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Identity And Regulatory Status — Evidence Review

By Editorial Desk · published 2025-10-22 · last reviewed 2025-11-24 · Guide

GW501516 comes up often in conversation and rarely with the context attached. Here we lay out the basics in order, then work through the practical considerations.

Last reviewed on 2025-11-24. Where a claim depends on a specific study, the study is described rather than over-claimed.

Identity and Regulatory Status

Cardarine is a common name for GW501516, an investigational compound developed in the 1990s for metabolic conditions. It acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in lipid and energy metabolism. The compound is frequently mislabeled as a selective androgen receptor modulator, or SARM, but its molecular target is different. GW501516 reached early clinical testing before development was discontinued. It has no approved therapeutic use in any country. The name cardarine is not a formal international nonproprietary name.

Regulatory treatment varies, but cardarine is not approved as a medicine. Sports authorities list GW501516 as a prohibited substance, and it is banned at all times under the World Anti-Doping Agency code. Many countries restrict sales for human consumption, while online vendors market it as a research chemical. Such products may lack purity data, and their actual contents can differ from the label. Purchasing or possessing cardarine may carry legal consequences depending on jurisdiction. The compound is not a dietary supplement ingredient in regulated markets.

Clinical development stopped after rodent studies showed tumors at multiple sites. Whether those findings predict human cancer risk remains an open question, but they led sponsors to discontinue programs. Human safety data are limited to small, short-term studies that were not designed to assess cancer risk. Reported effects in those studies included changes in blood lipids, but the evidence is insufficient for medical use. Long-term consequences of nonmedical use are not well characterized. Questions about dose, duration, and individual susceptibility remain unresolved.

Detection and Regulatory Landscape

Cardarine is explicitly prohibited by the World Anti-Doping Agency under the class of PPARδ agonists. Its presence in urine or blood samples can be detected using mass spectrometry-based methods, often liquid chromatography-tandem mass spectrometry. Athletes who test positive may face sanctions, including bans from competition. The compound is also regulated as a prescription-only or unapproved drug in many countries. Enforcement varies by jurisdiction, and some regions treat it as a controlled substance. Online sales may occur despite these restrictions, creating quality and legal risks.

Laboratory detection of cardarine typically involves sample preparation followed by chromatographic separation and mass spectrometric identification. Urine is the most common matrix for anti-doping tests, though blood and hair have also been explored. Methods can target the parent compound or its metabolites, depending on the expected window of detection. Reference standards are required for accurate quantification. Matrix effects and dilution can influence results, so laboratories use internal standards and validation protocols. The exact detection window varies with dose, route, and individual metabolism.

A common misconception is that cardarine has been proven safe for human use. In reality, human clinical data are limited, and long-term animal studies have raised concerns about cancer. Another misconception is that it is a supplement or vitamin-like compound. It is a synthetic research chemical with no approved medical indication. Scientific discussion often focuses on its mechanism and detection rather than therapeutic use. Regulatory and anti-doping literature treats it primarily as a prohibited substance.

Cardarine at a glance

PropertyValueNotes
Common synonymsGW501516; GW-1516; endurobolGW501516 is the research code
Drug classPPARδ agonistNot a selective androgen receptor modulator
Molecular formulaC21H18F3NO3S2Established chemical formula
Molar mass453.5 g/molCalculated from the formula
Regulatory statusProhibited in sport; not approved as medicineStatus varies by country

Preclinical Findings and Safety Signals

Safety concerns emerged from long-term animal studies. In rodents given the compound for extended periods, researchers found an increased incidence of certain cancers, including liver and bladder tumors. These findings contributed to the discontinuation of clinical development. Whether similar risks apply to short-term or low-level exposure in humans is not established, and controlled human safety data are limited. The relevance of high-dose rodent carcinogenicity findings to human use remains a subject of debate.

Human trials of GW501516 were small and short in duration. They examined lipid levels, glucose handling, and other metabolic markers, but the programs were halted after the animal cancer findings. No approved therapeutic product exists, and published human data are insufficient for establishing long-term safety. Reports of use for athletic performance come mainly from non-clinical settings and cannot be verified through controlled trials. Independent testing of products sold as cardarine has found inconsistent purity and labeling.

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Identity and Pharmacological Mechanism

Cardarine is a common name for GW501516, a synthetic compound studied for its effects on lipid and glucose metabolism. It functions as an agonist at peroxisome proliferator-activated receptor delta, or PPARδ, a nuclear receptor that influences gene expression. The molecule is not a steroid, nor is it a selective androgen receptor modulator. It is also known in research and sports literature as GW-501516 and endurobol. Early laboratory work examined its metabolic activity in cell cultures and animal models.

Activation of PPARδ changes transcription of genes involved in fatty acid transport, mitochondrial function, and skeletal muscle fuel preference. In rodent studies, pharmacological PPARδ activation was associated with increased endurance and altered body composition. These findings generated interest in performance enhancement, but species differences and study designs limit direct extrapolation to humans. Small human trials were conducted in the 2000s and later discontinued. The extent to which cardarine produces similar metabolic or performance effects in people remains an open question.

The compound is typically described as a laboratory compound rather than a therapeutic product. Published reports have explored its role in lipid disorders, insulin sensitivity, and exercise metabolism, yet no major drug regulator has approved it for medical use. Commercial samples sold under the cardarine name may vary in purity and identity. Analytical confirmation is therefore necessary when the material is discussed in scientific or regulatory contexts. Its classification as a prohibited substance in sport further shapes how it is studied and reported.

Supporting material

=== Neuroadaptation and sensitization === Reward sensitization is a process that causes an increase in the amount of reward (specifically, incentive salience) that is assigned by the brain to a rewarding stimulus (e.g., a drug). In simple terms, when reward sensitization to a specific stimulus (e.g., a drug) occurs, an individual's "wanting" or desire for the stimulus itself and its associated cues increases. Reward sensitization normally occurs following chronically high levels of exposure to the stimulus. On the incentive-sensitization account, "cue-induced wanting" or "cue-triggered wanting" – a form of craving triggered by drug-associated cues – drives much of the compulsive behavior seen in addiction. During the development of an addiction, the repeated association of otherwise neutral and even non-rewarding stimuli with drug consumption triggers an associative learning process that causes these previously neutral stimuli to act as conditioned positive reinforcers of addictive drug use (i.e., these stimuli start to function as drug cues). As conditioned positive reinforcers of drug use, these previously neutral stimuli are assigned incentive salience (which manifests as a craving) – sometimes at pathologically high levels due to reward sensitization – which can transfer to the primary reinforcer (e.g., the use of an addictive drug) with which it was originally paired. Incentive sensitization is one of several competing accounts of addiction.

==== Other factors ==== Oxytocin reaches lactotrophs via portal vessels and fulfils the criteria of a prolactin-releasing factor during suckling. Serotonin mediates the nocturnal prolactin surge and suckling-induced prolactin release via 5-HT1A and 5-HT2 receptors. Other reported stimulatory factors include neurotensin, angiotensin II, and galanin. Prolactin-releasing peptide (PrRP), despite its name, does not appear to function as a classical hypophysiotropic releasing factor in vivo.

=== Nutritional value === Milk powders contain all 21 standard amino acids, the building blocks of proteins, and are high in soluble vitamins and minerals. According to USAID, the typical average amounts of major nutrients in the unreconstituted nonfat dry milk are (by weight) 36% protein, 52% carbohydrates (predominantly lactose), calcium 1.3%, potassium 1.8%. Whole milk powder, on the other hand, contains on average 25–27% protein, 36–38% carbohydrates, 26–40% fat, and 5–7% ash (minerals). In Canada, powdered milk must contain added vitamin D in an amount such that a reasonable daily intake of the milk will provide between 300 and 400 International units (IU) of vitamin D. However, inappropriate storage conditions, such as high relative humidity and high ambient temperature, can significantly degrade the nutritive value of milk powder. Commercial milk powders are reported to contain oxysterols (oxidized cholesterol) in higher amounts than in fresh milk (up to 30 μg/g, versus trace amounts in fresh milk). Oxysterols are derivatives of cholesterol that are produced either by free radicals or by enzymes. Some free radicals-derived oxysterols have been suspected of being initiators of atherosclerotic plaques. For comparison, powdered eggs contain even more oxysterols, up to 200 μg/g.

Sources: en.wikipedia.org

Notes from published material

Endoneurium. Each nerve axon, or fiber is surrounded by the endoneurium, which is also called the endoneurial tube, channel or sheath. This is a thin, delicate, protective layer of connective tissue. Perineurium. Each nerve fascicle containing one or more axons, is enclosed by the perineurium, a connective tissue having a lamellar arrangement in seven or eight concentric layers. This plays a very important role in the protection and support of the nerve fibers and also serves to prevent the passage of large molecules from the epineurium into a fascicle. Epineurium. The epineurium is the outermost layer of dense connective tissue enclosing the (peripheral) nerve.

On February 28, 2022, Pritzker lifted most of Illinois's COVID-19 restrictions, including the statewide mask mandate, which came just a few days after the CDC issued new, more relaxed masking guidance. On July 14, 2022, Pritzker announced the lifting of the COVID-19 vaccine mandate for college students.

World War I St. Mihiel Meuse-Argonne Lorraine 1918 World War II Sicily Naples-Foggia Normandy (with arrowhead) Rhineland (with arrowhead) Ardennes-Alsace Central Europe Armed Forces Expeditions Dominican Republic Grenada Panama Southwest Asia Defense of Saudi Arabia Liberation and Defense of Kuwait

The hospital specialized in the treatment of heart, lung and eye problems. UCC also provided a $2.2 million grant to Arizona State University to establish a vocational-technical centre in Bhopal, which was opened, but was later closed by the state government. They also donated $5 million to the Indian Red Cross after the disaster. They also developed a Responsible Care system with other members of the chemical industry as a response to the Bhopal crisis, which was designed to help prevent such an event in the future.

Sources: en.wikipedia.org

Background from the literature

Scottish economist Adam Smith stated that free labour was economically better than slave labour, and that it was nearly impossible to end slavery in a free, democratic, or republican form of government since many of its legislators or political figures were slave owners and would not punish themselves. He further stated that slaves would be better able to gain their freedom under centralized government, or a central authority like a king or church. Similar arguments appeared later in the works of Auguste Comte, especially given Smith's belief in the separation of powers, or what Comte called the "separation of the spiritual and the temporal" during the Middle Ages and the end of slavery, and Smith's criticism of masters, past and present. As Smith stated in the Lectures on Jurisprudence, "The great power of the clergy thus concurring with that of the king set the slaves at liberty. But it was absolutely necessary both that the authority of the king and of the clergy should be great. Where ever any one of these was wanting, slavery still continues..."

== Honours and awards == Commonwealth Scholar at Trinity College, Cambridge, 1960-1963 Powell Prize for English Verse, Trinity College, 1961 Vidya Jyothi from the President of Sri Lanka, 1992 Honorary DLitt, Sōka University (Japan), 1996 Doctor of Science (honoris causa), University of Ruhuna, Sri Lanka, 2004 Visiting By-Fellowship, visiting scholar, Churchill College, Cambridge, England 2015/16 Ada Derana Sri Lankan of the Year 2017 - Global Scientist Wickramasinghe was appointed Member of the Order of the British Empire (MBE) in the 2022 New Year Honours for services to science, astronomy and astrobiology.

This research provided a new drug that could serve as a new treatment for amebiasis caused by the Entamoeba histolytica. In 2017, auranofin completed phase I clinical trials against Entamoeba histolytica and Giardia The Barrios Lab in the Department of Pharmacy at the University of Utah largely focuses on developing chemical probes to study biological substrates, substrate selectivity, cellular regulation, and druggability for use in therapeutics. Human protein tyrosine phosphatases (PTPs) hold substantial relevance in human autoimmunity and T-cell receptor signaling, as well as cell signaling in diseases. Novel chemical probes to better understand the activity and regulation of this family of enzymes aids in developing human therapeutics. These developments in the Barrios Lab include fluorogenic probes to investigate PTP activity, along with profiling substrate selectivity for the use of developing potent, selective inhibitors. Additionally, the Barrios Lab also focuses on chemical tools used to study the therapeutic roles of metal ions as biological targets of gold-based compounds.

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine a SARM?

No. Cardarine is GW501516, a PPARδ agonist, while SARMs act on androgen receptors. The two classes are often grouped in informal discussions despite different mechanisms.

Is cardarine approved for human use?

No. It has no approved medical indication in any country. Regulatory agencies have not cleared it for treatment or prevention of any condition.

Why was its development discontinued?

Early clinical work stopped after rodent carcinogenicity findings. Those animal results raised concerns about long-term human risk, although direct human evidence is lacking. The human relevance of the tumors remains an open scientific question.

Is cardarine banned in sports?

Yes, WADA prohibits cardarine as a PPARδ agonist. It appears on the prohibited list and can be detected in urine or blood. Athletes using it risk sanctions.

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