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Background And Regulatory Status — Background and Details

By Editorial Desk · published 2025-12-08 · last reviewed 2025-12-24 · Info

clinical development is one of those subjects where the details matter more than the headlines. This page pulls together the background, the mechanisms, and the practical points readers ask about most.

Updated 2025-12-24. Numbers and descriptions here follow the published literature rather than marketing material.

Background and Regulatory Status

Legal status varies by country. In some places, cardarine is controlled under medicines or psychoactive substances laws; in others, it may be sold with minimal oversight as a research chemical. Customs agencies have intercepted shipments, and several national health agencies have issued warnings about products marketed for bodybuilding or performance enhancement. The lack of a standardized pharmaceutical supply means identity, purity, and contamination levels can differ widely between samples. These factors make cardarine a regulatory and public health concern rather than a conventional prescription drug.

Cardarine is a common name for GW501516, a synthetic compound first described in the 1990s as a selective agonist of the peroxisome proliferator-activated receptor delta. It was studied in preclinical models for metabolic and cardiovascular conditions, but it has not been approved as a medicine in the United States, Europe, or other major jurisdictions. Retail products labeled as cardarine are generally research chemicals or supplements, not pharmaceutical formulations. Because human safety and efficacy data remain limited, regulatory agencies treat it as an unapproved substance rather than a therapeutic product.

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.

Laboratory studies indicate that GW501516 activates PPARδ, a nuclear receptor involved in fatty acid oxidation and energy metabolism. In rodent experiments, treated animals often showed increased endurance and reduced fat mass. These effects were observed under controlled conditions and do not establish safe or effective use in humans. The exact dose-response relationship in humans remains poorly characterized. Species differences in metabolism can affect how results translate across animals and people.

Cardarine at a glance

PropertyValueNotes
IUPAC name{4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acidSystematic name for GW501516
CAS Registry Number317318-70-0Unique identifier for the parent compound
Molecular formulaC21H18F3NO3S2Includes carbon, hydrogen, fluorine, nitrogen, oxygen, and sulfur
Molecular weight453.5 g/molApproximate value for the neutral form
AppearanceWhite to off-white powderTypical description for purified laboratory material

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.

Related pages on this site

Cardarine Identity and Mechanism

At the molecular level, GW501516 binds and activates PPARδ, a nuclear receptor that regulates transcription. Activation shifts expression of genes involved in fatty acid oxidation, energy expenditure, and lipid transport in skeletal muscle and liver. Animal studies report increased endurance and altered lipid profiles after exposure. Human data are limited to small trials and do not establish long-term safety or efficacy. PPARδ also has roles in cell proliferation, so the relationship between activation and cancer risk remains an open question.

Published literature on cardarine includes in vitro assays, rodent experiments, and a small number of human studies. Reports describe effects on exercise capacity and lipid metabolism in animals, while human evidence is sparse. Many online descriptions present the compound as a proven endurance aid, a claim not supported by regulatory approval or large clinical trials. Analytical studies focus on identifying the parent compound and its metabolites in biological samples. Important uncertainties include species differences, dose-response relationships, and the relevance of rodent tumor findings to humans.

Mechanism and Detection

GW501516 acts as a ligand for PPAR delta, a nuclear receptor that regulates transcription of genes involved in fatty acid oxidation and energy use. Activation of this receptor in skeletal muscle shifts metabolism toward fat burning in animal models. The compound does not burn fat directly; it changes gene expression over hours to days. Researchers study it to understand metabolic flexibility and exercise adaptation. Effects observed in rodents are not automatically expected in humans.

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.

Supporting material

ATC code A10 Drugs used in diabetes is a therapeutic subgroup of the Anatomical Therapeutic Chemical Classification System, a system of alphanumeric codes developed by the World Health Organization (WHO) for the classification of drugs and other medical products. Subgroup A10 is part of the anatomical group A Alimentary tract and metabolism. Codes for veterinary use (ATCvet codes) can be created by placing the letter Q in front of the human ATC code: for example, QA10. National versions of the ATC classification may include additional codes not present in this list, which follows the WHO version.

=== Prelude to the conflict === One 2006 cable reported that Ruslan Khasbulatov was responsible for bombing of Sukhumi in 1993 when Eduard Shevardnadze was personally defending the city. The cables suggested that Russia had been at war with Georgia since 2004. According to a leaked diplomatic cable, the US diplomat Kurt Volker in 2006 had rationalized to Russian deputy Foreign Minister Alexander Grushko as to why the secession of Kosovo should be viewed as an isolated case and should not be transferred to other conflicts. Grushko, on the other hand, made clear the position of Putin who saw Kosovo as a model for the independence of South Ossetia and Abkhazia. Georgian president Saakashvili told United States Under Secretary of State R. Nicholas Burns in 2007 that "Putin was personally committed to removing Abkhazia from Georgia." U.S. dispatches had reported as early as 2007 that Grad missiles and other arms were provided to separatists in South Ossetia and Abkhazia. Russia had engaged in a large variety of covert activities aimed at destabilizing Georgia before the 2008 war. The cables reported that the Russian FSB was in control of South Ossetia.

=== Redox-responsive nanogels === Redox-responsive nanogels generally contain crosslinks formed by disulfide bonds or specific crosslinking agents. Nanogels made of bioreducible and bifunctional monomers can also be used. In the presence of reducing agents such as glutathione, thioredoxin and peroxiredoxin, these nanogels respond by releasing their cargo. Given that these reducing agents and several others are found in larger concentrations inside cells compared to their external environment, redox-responsive nanogels are a promising strategy for targeted intracellular delivery.

== Disruption of traditional logistics and supply chain management == The shipping and logistics industry has long been viewed as conservative and slow-to-change, in part due to complex relationships within global shipping and transportation networks, difficult documentation and customs requirements, lack of transparency among involved parties, and obstacles to adapting quickly to sudden economic changes. Recent developments in freight technology are working to modernize and simplify freight transport. According to a report from the U.S. Department of Transportation, intelligent freight technologies have multifaceted benefits in shipping and logistics. These include increased operational flexibility and efficiency due to better planning and schedule adherence, better utilization of people and equipment, reduction of non-productive waiting times, shorter processing times, and increased shipper confidence. Transactional application programming interfaces (API) and distributed ledger technology are expanding in the shipping and logistics sector to reduce extensive paperwork, monitor conditions and location of freight and goods in transport and make this information available to involved parties, and increase transparency across the supply chain.

Sources: en.wikipedia.org

Supporting material

Glutamate synthase facilitates the ammonium assimilation pathway, which follows the enzymes, nitrite reductase and glutamine synthase. An ammonium produced by the nitrite reductase reaction will be incorporated into carbon skeleton backbone by glutamine synthase. Glutamine will be produced because of the introduction of ammonium in the carbon backbone, which can be converted into glutamate by glutamate synthase of another pathway. These processes are common in plant roots because if the nitrogen deficient conditions exist (with access to ammonium and nitrate ions), there will be a first priority of ammonium uptake. The reaction only proceeds in the direction of glutamic acid production: it converts one unit of glutamine and one 2-oxoglutarate into two units of product, using reduced nicotinamide adenine dinucleotide (NADH) as cofactor. This enzyme belongs to the family of oxidoreductases, specifically those acting on the CH-NH2 group of donors with NAD+ or NADP+ as acceptor. This enzyme participates in glutamate metabolism and nitrogen assimilation. It uses the cofactor, flavin mononucleotide.

=== Prehistory and Imperial China === The earliest known human traces in what is now Hong Kong are dated by some to 35,000-39,000 years ago during the Paleolithic period. The claim is based on an archaeological investigation in Wong Tei Tung in the Sai Kung Peninsula in 2003. The archaeological works revealed knapped stone tools from deposits dated by optical luminescence dating. During the Middle Neolithic period, about 6,000 years ago, the region had been widely occupied by humans. Neolithic to Bronze Age Hong Kong settlers were semi-coastal people. Early inhabitants are believed to have been Austronesians in the Middle Neolithic period, and later the Yue people. As hinted by the archaeological works in Sha Ha, Sai Kung, rice cultivation had been introduced since the Late Neolithic period. Bronze Age Hong Kong featured coarse pottery, hard pottery, quartz and stone jewelry, as well as small bronze implements.

Chavibetol is an organic chemical compound of the phenylpropanoid class. It is one of the primary constituents of the essential oil from the leaves of the betel plant (Piper betel) and catatia. It is an aromatic compound with a spicy odor.

=== Isometric activity === In 1993, isometric exercise training was applied for four weeks resulting in isometric peak power at 60% of maximal voluntary contraction. The increase in isometric power was later shown to have no significant effect on serum creatine kinase (CK) after two weeks of strength training.

==== 500–599 ==== Water Supply and Sewerage Services (Customer Service Standards) (Amendment) Regulations 1993 (S.I. 1993/500) Local Government Finance Act 1992 (Community Charge Benefits) Saving Order 1993 (S.I. 1993/502) Bovine Animals (Identification, Marking and Breeding Records) (Amendment) Order 1993 (S.I. 1993/503) Prisoner Escorts Rules 1993 (S.I. 1993/515) Prison (Amendment) Rules 1993 (S.I. 1993/516) Common Agricultural Policy (Wine) Regulations 1993 (S.I. 1993/517) Social Security Benefits (Miscellaneous Amendments) Regulations 1993 (S.I. 1993/518) Occupational and Personal Pension Schemes (Miscellaneous Amendments) Regulations 1993 (S.I. 1993/519) Local Authorities (Capital Finance) (Amendment) Regulations 1993 (S.I. 1993/520) National Health Service (General Medical and Pharmaceutical Services) (Scotland) Amendment Regulations 1993 (S.I. 1993/521) National Health Service (Charges for Drugs and Appliances) (Scotland) Amendment Regulations 1993 (S.I. 1993/522) National Health Service (Dental Services) (Miscellaneous Amendments) (Scotland) Regulations 1993 (S.I. 1993/523) National Health Service (Optical Charges and Payments) (Scotland) Amendment Regulations 1993 (S.I. 1993/524) Education (Fees and Awards) (Scotland) Amendment Regulations 1993 (S.I. 1993/525) Council Tax (Dwellings) (Scotland) Regulations 1993 (S.I. 1993/526) Council Tax (Transitional Reduction Scheme) (Scotland) Amendment (No.2) Regulations 1993 (S.I. 1993/527) Legal Aid in Contempt of Court Proceedings (Scotland) Amendment Regulations 1993 (S.I.

Sources: en.wikipedia.org

Notes from published material

== Risk factors == Hospitals are primary transmission sites for CRE-based infections. Up to 75% of hospital admissions attributed to CRE were from long-term care facilities or transferred from another hospital. Suboptimal maintenance practices are the largest cause of CRE transmission. This includes the failure to adequately clean and disinfect medication cabinets, other surfaces in patient rooms, and portable medical equipment, such as X-ray and ultrasound machines that are used for both CRE and non-CRE patients. Thus far, CRE have primarily been nosocomial infectious agents. Almost all CRE infections occur in people receiving significant medical care in hospitals, long-term acute care facilities, or nursing homes. Independent risk factors for CRE infection include use of beta-lactam antibiotics and the use of mechanical ventilation. Patients with diabetes have also been shown to be at an elevated risk for acquiring CRE infections. When compared to other hospitalized patients, those admitted from long-term acute care (LTAC) facilities have significantly higher incidence of colonization and infection rates. Another 2012 multicenter study found that over 30% of patients with recent exposure to LTAC were colonized or infected with CRE. A person susceptible to CRE transmission is more likely to be female, have a greater number of parenteral nutrition-days (days when the person received nutrition via the bloodstream), and to have had a significant number of days breathing through a ventilator.

=== Effect of amino acid sequence on polymerization === In general, amyloid polymerization (aggregation or non-covalent polymerization) is sequence-sensitive, that is mutations in the amino acid sequence can induce or prevent self-assembly. For example, humans produce amylin, an amyloidogenic peptide associated with type II diabetes, but in rats and mice, prolines are substituted in critical locations and amyloidogenesis does not occur. Studies comparing synthetic to recombinant β amyloid peptide in assays measuring rate of fibrillation, fibril homogeneity, and cellular toxicity showed that recombinant β amyloid peptide has a faster fibrillation rate and greater toxicity than synthetic β amyloid peptide. There are multiple classes of amyloid-forming polypeptide sequences. Glutamine-rich polypeptides are important in the amyloidogenesis of Yeast and mammalian prions, as well as trinucleotide repeat disorders including Huntington's disease. When glutamine-rich polypeptides are in a β-sheet conformation, glutamines can brace the structure by forming inter-strand hydrogen bonding between its amide carbonyls and nitrogens of both the backbone and side chains. The onset age for Huntington's disease shows an inverse correlation with the length of the polyglutamine sequence, with analogous findings in a C. elegans model system with engineered polyglutamine peptides.

Gopsill, Frank Peter; Sexton, Brian (2006) [2001]. "Le natura, si – un schema, no". Historia de interlingua (in Interlingua). Archived from the original on 2022-04-12. Retrieved 2025-01-14. Hill-Meyer, Tobi; Scarborough, Dean (2014). "Sexuality". In Erickson-Schroth, Laura (ed.). Trans Bodies, Trans Selves: A Resource for the Transgender Community (1st ed.). Oxford UP. ISBN 978-0-19-932535-1. OCLC 944726648. Houglum, Peggy A.; Bertoli, Dolores B. (2012). Brunnstrom's Clinical Kinesiology. F. A. Davis Company. ISBN 978-0-8036-2352-1. Janeway CA, Travers P, Walport M (2001). "Effector mechanisms in allergic reactions". Immunobiology (5th ed.). Garland Science. Janeway CA (2005). Immunobiology (6th ed.). Garland Science. ISBN 0-443-07310-4. Kendall, Florence Peterson; et al. (2005). Muscles : testing and function with posture and pain (5th ed.). Baltimore, MD: Lippincott Williams & Wilkins. ISBN 0-7817-4780-5. Knight, Sarah; Tilg, Stefan, eds. (2015). The Oxford Handbook of Neo-Latin. New York: Oxford University Press. ISBN 978-0-19-088699-8. OL 28648475M. Krishnaswamy G, Ajitawi O, Chi DS (2006). "The human mast cell: an overview". Mast Cells. Methods in Molecular Biology. Vol. 315. pp. 13–34. doi:10.1385/1-59259-967-2:013. ISBN 1-59259-967-2. PMID 16110146. McArthur, Tom (ed.): The Oxford Companion to the English Language, (Oxford University Press, 1992). ISBN 0-19-214183-X Murphy K, Weaver C (2016). Immunobiology (9 ed.). Garland Science. ISBN 978-0-8153-4505-3.

The lawsuit was brought against VPX and its owner for claims of false advertising under the Lanham Act, California laws regarding unfair competition and false advertising, as well as trade libel. The jury issued the verdict on September 29, 2022. Following a trial lasting over a month, the jury awarded Monster Energy $293 million in damages. Among the damages were $272 million awarded for false advertising, $18 million for Bang's interference with contracts, and $3 million for trade secret theft. In October 2023, a judge awarded an additional $43 million dollars to Monster Energy for attorney fees and expenses.

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine approved for human use?

No. Major drug regulators have not approved GW501516 for treating any medical condition. Products sold as cardarine are typically unapproved research chemicals or supplements, so their contents and safety are not assured.

Why is cardarine banned in sport?

It is prohibited by the World Anti-Doping Agency as a hormone and metabolic modulator. Athletes who test positive for GW501516 can face sanctions, including suspensions and loss of results.

What is the difference between cardarine and GW501516?

Cardarine is a common or trade-style name, while GW501516 is the research code for the same chemical entity. Some sources also use Endurobol or GSK-516. The names refer to the same compound, not distinct drugs.

What did animal studies show?

Rodent studies reported increased endurance and fat oxidation after GW501516 exposure. Long-term studies also found higher rates of some tumors, which led to halted development.

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