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Background And Regulatory History — Reference Sheet

By Editorial Desk · published 2026-07-05 · last reviewed 2026-07-20 · Info

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

Last reviewed on 2026-07-20. Where a claim depends on a specific study, the study is described rather than over-claimed.

Background and Regulatory History

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.

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.

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.

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.

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.

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Regulation and Analytical Detection

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.

Regulation and Detection

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.

Anti-doping laboratories identify GW501516 and related metabolites using liquid chromatography coupled with tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be analyzed. The method targets the parent compound and phase I and phase II metabolites, which extend the detection window. Because the substance is prohibited at all times, athletes can be tested outside competition. Detection limits and windows depend on the assay, sample type, and individual metabolism.

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.

Notes from published material

== Works == Gish, Duane T. 15 Scopus Publishers. Gish, Duane T. (1972). Speculations and Experiments on the Origins of Life. New Leaf Pr. ISBN 0-89051-010-5. Gish, Duane T. (1972). Evidence against evolution. Wheaton, Ill: Tyndale House Publishers. ISBN 0-8423-0790-7. Gish, Duane T. (1986) [1972]. Evolution, the fossils say no!. San Diego, Calif: Institute for Creation Research Publishing. ISBN 0-89051-057-1. Gish, Duane T. (1973). Have You Been... Brainwashed?. Seattle, Washington: Life Messengers. p. 32. OCLC 10930514. Hillestad, George M.; Morris, Henry; Gish, Duane T. (1974). Creation: acts, facts, impacts. San Diego, Calif: ICR Pub. Co. ISBN 0-89051-020-2. Gish, Duane T. (1977). Dinosaurs: Those Terrible Lizards. Green forest, Arkansas: Master Books. ISBN 0-89051-039-3. Rohrer, Donald H.; Gish, Duane T. (1978). Up with creation!: ICR acts/facts/impacts, 1976-1977. San Diego, California: Creation-Life Publishers. ISBN 0-89051-048-2. Gish, Duane T.; Wilson, Clifford (1981). Manipulating life, where does it stop?: Genetic engineering. Green Forest, Arkansas: Master Books. ISBN 0-89051-071-7. Gish, Duane T. (1985). Evolution: the challenge of the fossil record. San Diego, Calif: Creation-Life Publishers. ISBN 0-89051-112-8. Gish, Duane T. (1988). Creationist Research 1964-1988. Creation Research Society. ISBN 0-940384-06-X. Bonnie Snellenberger; Gish, Duane T.; D Dish; Earl Snellenberger (1990). The Amazing Story of Creation: From Science and the Bible. Green Forest, Arkansas: Master Books. ISBN 0-89051-120-9.

=== Immunity === The main immune cells active in the tissue are macrophages and neutrophils, although other leukocytes are also present. These work to phagocytize old or damaged tissue, and protect the healing tissue from pathogenic infection. This is necessary both to aid the healing process and to protect against invading pathogens, as the wound often does not have an effective skin barrier to act as a first line of defense.

The chemical structure of penicillin was first proposed by Edward Abraham in 1942 and was later confirmed in 1945 using X-ray crystallography by Dorothy Crowfoot Hodgkin, who was also working at Oxford. She later in 1964 received the Nobel Prize in Chemistry for this and other structure determinations. The chemist John C. Sheehan at the Massachusetts Institute of Technology (MIT) completed the first chemical synthesis of penicillin in 1957. Sheehan had started his studies into penicillin synthesis in 1948, and during these investigations developed new methods for the synthesis of peptides, as well as new protecting groups—groups that mask the reactivity of certain functional groups. Although the initial synthesis developed by Sheehan was not appropriate for mass production of penicillins, one of the intermediate compounds in Sheehan's synthesis was 6-aminopenicillanic acid (6-APA), the nucleus of penicillin. 6-APA was discovered by researchers at the Beecham Research Laboratories (later the Beecham Group) in Surrey in 1957 (published in 1959). Attaching different groups to the 6-APA 'nucleus' of penicillin allowed the creation of new forms of penicillins which are more versatile and better in activity.

==== Sen-chan ==== Senichi Enari (江成 仙一, Enari Sen'ichi), also known as "Sen-chan" (センちゃん), is the eccentric, yet calmest and smartest member, of the team, due in part to his ability to think things through and being able to do his best thinking while in a handstand, which he considers his "thinking pose". Sen-chan serves as Deka Green (デカグリーン, Deka Gurīn). The oldest of seven siblings from a poor family, he displays nycto- and claustrophobia after accidentally falling into a well when he was a child. He was subsequently rescued by a policeman, which inspired him to take up police work. Despite his usually calm demeanor, he is said to be scary when angered. He also displays a crush on his teammate Umeko, but avoids showing it publicly. As of the crossover film Mahō Sentai Magiranger vs. Dekaranger, they have moved in together. As Deka Green, Sen-chan wields the D-Knuckle and D-Rod, which can combine to form the D-Blaster (ディーブラスター, Dī Burasutā) rifle. He also shares riding the Machine Bull (マシンブル, Mashin Buru) police car with Umeko. Using the D-Rod, Sen-chan can perform the Green Crash (グリーンクラッシュ, Gurīn Kurasshu) attack. Sen-chan is portrayed by Yousuke Itou (伊藤 陽佑, Itō Yōsuke). As a child, he is portrayed by Kengo Tajima (田島 健吾, Tajima Kengo).

Common side effects include low blood sugar, nausea, dizziness, abdominal pain, and pain at the site of injection. Gastrointestinal side-effects tend to be strongest at the beginning of treatment period and subside over time. Other serious side effects may include angioedema, pancreatitis, gallbladder disease, and kidney problems. Use in pregnancy and breastfeeding is of unclear safety. A boxed warning in the US prescribing information cautions that medullary thyroid cancers have been observed in rats treated with liraglutide, but it is "unknown whether liraglutide causes thyroid C-cell tumors, including medullary thyroid carcinoma, in humans, as relevance to humans of such tumors in rodents has not been determined."

Sources: en.wikipedia.org

Background from the literature

Many substances regarded as poisons are toxic only indirectly, by toxication. An example is "wood alcohol" or methanol, which is not poisonous itself, but is chemically converted to toxic formaldehyde and formic acid in the liver. Many drug molecules are made toxic in the liver, and the genetic variability of certain liver enzymes makes the toxicity of many compounds differ between individuals. Exposure to radioactive substances can produce radiation poisoning, an unrelated phenomenon. Two common cases of acute natural poisoning are theobromine poisoning of dogs and cats, and mushroom poisoning in humans. Dogs and cats are not natural herbivores, but a chemical defense developed by Theobroma cacao can be incidentally fatal nevertheless. Many omnivores, including humans, readily consume edible fungi, and thus many fungi have evolved to become decisively inedible, in this case as a direct defense.

Other major football, ice hockey, and basketball teams are based in Moscow. Because sports organizations in the Soviet Union were once centralized, two of the best Union-level teams represented defense and law-enforcement agencies: the Armed Forces (CSKA) and the Ministry of Internal Affairs (Dinamo). Most major cities had army and police sports teams. As a result, Spartak, CSKA, and Dinamo were among the best-funded teams in the USSR. The Irina Viner-Usmanova Gymnastics Palace is located in the Luzhniki Olympic Complex. Construction of the Palace started in 2017, and the opening ceremony took place on 18 June 2019. The Palace was financed by billionaire Alisher Usmanov, husband of the former gymnast and gymnastics coach Irina Viner-Usmanova. The total area of the building is 23,500 square meters (253,000 sq ft), which includes three fitness rooms, locker rooms, rooms for referees and coaches, saunas, a canteen, a cafeteria, two ball halls, a medical center, a hall for journalists, and a hotel for athletes. Because of Moscow's cold climate, winter sports are popular. Many of Moscow's parks offer marked trails for skiing and frozen ponds for skating.

Medical acupuncture attempts to integrate reflexological concepts, the trigger point model, and anatomical insights (such as dermatome distribution) into acupuncture practice, and emphasizes a more formulaic approach to acupuncture point location. Cosmetic acupuncture is the use of acupuncture in an attempt to reduce wrinkles on the face. Bee venom acupuncture is a treatment approach of injecting purified, diluted bee venom into acupoints. Veterinary acupuncture is the use of acupuncture on domesticated animals.

=== Techniques === MRI: Meningeal findings are described with the following characteristics: Nodular meningeal tumor, meningeal thickening >3 mm and a subjectively strong contrast enhancement. A smooth contrast enhancement of the meninges was judged to be typical for inflammatory, nonneoplastic meningitis. CSF cytology: is performed after drawing the CSF by lumbar puncture. Cytogenetic: measures chromosomal content of cells and fluorescence in situ hybridization which detects numerical and structural genetic aberrations as a sign of malignancy. This is especially useful for liquid tumors such as leukemia and lymphoma. Some of the techniques that achieve this are flow cytometry and DNA single-cell cytometry. However, cytogenetic only assist in diagnosis and is less preferred. Meningeal Biopsy: may be performed when all of the above criteria is inconclusive, or if the primary malignancy is unknown. Biopsy is only effective when performed at the region where there's enhancement on the MRI.

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 also known as?

Cardarine is commonly known as GW501516 or GW-1516. These names refer to the same synthetic compound. It is not a brand-name approved medicine.

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