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Background And Regulatory History — Complete Guide

By Editorial Desk · published 2025-08-12 · last reviewed 2025-09-02 · Guide

If you have been reading about GW501516 and want a single page that covers the useful parts, this is it: definitions, context, how it is studied, and the questions that come up repeatedly.

Updated 2025-09-02. Numbers and descriptions here follow the published literature rather than marketing material.

Background and Regulatory History

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.

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 Regulatory Status

Sporting authorities added GW501516 to prohibited lists after it appeared in athlete samples and online markets. The World Anti-Doping Agency classifies it as a hormone and metabolic modulator, and its use can lead to an anti-doping rule violation. Some early laboratory work suggested effects on fatty acid oxidation and endurance-related metabolism in animals, but those findings do not establish safe or effective use in people. Reports of adverse events in humans are scarce and often anecdotal, which complicates risk assessment.

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.

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.

Notes from published material

== Amino-acid sequences == Analysis of the suite of known cyclotides reveals many sequence similarities that are important for understanding their unique physico-chemical properties, bioactivities and homology. The cyclotides fall into two main structural subfamilies. Moebius cyclotides, the less common of the two, contain a cis-proline in loop 5 that induces a local 180° backbone twist (hence likening it to a Möbius strip), whereas bracelet cyclotides do not. There is smaller variation in sequences within these subfamilies than between them. A third subfamily of cyclotides are trypsin inhibitors and are more homologous to a family of non-cyclic trypsin inhibitors from squash plants known as knottins or inhibitor cystine knots than they are to the other cyclotides. It is convenient to discuss sequences in terms of the backbone segments, or loops, between successive cysteine residues. The six cysteine residues are absolutely conserved throughout the cyclotide suite and presumably contribute to preserving the CCK motif. Although the cysteines appear essential to maintaining the overall fold, several other residues highly conserved in cyclotides are thought to provide additional stability. Throughout the known cyclotides loop 1 is the most conserved. Apart from the six cysteine residues, the glutamic acid and serine/threonine residues of loop 1 are the only residues to have 100% identity across the bracelet and Möbius subfamilies. Furthermore, the remaining residue of this loop exhibits only a conservative change i.e. glycine/alanine.

=== Cardiovascular disease === There is no evidence that vitamin C supplementation decreases the risk of cardiovascular disease, although there may be an association between higher circulating vitamin C levels or dietary vitamin C and a lower risk of stroke. There is a positive effect of vitamin C on endothelial dysfunction when taken at doses greater than 500 mg per day. (The endothelium is a layer of cells that line the interior surface of blood vessels.)

Desmetramadol (INNTooltip International Nonproprietary Name), also known as O-desmethyltramadol (O-DSMT), is an opioid analgesic and the main active metabolite of tramadol. Tramadol is demethylated by the liver enzyme CYP2D6 to desmetramadol in the same way as codeine, and so similarly to the variation in effects seen with codeine, individuals who have a less active form of CYP2D6 will tend to have reduced analgesic effects from tramadol. Because desmetramadol itself does not need to be metabolized to induce an analgesic effect, it can be used in individuals with CYP2D6 inactivating mutations. Desmetramadol is commonly encountered as a designer drug online in powder form or as an ingredient in pressed pills due to being unscheduled in many jurisdictions. Outside of its role as a metabolite, a chemical used in research, and as a recreational drug, desmetramadol has a very limited history of human usage and is not approved for medicinal use in any country as of 2025.

Genetic variation in BCG strains Genetic variation in the BCG strains may explain the variable efficacy reported in different trials. Genetic variation in populations Differences in the genetic makeup of different populations may explain the difference in efficacy. The Birmingham BCG trial was published in 1988. The trial, based in Birmingham, United Kingdom, examined children born to families who originated from the Indian subcontinent (where vaccine efficacy had previously been shown to be zero). The trial showed a 64% protective effect, similar to the figure from other UK trials, thus arguing against the genetic variation hypothesis. Interference by nontuberculous mycobacteria Exposure to environmental mycobacteria (especially Mycobacterium avium, Mycobacterium marinum and Mycobacterium intracellulare) results in a nonspecific immune response against mycobacteria. Administering BCG to someone with a nonspecific immune response against mycobacteria does not augment the response. BCG will, therefore, appear not to be efficacious because that person already has a level of immunity and BCG is not adding to that immunity. This effect is called masking because the effect of BCG is masked by environmental mycobacteria. Clinical evidence for this effect was found in a series of studies performed in parallel in adolescent school children in the UK and Malawi.

Sources: en.wikipedia.org

Related pages on this site

Further detail

==== Yellow ==== Yellowing of feces can be caused by an infection known as giardiasis, which derives its name from Giardia, an anaerobic flagellated protozoan parasite that can cause severe and communicable yellow diarrhea. Another cause of yellowing is a condition known as Gilbert's Syndrome. Yellow stool can also indicate that food is passing through the digestive tract relatively quickly. Yellow stool can be found in people with gastroesophageal reflux disease (GERD).

For example, if the first residue is a phenylalanine then the enzyme chymotrypsin will cleave at site 1, and if the third residue of the tripeptide is a lysine then trypsin would cleave at the third cleavage site.

== Clinical significance == Mice that have the lumican gene knocked out (Lum-/-) develop opacities of the cornea in both eyes and fragile skin. The lumican (LUM) gene was thought to be a candidate susceptibility gene for high myopia; however, a meta-analysis showed no association between LUM polymorphism and high myopia susceptibility in all genetic models studied. Lum knockout mice also have abnormal collagen in their heart tissue, with fewer and thicker fibrils. Mice deficient in both lumican and fibromodulin develop severe tendinopathy (tendon pathology), revealing the importance of these SLRPs in the development of correctly sized and aligned collagen fibers in tendon. Along with other extracellular matrix components, lumican expression was increased in equine flexor tendons six weeks after an injury. Lumican is present in the extracellular matrix of uteral tissues in fertile women. There is an increase of lumican during the proliferative to secretory phase of the endometrium. In menopausal endometrial tissue, the level of lumican expression decreases and is also low in pathological compared to normal endometrium. Lumican is highly expressed in pleural effusions (lung fluid) of patients with adenocarcinoma. Its expression was low in cancer cells but high in the extracellular matrix surrounding the tumor. Lumican expression was not associated with tumor grade or stage.

Animals have several characteristics that they share with other living things. Animals are eukaryotic, multicellular, and aerobic, as are plants and fungi. Unlike plants and algae, which produce their own food, animals cannot produce their own food, a feature they share with fungi. Animals ingest organic material and digest it internally.

{\displaystyle {\begin{cases}{\ce {^{235}_{92}U + ^{11}_{5}B -> ^{242}_{97}Bk + 4^{1}_{0}n}}&{\ce {^{232}_{90}Th + ^{14}_{7}N -> ^{242}_{97}Bk + 4^{1}_{0}n}}\\{\ce {^{238}_{92}U + ^{10}_{5}B -> ^{242}_{97}Bk + 6^{1}_{0}n}}&{\ce {^{232}_{90}Th + ^{15}_{7}N -> ^{242}_{97}Bk + 5^{1}_{0}n}}\end{cases}}}

Sources: en.wikipedia.org

Supporting material

Interferon beta-1a (also interferon beta 1-alpha) is a cytokine in the interferon family used to treat multiple sclerosis (MS). It is produced by mammalian cells, while interferon beta-1b is produced in modified E. coli. Some research indicates that interferon injections may result in an 18–38% reduction in the rate of MS relapses. Interferon beta has not been shown to slow the advance of disability. Interferons are not a cure for MS (there is no known cure); the claim is that interferons may slow the progress of the disease if started early and continued for the duration of the disease.

=== Membership pharmacy === The Membership Pharmacy Model is an emerging practice area that structurally departs from traditional volume-based pharmacy by shifting the primary revenue source from drug sales to recurring patient membership fees. This model centers its practice on providing medications at or near their Actual Acquisition Cost (AAC) and prioritizing medication adherence and value-based patient outcomes over dispensing volume. The resulting financial incentives align the pharmacy's success with patient benefit, encouraging the efficient use of medications rather than maximizing the number of prescriptions filled. The core function of a membership pharmacy model involves two primary operational shifts. First, the pharmacy treats prescription fulfillment as an expense, incentivizing efficiency. Second, it shifts its inventory model from "Just-in-Case" (JIC) to a highly efficient "Just-in-Time" (JIT) approach. This is achieved by systematically coordinating all member refills to a single, periodic dispensing date. This efficiency enables the pharmacy to reduce operational costs, key to the model of treating prescription fulfillment, as an expense, rather than a profit center.

The violin pattern is not a definitive identifier, as other spiders can have similar markings (e.g. cellar spiders and pirate spiders). Instead, while most spiders have eight eyes, recluse spiders have six eyes arranged in pairs (dyads) with one median pair and two lateral pairs. Only a few other spiders have three pairs of eyes arranged in this way (e.g., scytodids). Recluses have no obvious coloration patterns on the abdomen or legs, and the legs lack spines. The violin marking can vary in intensity depending on the age of the brown recluse spider, with mature spiders typically having dark violin shapes.

The underlying principle of COLD-PCR is that single nucleotide mismatches will slightly alter the melting temperature (Tm) of the double-stranded DNA. Depending on the sequence context and position of the mismatch, Tm changes of 0.2–1.5 °C (0.36–2.7 °F) are common for sequences up to 200bp or higher. Knowing this the authors of the protocol took advantage of two observations:

Bio Products Laboratory Limited (BPL) is a company involved in the manufacture of human blood plasma products, located in Elstree, Hertfordshire, England. It is run as a commercial business and supplies plasma derived products to the National Health Service in the UK as well as to markets in over 45 countries. BPL was a state owned organization and it was part of the U.K. National Health Service for most of its existence. On 1 September 2022, Permira and the Marcucci family acquired BPL and announced that their operations will be merged with another company acquired by the duo, Kedrion.

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.

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.

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