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Identity And Regulatory Status — Explained

By Editorial Desk · published 2026-02-11 · last reviewed 2026-03-16 · Data

If you have been reading about clinical development 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 2026-03-16. Numbers and descriptions here follow the published literature rather than marketing material.

Identity and Regulatory Status

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.

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.

Regulatory Status and Detection Context

Analytical laboratories typically identify cardarine and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is a common matrix in anti-doping testing, while blood and tissue may be used in research settings. Detection windows depend on the assay, the sample matrix, and the compound's metabolism. Because cardarine is extensively metabolized, laboratories often target specific metabolites to improve sensitivity and confirmation. Reference standards are required for reliable quantification. Method validation includes checks for selectivity, linearity, and carryover.

A persistent misconception is that cardarine is a fat-burning drug or a safe alternative to anabolic steroids. No approved therapeutic product exists, and human safety data are limited. The tumor findings in rodents remain a central concern in scientific reviews. Products sold online may contain inaccurate labels, impurities, or different compounds entirely, which complicates any assessment of effects. Independent testing of such products has reported frequent mislabeling. For these reasons, discussions in the literature emphasize risks and unknowns rather than benefits.

Cardarine is not approved for human therapeutic use in any major jurisdiction. It appears on the World Anti-Doping Agency Prohibited List as a PPARδ agonist within the hormone and metabolic modulators category. Sports organizations test for it because it has been detected in athlete samples and seized products. Regulatory actions against marketed research chemical versions have occurred in several countries, though enforcement varies. Availability through unregulated channels complicates oversight.

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

Detection, Regulation, and Quality Context

Cardarine can be detected in biological samples and product materials using liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS). The method separates compounds by chromatography and identifies them by mass-to-charge transitions, allowing low-level detection in urine or blood. Sample preparation often involves enzymatic hydrolysis, solid-phase extraction, or protein precipitation. Certified reference materials and isotope-labeled internal standards improve quantification. Detection windows depend on metabolism, matrix, and assay sensitivity, so no single universal window applies.

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.

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Detection, Stability, and Quality

Stability of GW501516 depends on form, temperature, light exposure, and moisture. Solid reference material is typically stored frozen or refrigerated in a desiccator and protected from light. Solutions in organic solvents such as dimethyl sulfoxide are often kept frozen in aliquots to reduce freeze-thaw cycling. Aqueous solubility is low, so aqueous stock solutions can be difficult to prepare without cosolvents. Degradation may appear as changes in chromatographic purity or mass spectral signal. Stability studies are needed to establish shelf life for any specific preparation.

Quality assessment for cardarine samples usually combines identity, purity, and impurity testing. Nuclear magnetic resonance spectroscopy and mass spectrometry can confirm molecular structure, while high-performance liquid chromatography estimates purity. Certificates of analysis from testing laboratories may list these results, but they do not establish safety or legality. In the absence of approved manufacturing, products sold online may contain the wrong compound, variable amounts, or unlisted contaminants. Independent verification is therefore central to analytical work and to interpreting any reported biological activity.

Laboratory detection of GW501516 commonly uses liquid chromatography coupled with tandem mass spectrometry. The method can identify the parent compound or its metabolites in urine and blood after sample cleanup. Protein precipitation, solid-phase extraction, or enzymatic hydrolysis may precede analysis, depending on the matrix. Reference standards are required for accurate quantification and confirmation. Because the compound is not approved, testing often occurs in anti-doping, forensic, or research settings rather than routine clinical care. Results are reported with limits of detection and quantification.

Preclinical Findings and Safety Signals

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.

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.

Further detail

=== Mast cell activation disorders === Mast cell activation disorders (MCAD) are a spectrum of immune disorders that are unrelated to pathogenic infection and involve similar symptoms that arise from secreted mast cell intermediates, but differ slightly in their pathophysiology, treatment approach, and distinguishing symptoms. The classification of mast cell disorders is complex and has been repeatedly modified. The World Health Organization (WHO) classification of 2016 was updated in the WHO 5th Edition Classification of Haematolymphoid Tumours of 2022 and the International Consensus Classification (ICC) schema of 2022, which differ somewhat in their classification of subcategories of systemic mastocytosis. The incidence and prevalence of MCAD's subcategories of mastocytosis and MCAS have not yet been established through epidemiological studies.

Contrary to common belief, lactic acid accumulation does not actually cause the burning sensation we feel when we exhaust our oxygen and oxidative metabolism, but in actuality, lactic acid in presence of oxygen recycles to produce pyruvate in the liver which is known as the Cori cycle. Substrates produce metabolic fatigue by being depleted during exercise, resulting in a lack of intracellular energy sources to fuel contractions. In essence, the muscle stops contracting because it lacks the energy to do so.

=== Thailand === In the Kingdom of Thailand, members of parliament (Thai: สมาชิกรัฐสภา; RTGS: Samachik Ratthasapha) refer to the members of the National Assembly of Thailand, that is, the members of the House of Representatives and the senators. Following the military coup d'état on 19 September 2006, all members of the assembly were suspended from duty until the next election. The assembly was fully reconvened after the general elections under a slightly amended new constitution. Under the 2007 constitution there are 650 members of parliament, consisting of 500 members in the House of Representatives, of which 375 elected from constituencies and the other 125 by party-list, and 150 senators.

The lichen's survival is closely linked to its dependence on atmospheric humidity. Lacking specialized water-absorbing structures such as roots or stomata, X. parietina absorbs ambient moisture for metabolic activity. When humidity drops, the lichen enters a dormant state, suspending photosynthesis until moisture returns. This poikilohydric strategy enables it to withstand prolonged dry periods, although growth and reproduction are largely confined to humid conditions. In wetter climates, continuous hydration supports ongoing metabolism and faster thallus expansion. Environmental factors—air temperature, wind, and evaporative demand—influence its physiology: higher temperatures accelerate water loss, and strong, dry winds intensify desiccation, particularly in low-altitude coastal regions; conversely, moderate winds with adequate humidity can enhance gaseous exchange and temporarily boost photosynthetic efficiency. This balance between moisture availability and air movement is a key determinant of lichen growth rates across different habitats. The thallus of X. parietina progresses through distinct ontogenetic stages that reflect its ecological adaptations. In the juvenile and immature phases, the lichen establishes its foliose form and develops a homeomeric structure with a protective upper crust. As it advances to virginal stages, the characteristic rosette shape forms.

Sources: en.wikipedia.org

Supporting material

Turin is split up into 8 boroughs, locally called circoscrizioni; these do not necessarily correspond to the historical districts of the city, which are rather called quartieri, rioni, borghi, borgate or zone. The circoscrizioni system originally comprised 10 of them, that were reduced to 8 by merging borough 9 into 8, and 10 into 2. The following list enumerates the boroughs and the location of the historical districts inside them:

=== 2 December === Ukrainian Presidential Advisor Mykhailo Podolyak claimed that 10–13,000 Ukrainian soldiers have been killed since 24 February, the figure last given in August was 9,000. The Ukrainians struck a Russian concentration near Starobilsk, in the rear area of Luhansk Oblast, reportedly killing 14 Russian personnel and wounding 30.

Research into automated cell counting began in the early 20th century. A method developed in 1928 used the amount of light transmitted through a diluted blood sample, as measured by photometry, to estimate the red blood cell count, but this proved inaccurate for samples with abnormal red blood cells. Other unsuccessful attempts, in the 1930s and 1940s, involved photoelectric detectors attached to microscopes, which would count cells as they were scanned. In the late 1940s, Wallace H. Coulter, motivated by a need for better red blood cell counting methods following the bombing of Hiroshima and Nagasaki, attempted to improve on photoelectric cell counting techniques. His research was aided by his brother, Joseph R. Coulter, in a basement laboratory in Chicago. Their results using photoelectric methods were disappointing, and in 1948, after reading a paper relating the conductivity of blood to its red blood cell concentration, Wallace devised the Coulter principle—the theory that a cell suspended in a conductive medium generates a drop in current proportional to its size as it passes through an aperture. That October, Wallace built a counter to demonstrate the principle. Owing to financial constraints, the aperture was made by burning a hole through a piece of cellophane from a cigarette package. Wallace filed a patent for the technique in 1949, and in 1951 applied to the Office of Naval Research to fund the development of the Coulter counter.

Sources: en.wikipedia.org

Supporting material

== History == Originally discovered and developed by Eli Lilly, oritavancin was acquired by Intermune in 2001, and then by Targanta Therapeutics in 2005. In 2009, The Medicines Company acquired the development rights, completed clinical trials and submitted a new drug application to the FDA in February 2014. In August 2014, the US Food and Drug Administration approved oritavancin to treat skin infections. A marketing authorization valid throughout the European Union was granted in March 2015, for the treatment of acute bacterial skin and skin structure infections in adults.

limb muscle atrophy nonreactive degeneration of anterior horn cells degeneration and partial loss of pyramidal neurons of the motor cortex behavioral dysfunction conduction deficits in the central motor pathway neuropathological changes of motor cortex Betz cells There are reports that low BMAA concentrations can selectively kill cultured motor neurons from mouse spinal cords and produce reactive oxygen species. Scientists have also found that newborn rats treated with BMAA show a progressive neurodegeneration in the hippocampus, including intracellular fibrillar inclusions, and impaired learning and memory as adults. BMAA has been reported to be excreted into rodent breast milk, and subsequently transferred to the suckling offspring, suggesting mothers' and cows' milk might be other possible exposure routes.

On 4 September, a Decree-Law on the Safety of the State was issued, practically outlawing the IMRO and assigning the investigation of its activities to the military courts, the police and the army. Mass arrests of IMRO activists and confiscations of weapons and property began. Over the next two years, the Sofia Military Field Court dealt with dozens of cases of murders, kidnappings and racketeering committed by IMRO activists in southwestern Bulgaria. Numerous heavy sentences were handed down, including 21 death sentences against the organization's leader, Ivan Mihailov. The government made changes in foreign policy, in which it advocated continuity with the previous cabinets, strengthening good relations with neighbouring countries, which had concluded the Balkan Pact at the beginning of the year. The goal of the new government was to completely "renovate" the Bulgarian parliamentary system and change the country's foreign policy. It released the following declaration on foreign policy: "Reestablishment of our relations with Soviet Russia; peace and good relations with all the Great Powers and especially with our neighbors." The government's readiness to disband the Internal Macedonian Revolutionary Organization (IMRO) was demonstrated by its proclamation of the "reéstablishment of the public authority over the entire extent of the territory." In fact, it moved right away to restructure the local administration into seven departments, each headed by a governor with extensive powers.

== Mechanism of catalysis == The molecular mechanism of O-linked N-acetylglucosamine transferase has not been extensively studied either, since there is not a confirmed crystal structure of the enzyme. A proposed mechanism by Lazarus et al. is supported by product inhibition patterns of UDP at saturating peptide conditions. This mechanism proceeds with starting materials Uridine diphosphate N-acetylglucosamine, and a peptide chain with a reactive serine or threonine hydroxyl group. The proposed reaction is an ordered sequential bi-bi mechanism.

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 approved for any medical use?

No. Cardarine has not received approval for human therapeutic use in major jurisdictions. It remains an investigational compound.

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