beliefs. These Mennonite population comprises so-called Russian Mennonites of German descent who settled in the Russian Empire during the 18th and 19th centuries, where they developed into an ethnoreligious group. In the 1870s many of them migrated to Canada, then between 1922 and 1925 to Mexico and in the years after 1958 to Belize. Most Russian Mennonites live in Mennonite settlements like Spanish Lookout, Shipyard, Little Belize, and Blue Creek. The Russian Mennonites speak Plautdietsch, a Low German dialect, in everyday life, but use mostly Standard German for reading (the Bible) and writing. The Plautdietsch-speaking Mennonites came mostly from Mexico and most men are trilingual with proficiency in German, Spanish and English. There are also more than a thousand mainly Pennsylvania Dutch-speaking Old Order Mennonites who came from the United States and Canada in the late 1960s. They live primarily in Upper Barton Creek, Springfield and associated settlements. These Mennonites attracted people from different conservative Anabaptist backgrounds who formed a new community. They look quite similar to Old Order Amish, but are different from them.

=== Red flags === Imaging is not typically needed in the initial diagnosis or treatment of back pain. However, if there are certain "red flag" symptoms present, plain radiographs (X-ray), CT scan or magnetic resonance imaging may be recommended. These red flags include:

=== Techniques === Single-cell genomics is heavily dependent on increasing the copies of DNA found in the cell so that there is enough statistical power for accurate sequencing. This has led to the development of strategies for whole genome amplification (WGA). Currently, WGA strategies can be grouped into three categories:

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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