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Background And Regulatory History — Evidence Review

By Editorial Desk · published 2026-03-02 · last reviewed 2026-03-21 · Guide

The short version of GW501516 fits in a sentence. The long version — which is the one that helps — is below.

This page was last updated on 2026-03-21 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.

Mechanism and Research Context

GW501516 acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in transcription of genes related to lipid handling and energy use. Activation of PPARδ can shift skeletal muscle toward greater fatty acid oxidation in animal models, which is one reason it drew interest for metabolic disease and exercise research. The exact downstream effects depend on tissue, species, dose, and duration. Human data are sparse, so many proposed benefits remain hypotheses rather than established clinical outcomes.

Laboratory studies have examined GW501516 in cell cultures and rodents for conditions such as dyslipidemia, insulin resistance, and obesity. Some trials in humans were initiated, but development was discontinued after preclinical findings raised concerns about cancer in certain models. Those findings do not prove that the compound causes cancer in people, but they contributed to regulatory caution. Later reviews often describe the evidence as preliminary and insufficient for assessing long-term safety.

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.

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.

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Detection, Regulation, and Quality Context

Regulatory treatment of cardarine differs by context and jurisdiction. In competitive sport, the World Anti-Doping Agency lists PPARδ agonists, including GW501516, as prohibited at all times. Outside sport, it lacks approval as a prescription medicine in major drug markets, and products sold for human consumption may be treated as unapproved drugs. Some countries also restrict importation or sale through general consumer protection and medicines laws. These classifications affect availability, testing, and legal risk without establishing therapeutic value.

Because cardarine is not an approved medicine, no pharmacopeial monograph defines its identity, purity, or storage requirements. Laboratories typically rely on in-house methods and reference standards when testing materials labeled as GW501516. Certificates of analysis may report purity and identity for a specific batch, but their scope varies and they do not guarantee safety or legal status. Independent verification can include high-performance liquid chromatography, mass spectrometry, nuclear magnetic resonance, and elemental analysis. The distinction between research chemical labeling and human use is significant because quality standards and oversight differ.

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.

Identity and Pharmacological Mechanism

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.

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.

Supporting material

Official website Tracy Morgan at IMDb Tracy Morgan at Emmys.com Interview with Tracy Morgan National Transportation Safety Board report on Morgan's 2014 accident "Tracy Morgan: Film Actor, Actor, Television Actor, Comedian (1968–)". Biography.com. Archived from the original on April 10, 2019.

== Prevention == Nickel has a wide utility of application in manufactured metals because it is both strong and malleable, leading to ubiquitous presence and the potential for consumers to be in contact with it daily. However, for those who have the rash of allergic contact dermatitis (ACD) due to a nickel allergy, it can be a challenge to avoid. Foods, common kitchen utensils, cell phones, jewelry, and many other items may contain nickel and be a source of irritation due to the allergic reaction caused by the absorption of free released nickel through direct and prolonged contact. The most appropriate measure for nickel-allergic persons is to prevent contact with the allergen. In 2011, researchers showed that applying a thin layer of glycerine emollient containing nanoparticles of either calcium carbonate or calcium phosphate on an isolated piece of pig skin (in vitro) and on the skin of mice (in vivo) prevents the penetration of nickel ions into the skin. The nanoparticles capture nickel ions by cation exchange, and remain on the surface of the skin, allowing them to be removed by simple washing with water. Approximately 11-fold fewer nanoparticles by mass are required to achieve the same efficacy as the chelating agent ethylenediamine tetraacetic acid. Using nanoparticles with diameters smaller than 500 nm in topical creams may be an effective way to limit the exposure to metal ions that can cause skin irritation'.

Her parents divorced when she was 12. Schumer moved to Long Island with her mother and lived in Rockville Centre where she attended South Side High School. She was voted both "Class Clown" and "Teacher's Worst Nightmare" upon graduation in 1999. She attended the Hebrew school of the Central Synagogue of Nassau County, a Reform synagogue in Rockville Centre, where her mother served on the school's board. After graduating from high school, Schumer attended Towson University in Towson, Maryland, where she graduated with a degree in theater in 2003. After graduating from college, she returned to New York City, where she studied at the William Esper Studio for two years and worked as a bartender and a waitress. She also lived with her boyfriend in Santa Barbara, California, where she worked as a pedicab driver. She has a younger sister, Kim Caramele, who is a comedy writer and a producer, and a half-brother, Jason Stein, who is a musician in Chicago, Illinois.

Sources: en.wikipedia.org

Notes from published material

The first clinical study of vosilasarm, a small (n=22) phase 1 study in women with metastatic breast cancer, was started in 2017 and completed in 2020, with results published in 2019, 2020, and 2022. As of March 2023, vosilasarm is in phase 1/2 clinical trials for the treatment of breast cancer. Aside from its development as a potential pharmaceutical drug, vosilasarm is on the World Anti-Doping Agency list of prohibited substances and is sold for physique- and performance-enhancing purposes by black-market Internet suppliers. Vosilasarm is often used in these contexts at doses that have not been evaluated in clinical trials, with unknown effectiveness and safety. Many products sold online that are purported to be a specific SARM either contain none or contain other unrelated substances. Social media has played an important role in facilitating the widespread non-medical use of SARMs.

On 1 December 1978, the Health and Safety Executive announced their intention to prosecute the university for breach of safety legislation. The case was heard in October 1979 at Birmingham Magistrates' Court. Although the source of infection was traced, the mode and cause of transmission was not. Evidence presented by several internationally recognised experts, including Kevin McCarthy, Allan Watt Downie and Keith R. Dumbell, showed that airborne transmission from the laboratory to the telephone room where Parker was supposedly infected was highly improbable. The experts calculated that it would require 53,700 litres (11,812 imp gal) of virus fluid to have been aspirated (meaning, in this context, removed by suction of fluid and cells through a needle) and it would take 20,000 years for one particle to travel to the telephone room at the rate the fluid was aspirated. It was additionally found that although the Shooter Inquiry noted the poor state of the duct sealing in the laboratory, this was caused after the outbreak by engineers fumigating the laboratory and ducts. The university was found not guilty of causing Parker's death.

=== Chemical properties === Like the lanthanides, all actinides are highly reactive with halogens and chalcogens; however, the actinides react more easily. Actinides, especially those with a small number of 5f-electrons, are prone to hybridization. This is explained by the similarity of the electron energies at the 5f, 7s and 6d shells. Most actinides exhibit a larger variety of valence states, and the most stable are +6 for uranium, +5 for protactinium and neptunium, +4 for thorium and plutonium and +3 for actinium and other actinides. Actinium is chemically similar to lanthanum, which is explained by their similar ionic radii and electronic structures. Like lanthanum, actinium almost always has an oxidation state of +3 in compounds, but it is less reactive and has more pronounced basic properties. Among other trivalent actinides Ac3+ is least acidic, i.e. has the weakest tendency to hydrolyze in aqueous solutions. Thorium is rather active chemically. Owing to lack of electrons on 6d and 5f orbitals, tetravalent thorium compounds are colorless. At pH < 3, solutions of thorium salts are dominated by the cations [Th(H2O)8]4+. The Th4+ ion is relatively large, and depending on the coordination number can have a radius between 0.95 and 1.14 Å. As a result, thorium salts have a weak tendency to hydrolyse. The distinctive ability of thorium salts is their high solubility both in water and polar organic solvents. Protactinium exhibits two valence states; the +5 is stable, and the +4 state easily oxidizes to protactinium(V).

Sources: en.wikipedia.org

Further detail

In Euclidean geometry, a tangential quadrilateral (sometimes just tangent quadrilateral) or circumscribed quadrilateral is a convex quadrilateral whose sides all can be tangent to a single circle within the quadrilateral. This circle is called the incircle of the quadrilateral or its inscribed circle, its center is the incenter and its radius is called the inradius. Since these quadrilaterals can be drawn surrounding or circumscribing their incircles, they have also been called circumscribable quadrilaterals, circumscribing quadrilaterals, and circumscriptible quadrilaterals. Tangential quadrilaterals are a special case of tangential polygons. Other less frequently used names for this class of quadrilaterals are inscriptable quadrilateral, inscriptible quadrilateral, inscribable quadrilateral, circumcyclic quadrilateral, and co-cyclic quadrilateral. Due to the risk of confusion with a quadrilateral that has a circumcircle, which is called a cyclic quadrilateral or inscribed quadrilateral, it is preferable not to use any of the last five names. All triangles can have an incircle, but not all quadrilaterals do. An example of a quadrilateral that cannot be tangential is a non-square rectangle. The section characterizations below states what necessary and sufficient conditions a quadrilateral must satisfy to be able to have an incircle.

== Personal life == Kahn is married to Susan Becker Kahn, also formerly of Louisville. They have two children. Stacy Anne Kahn is a pediatric gastroenterologist at the Boston Children's Hospital. Jeffrey Adam Kahn is managing partner of Continuum Search based in Denver, Colorado. His brother Arnold Kahn was emeritus professor of developmental biology of the University of California San Francisco.

The observation of such magnetic resonance frequencies of the nuclei present in a molecule makes it possible to determine essential chemical and structural information about the molecule. The improvements of the NMR method benefited from the development of electromagnetic technology and advanced electronics and their introduction into civilian use. Originally as a research tool it was limited primarily to dynamic nuclear polarization, by the work of Anatole Abragam and Albert Overhauser, and to condensed matter physics, where it produced one of the first demonstrations of the validity of the BCS theory of superconductivity by the observation by Charles Slichter of the Hebel-Slichter effect. It soon showed its potential in organic chemistry, where NMR has become indispensable, and by the 1990s improvement in the sensitivity and resolution of NMR spectroscopy resulted in its broad use in analytical chemistry, biochemistry and materials science. In the 2020s zero- to ultralow-field nuclear magnetic resonance (ZULF NMR), a form of spectroscopy that provides abundant analytical results without the need for large magnetic fields, was developed. It is combined with a special technique that makes it possible to hyperpolarize atomic nuclei.

==== Fibrates ==== Fibrates, known as derivatives of fibric acids, are peroxisome proliferator-activated receptor alpha (PPAR-α) agonists primarily used for lowering TG levels and management of atherogenic dyslipidemia. Typical drugs of the class include fenofibrate, bezafibrate, ciprofibrate and gemfibrozil. Through activation of PPAR-α receptors, fibrates decreases circulating TG via upregulation of lipoprotein lipase (LPL) expression and downregulation of apolipoprotein C-III (ApoC-III) gene expression. LPL is a hepatic enzyme involved in lipolysis, whereas ApoC-III is an inhibitor of LPL. Comparable to statins and ezetimibe, fibrates are usually well-tolerated with mild adverse reactions, with the exception of gemfibrozil. Some of the more prevalent side effects are minor gastrointestinal disturbances such as abdominal pain and cholithiasis on account of the increased excretion of biliary cholesterol. Among atypical adverse effects, myositis can occur in patients under gemfibrozil therapy, especially in those with renal insufficiency or under co-treatment with statins. In contrast, the risk of myopathy is much lower if fenofibrate is used in replacement of gemfibrozil owing to its different pharmacokinetic pathway. Other rare effects are increased serum transaminase levels, agranulocytosis and anaemia. As fenofibrate possess the same binding mechanism as warfarin in the blood, this combination should be addressed with caution as fenofibrate may potentiate the anticoagulant effect of warfarin.

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.

How does cardarine work in the body?

It binds and activates PPARδ, a nuclear receptor that influences gene expression related to fatty acid metabolism and energy balance. This mechanism has been studied mainly in animals and cell models, not established as a safe human therapy.

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