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Background And Regulatory History — Evidence Review

By Editorial Desk · published 2026-05-06 · last reviewed 2026-05-23 · Blog

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

This page was last updated on 2026-05-23 and is reviewed periodically as new material appears.

Background and Regulatory History

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.

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.

Cardarine as Investigational PPARδ Agonist

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.

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.

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.

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.

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Identity and Pharmacological Classification

Published studies have examined GW501516 in animal models of obesity, insulin resistance, and exercise endurance. Early human trials reportedly ended, and development was discontinued after preclinical findings raised concerns about cancer in some rodent studies. Regulatory agencies have not approved cardarine for any medical use. Its availability through non-pharmaceutical channels raises questions about identity, purity, and legal status that are separate from its laboratory pharmacology. Those questions are often addressed through analytical testing rather than assumptions about product labels.

Cardarine is a common name for GW501516, also GW-1516, a synthetic compound developed as a peroxisome proliferator-activated receptor delta (PPARδ) agonist. It belongs to a class of agents that modulate gene transcription related to lipid and energy metabolism. The compound was studied in preclinical and early clinical research for metabolic and cardiovascular conditions, but it did not progress to approved therapeutic use. Its name appears in fitness and sports contexts despite not being approved as a drug.

Regulation and Analytical Detection

Products sold as cardarine have been found to contain incorrect compounds, variable amounts, or no active ingredient at all. Independent testing is required to verify identity and purity. Common analytical approaches include high-performance liquid chromatography, mass spectrometry, and nuclear magnetic resonance for structural confirmation. These methods can distinguish GW501516 from related PPAR agonists and from unrelated steroids. For regulators and researchers, such verification is central to interpreting both biological results and adverse event reports.

Cardarine is prohibited in competitive sport under the World Anti-Doping Agency code, where it is classified as a metabolic modulator. It is not approved as a prescription medicine in the United States, European Union, or other major markets. Regulatory action has focused on its presence in sports and in products marketed as research chemicals. Because it has no accepted medical indication, supply is often unregulated. This status creates legal and safety uncertainties for anyone who encounters the substance.

Anti-doping laboratories detect GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be used in some programs. Detection depends on factors such as dose, timing, metabolism, and the sensitivity of the assay. Published methods describe limits of detection in the low nanogram per milliliter range for related compounds. Exact detection windows are not fixed for all situations and remain an area of ongoing study.

Notes from published material

The following is a partial list of the "E" codes for Medical Subject Headings (MeSH), as defined by the United States National Library of Medicine (NLM). This list continues the information at the List of MeSH codes (E04). Codes following these are found in the List of MeSH codes (E06). For other MeSH codes, see List of MeSH codes. The source for this content is the set of 2006 MeSH Trees from the NLM.

In contrast with the previous study on PFK1, this study found that elevating OGT or O-GlcNAc upregulated PFK1, though the two studies are consistent in finding that O-GlcNAc levels are positively associated with flux through the pentose phosphate pathway. This study also found that decreasing O-GlcNAc selectively killed cancer cells via ER stress-induced apoptosis. Human pancreatic ductal adenocarcinoma (PDAC) cell lines have higher O-GlcNAc levels than human pancreatic duct epithelial (HPDE) cells. PDAC cells have some dependency upon O-GlcNAc for survival as OGT knockdown selectively inhibited PDAC cell proliferation (OGT knockdown did not significantly affect HPDE cell proliferation), and inhibition of OGT with 5S-GlcNAc showed the same result. Hyper-O-GlcNAcylation in PDAC cells appeared to be anti-apoptotic, inhibiting cleavage and activation of caspase-3 and caspase-9. Numerous sites on the p65 subunit of NF-κB were found to be modified by O-GlcNAc in a dynamic manner; O-GlcNAc at p65 T305 and S319 in turn positively regulate other modifications associated with NF-κB activation such as p300-mediated K310 acetylation and IKK-mediated S536 phosphorylation. These results suggested that NF-κB is constitutively activated by O-GlcNAc in pancreatic cancer. OGT stabilization of EZH2 in various breast cancer cell lines has been found to inhibit expression of tumor suppressor genes.

For example, a number of males may break off from the main group in order to hunt or forage for food during the day, but at night they may return to join (fusion) the primary group to share food and partake in other activities. Many mammals exhibit this, such as primates (for example orangutans and spider monkeys), elephants, spotted hyenas, lions, and dolphins. Solitary animals defend a territory and avoid social interactions with the members of its species, except during breeding season. This is to avoid resource competition, as two individuals of the same species would occupy the same niche, and to prevent depletion of food. A solitary animal, while foraging, can also be less conspicuous to predators or prey.

About one year after his retirement from The Price Is Right, Barker appeared in a public service announcement promoting the transition to digital television in the United States. The advertisement was produced under the first proposed date of February 16, 2009, for the transition. He later appeared in a commercial for State Farm Insurance's "Magic Jingle" campaign, where he made "a new car!" appear for a woman whose previous car was totaled by a giant concrete cylinder. In another TV advertisement, Barker endorsed David Jolly, a candidate for the Republican Party nomination for the 2014 Florida's 13th congressional district special election. Jolly won the nomination and ultimately won the seat. Barker was honored after his death with an hour-long TV special celebrating his life. It aired on August 31, 2023.

Sources: en.wikipedia.org

Further detail

=== Secondary intention === Secondary intention is implemented when primary intention is not possible because of significant tissue damage or loss, usually due to the wound having been created by major trauma. The wound is allowed to granulate. Surgeon may pack the wound with a gauze or use a drainage system. Granulation results in a broader scar. Healing process can be slow due to presence of drainage from infection. Wound care must be performed daily to encourage wound debris removal to allow for granulation tissue formation. Using antibiotics or antiseptics for the surgical wound healing by secondary intention is controversial. Examples: gingivectomy, gingivoplasty, tooth extraction sockets, poorly reduced fractures, burns, severe lacerations, pressure ulcers. There is insufficient evidence that the choice of dressings or topical agents affects the secondary healing of wounds. There is lack of evidence for the effectiveness of negative pressure wound therapy in wound healing by secondary intention.

=== Vegetarian casings === Some innovative coextrusion processes have been developed in recent years, allowing 100% plant-based vegetarian casings to be created. Some special alginate coextrusion equipment is required to make casings that can be used in halal or kosher food making.

In molecular biology, the collagen triple helix or type-2 helix is the main secondary structure of various types of fibrous collagen, including type I collagen. In 1954, Ramachandran & Kartha (13, 14) advanced a structure for the collagen triple helix on the basis of fiber diffraction data. It consists of a triple helix made of the repetitious amino acid sequence glycine-X-Y, where X and Y are frequently proline or hydroxyproline. Collagen folded into a triple helix is known as tropocollagen. Collagen triple helices are often bundled into fibrils which themselves form larger fibres, as in tendons.

=== Oxidative stress === Oxidative stress results from the lack of balance between the systemic production of reactive oxygen species (ROS) and the biological system's capacity to detoxify them or repair the resulting damage. It is known that reactive oxygen species take part in dermal changes taking place outside the cells in both aging caused by internal factors and those caused by external factors. ROS can be created within many dissimilar sources, which include the mitochondria, endoplasmic reticulum and peroxisomes. In normal conditions the binding of ligands to receptor tyrosine kinases (RTKs) activates them, while the various actions of RTKs on the cells' surface are repressed by receptor protein tyrosine phosphatases.

Connective tissue neoplasms including sarcomas such as hemangiopericytoma and malignant peripheral nerve sheath tumor in nervous tissue. Congenital diseases include Marfan syndrome and Ehlers–Danlos syndrome. Myxomatous degeneration – a pathological weakening of connective tissue. Mixed connective tissue disease – a disease of the autoimmune system, also undifferentiated connective tissue disease. Systemic lupus erythematosus (SLE) – a major autoimmune disease of connective tissue Scurvy, caused by a deficiency of vitamin C which is necessary for the synthesis of collagen. Fibromuscular dysplasia is a disease of the blood vessels that leads to an abnormal growth in the arterial wall.

Sources: en.wikipedia.org

Supporting material

==== Hydrides and halides ==== The hydride InH3 has at best a transitory existence in ethereal solutions at low temperatures. It polymerizes in the absence of bases. Lewis bases stabilize a rich collection of indium hydrides of the formula LInH3 (L = tertiary phosphine and N-Heterocyclic carbenes). Chlorination, bromination, and iodination of In produce colorless InCl3, InBr3, and yellow InI3. The compounds are Lewis acids, somewhat akin to the better known aluminium trihalides. Again like the related aluminium compound, InF3 is polymeric. Indium halides dissolves in water to give aquo complexes such as [In(H2O)6]3+ and [InCl2(H2O)4]+. Similar complexes can be prepared from nitrates and acetates. Overall, the pattern is similar to that for aluminium(III).

=== Fluorinated cyclooctynes === The cyclooctane derivative OCT was the first one developed for Cu-free click chemistry; it had only ring strain to drive the reaction forward, and the kinetics were barely improved over the Staudinger ligation. After OCT and MOFO (monofluorinated cyclooctyne), the difluorinated cyclooctyne (DIFO) was developed. An improved synthetic approach to a monofluorosubstituted cyclooctyne (MFCO) was introduced that could easily be converted to a useful reactive intermediate for bioconjugation applications, although the reactivity was somewhat slower than DIFO. The MFCO demonstrated excellent stability characteristics for long-term storage. The substituted cyclooctyne is activated for a 1,3-dipolar cycloaddition by its ring strain and electron-withdrawing fluorine substituents, which allows the reaction to take place with kinetics comparable to the Cu-catalyzed Huisgen cycloaddition. Ring strain (~18 kcal/mol) arises from the deviation of the bond angles from the ideal 180° to form an eight-membered ring, the smallest of all cycloalkynes. The electron-withdrawing fluorine substituents were chosen due to their synthetic ease and compatibility with living biological systems. Additionally, the group cannot produce cross-reacting Michael acceptors that could act as alkylating agents toward nucleophilic species within cells. Like most cyclooctynes, DIFO prefers the chair conformation in both the ground state and the minimum energy traction path, although boat transition states may also be involved.

== External links == 5-lipoxygenase-activating+protein at the U.S. National Library of Medicine Medical Subject Headings (MeSH) Human ALOX5AP genome location and ALOX5AP gene details page in the UCSC Genome Browser.

Second Battle of Artois — In what was referred to as the Second Action of Givenchy, British and Canadian forces attacked northwest of La Bassée, France and captured the front line, but were pushed back by German grenades and a shortage of ammunition. An official inquiry led by Lord Mersey into the sinking of the RMS Lusitania began at Methodist Central Hall in Westminster, London. French airplanes raided Baden and Karlsruhe, Germany. Armenian genocide — A group of 20 activists with the Social Democrat Hunchakian Party were hanged in the Sultan Beyazıt Square of Constantinople. Among those executed were Armenian leaders Paramaz, Aram Achekbashian, and Kegham Vanigian. Other Armenian leaders who were executed that same day while en route to Severek, Turkey included Harutiun Jangülian, Rupen Zartarian, Sarkis Minassian, Khachatur Malumian, and Nazaret Daghavarian. Japanese Government Railways extended the Echigo Line in the Niigata Prefecture, Japan, with station Arahama serving the line. The Cornish Library opened in Winnipeg. It received damage from flooding in 1918 and was repaired. The sports club Magni Grenivík was established in Grenivík, Iceland. The village of Denmark, Wisconsin was established. Born: Thomas Huckle Weller, American virologist, recipient of the Nobel Prize in Physiology or Medicine for his research into poliomyelitis viruses; in Ann Arbor, Michigan, United States (d. 2008) Died: Konstantin Konstantinovich, 56, Russian noble, grandson of Nicholas I of Russia (b. 1862)

transfer RNA (tRNA) Formerly referred to as soluble RNA (sRNA). A special class of RNA molecule, typically 76 to 90 nucleotides in length, that serves as a physical adapter allowing mRNA transcripts to be translated into sequences of amino acids during protein synthesis. Each tRNA contains a specific anticodon triplet corresponding to an amino acid that is covalently attached to the tRNA's opposite end; as translation proceeds, tRNAs are recruited to the ribosome, where each mRNA codon is paired with a tRNA containing the complementary anticodon. Depending on the organism, cells may employ as many as 41 distinct tRNAs with unique anticodons; because of codon degeneracy within the genetic code, several tRNAs containing different anticodons carry the same amino acid.

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 an investigational synthetic compound that acts as a PPARδ agonist. It is also known as GW501516 and has been studied mainly in preclinical research. It is not an approved medicine.

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