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Background And Regulatory History — Field Notes

By Editorial Desk · published 2025-09-21 · last reviewed 2025-10-09 · Info

Everything below concerns Metabolite. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.

Last reviewed on 2025-10-09. Where a claim depends on a specific study, the study is described rather than over-claimed.

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.

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.

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 Analytical Detection

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.

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.

Related pages on this site

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.

Identity and Pharmacological Classification

PPARδ is a nuclear receptor that influences transcription of genes involved in fatty acid oxidation, lipid transport, and energy homeostasis. GW501516 binds and activates this receptor with high selectivity relative to PPARα and PPARγ in laboratory assays. Activation alters expression of target genes in skeletal muscle, liver, and adipose tissue in animal models. The exact clinical consequences of these changes in humans remain incompletely characterized, and observed effects in animals do not establish therapeutic benefit or safety.

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.

Notes from published material

An aphrodisiac is a substance that increases libido, sexual desire, sexual attraction, sexual pleasure, or sexual behavior. These substances range from a variety of plants, spices, and foods to synthetic chemicals. Natural aphrodisiacs, such as cannabis or cocaine, are classified into plant-based and non-plant-based substances. Synthetic aphrodisiacs include MDMA and methamphetamine. Aphrodisiacs can be classified by their type of effects (psychological or physiological). Aphrodisiacs that contain hallucinogenic properties, such as bufotenin, have psychological effects that can increase sexual desire and sexual pleasure. Aphrodisiacs that have smooth muscle relaxing properties, such as yohimbine, have physiological effects that can affect hormone concentrations and increase blood flow. Substances that have the opposite effects on libido are called anaphrodisiacs. Aphrodisiac effects can also be due to the placebo effect. Both males and females can potentially benefit from the use of aphrodisiacs, but they are more focused on males, as their properties tend to increase testosterone concentrations rather than estrogen concentrations. This is in part due to the historical context of aphrodisiacs, which focused solely on males. Only recently has attention been paid to understanding how aphrodisiacs can aid female sexual function. In addition, cultural influences on appropriate sexual behavior of males and females also play a part in the research gap.

DHIS2 (also spelled DHIS 2, formerly District Health Information Software) is a free and open-source software platform for the collection, reporting, analysis and dissemination of aggregate and individual-level data. DHIS2 is used as a national-scale HMIS in more than 70 countries, covering key health data for over 40% of the world’s population. The most common use of DHIS2 is for health data, where it can be implemented for individual health programs and/or as a national-scale Health Management Information System (HMIS). As of the end of 2022, DHIS2 was in use by Ministries of Health in more than 75 low- and middle-income countries (LMICs), with 69 countries using DHIS2 at national scale. Beyond health, DHIS2 is used in sectors such as education, supply chain and logistics, water and sanitation, nutrition and food security, agriculture and land management, and e-governance, among others. DHIS2 is officially recognized as a Digital Public Good. Development of the core DHIS2 software is coordinated by the HISP Centre at the University of Oslo (formerly the Health Information Systems Programme), where it is housed within the Department of Informatics. The DHIS2 project is supported financially by a coalition of global partners, including Norad; PEPFAR; The Global Fund to Fight AIDS, Tuberculosis and Malaria; UNICEF; Gavi, the Vaccine Alliance; the U.S. Centers for Disease Control and Prevention; the Bill & Melinda Gates Foundation; and the University of Oslo. The HISP Centre is an official Collaborating Centre of the World Health Organization.

== Recruitment == Finding a potential sperm donor, and motivating him to donate sperm, is referred to as recruitment. A sperm bank can recruit donors by advertising—-often in colleges, in local newspapers, and on the internet. A donor must be a fit and healthy male, normally between 18 and 45 years of age, willing to undergo frequent rigorous testing. The donor must also be willing to donate his sperm so that it can be used to impregnate people who are unrelated to him whom he does not know. Some sperm banks require two screenings and a laboratory screening before a donor is eligible. The donor must agree to relinquish all legal rights to all children who result from his donations. The donor must produce his sperm at the sperm bank, thus enabling the identity of the donor, once proven, to be ascertained. Some sperm banks have been accused of heightism due to minimum height requirements.

The pancreas plays a vital role in the digestive system. It does this by secreting pancreatic juice, a fluid that contains digestive enzymes, into the duodenum, the first part of the small intestine that receives food from the stomach. These enzymes help to break down carbohydrates, proteins and lipids (fats). This is the exocrine role of the pancreas. The cells responsible for this are acinar cells arranged in clusters called acini. Secretions into the middle of the acinus accumulate in intralobular ducts, which drain to the main pancreatic duct, which drains directly into the duodenum. About 1.5–3 liters of fluid are secreted in this manner every day. The cells in each acinus are filled with granules containing the digestive enzymes. These are secreted in an inactive form termed zymogens or proenzymes. When released into the duodenum, they are activated by the enzyme enterokinase present in the lining of the duodenum. The proenzymes are cleaved, creating a cascade of activating enzymes.

=== Distribution === The plasma protein binding of testosterone is 98.0 to 98.5%, with 1.5 to 2.0% free or unbound. It is bound 65% to sex hormone-binding globulin (SHBG) and 33% bound weakly to albumin.

Sources: en.wikipedia.org

Further detail

=== Awards === In 2007, British investors evaluated six nominated private companies and chose to Camurus as the best privately owned biotechnology company in the Medicon Valley. The company was awarded the Strictly Financing Award 2007. In 2013, Camurus was awarded CPhI Pharma Award for Best Innovation in Formulation.

== History == The physical principles of ion traps were first explored by F. M. Penning, who observed that electrons released by the cathode of an ionization vacuum gauge follow a long cycloidal path to the anode in the presence of a sufficiently strong magnetic field. Later Wolfgang Paul developed a method to trap ions without magnetic fields that was based on his work with quadrupole mass spectrometers. Ion traps were used in television receivers prior to the introduction of aluminized CRT faces around 1958, to protect the phosphor screen from ions. The ion trap must be delicately adjusted for maximum brightness.

==== Effects ==== RO5263397 has been found to increase the firing rates of ventral tegmental area (VTA) dopaminergic neurons and dorsal raphe nucleus (DRN) serotonergic neurons in mouse brain slices ex vivo. This is in contrast to the high-efficacy TAAR1 agonists p-tyramine, RO5166017, and RO5256390, which inhibit these neurons in such systems, but is similar to the increased firing rates with the TAAR1 antagonist EPPTB, supporting a partially agonistic profile of RO5263397 at the mTAAR1. RO5263397 can partially and dose-dependently reverse the suppressive effects of RO5256390 on monoaminergic neuron firing in brain slices ex vivo. In contrast to VTA dopaminergic and DRN serotonergic neurons, RO5263397 had no effect on locus coeruleus (LC) noradrenergic neurons in the system, where the TAAR1 is notably not expressed. The effects of RO5263397 on the firing frequencies of monoaminergic neurons are absent in TAAR1 knockout mice. RO5263397 has been found to fully prevent methamphetamine-induced dopamine release in rat nucleus accumbens core (NAcc) brain slices ex vivo. Conversely, RO5263397 by itself had no effect on dopamine overflow in rat NAcc slices ex vivo. RO5263397 alone has no effect on locomotor activity in rodents in vivo. Similarly, RO5263397 did not affect locomotor activity in monkeys. Conversely, RO5263397 has been found to dose-dependently and fully inhibit cocaine-induced hyperlocomotion in mice in vivo. Likewise, it dose-dependently inhibited hyperlocomotion induced by the NMDA receptor antagonists phencyclidine (PCP) and L-687,414 in mice in vivo.

Strontium commonly occurs in nature, being the 15th most abundant element on Earth (its heavier congener barium being the 14th), estimated to average approximately 360 parts per million in the Earth's crust and is found chiefly in two mineral forms: the sulfate (celestine, SrSO4) and the carbonate (strontianite, SrCO3). Of the two, celestine occurs much more frequently in deposits of sufficient size for mining. Because strontium is used most often in the carbonate form, strontianite would be the more useful of the two common minerals, but few deposits have been discovered that are suitable for development. Because of the way it reacts with air and water, strontium only exists in nature when combined to form minerals. Naturally occurring strontium is stable, but its synthetic isotope Sr-90 is only produced by nuclear fallout. In groundwater, strontium behaves chemically much like calcium. At intermediate to acidic pH, Sr(2+) is the dominant strontium species. In the presence of calcium ions, strontium commonly forms coprecipitates with calcium minerals such as calcite and anhydrite at an increased pH. At intermediate to acidic pH, dissolved strontium is bound to soil particles by cation exchange. The mean strontium content of ocean water is 8 mg/L. At a concentration between 82 and 90 μmol/L of strontium, the concentration is considerably lower than the calcium concentration, which is normally between 9.6 and 11.6 mmol/L. It is nevertheless much higher than that of barium, 13 μg/L.

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 legal?

Legal status varies by country. It is not approved as a medicine, and it is prohibited in sport. Some jurisdictions restrict import, sale, or possession.

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