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Identity And Regulatory Status — Questions and Answers

By Editorial Desk · published 2025-08-04 · last reviewed 2025-09-06 · Info

If you have been reading about Cardarine 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 2025-09-06. 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.

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.

Cardarine is the common name for GW501516, a synthetic compound studied as a peroxisome proliferator-activated receptor delta agonist. Researchers developed it to explore treatments for lipid disorders and metabolic conditions. It is not an approved medicine in any country. Early clinical work examined changes in HDL cholesterol and triglycerides, but development was discontinued after animal studies raised concerns about cancer. The compound remains available as a research chemical and appears in discussions of performance enhancement.

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

Background from the literature

== Research on supplement use == Theanine supplements have been marketed with a variety of claims that they improve cognitive performance, reduce stress, improve sleep quality, and alleviate menstrual cramps. Evaluating these claims in 2011, the European Food Safety Authority assessed they were not supported by evidence in studies provided at that time. A 2020 review of studies suggested that L-theanine supplementation of 200–400 milligrams per day may reduce stress and anxiety in people with acute stress, but there was insufficient evidence for the use of L-theanine as a medication to treat stress and anxiety. A 2024 review indicated that L-theanine supplementation may be more effective than placebo in alleviating psychopathological symptoms associated with anxiety disorders, ADHD, and schizophrenia. A 2025 review reported that theanine research has lacked rigor, was mainly based on anecdotes, had ill-defined mechanisms, and exhibited unreliable clinical trials.

=== Intrauterine administration === A one-year progesterone intrauterine device (IUD) for hormonal birth control was previously available in the United States and a few other countries under the brand name Progestasert. It was marketed between 1976 and 2001. The IUD was never widely used due to a relatively high contraceptive failure rate of 2.9% and the requirement of annual replacement. It contained 38 mg progesterone and released 65 μg progesterone into the uterus per day (totaling up to about 35 mg after one year). For comparison, a woman's body produces on average about 25 mg progesterone per day during the luteal phase. While effective as a form of contraception and for decreasing menstrual bleeding and discomfort, long-lived IUDs can fundamentally only deliver small amounts of progesterone per day, and hence intrauterine progesterone cannot achieve adequate circulating progesterone levels and is unsuitable as a form of systemic therapy. Aside from progesterone, IUDs of progestins, such as levonorgestrel (Mirena/Levosert/Skyla), are available as well.

=== 25 April === At least 11 people were killed in an RSF drone strike in Atbara that hit a displaced persons camp and energy facilities. RSF shelling from Salha in Omdurman hit the SAF's general headquarters in Khartoum.

This process is similar to angiogenesis but involves the creation of lymphatic vessels which are essential for draining excess fluid and fighting infections. This process is also key to conditions like inflammation and the spreading of cancer.

Sources: en.wikipedia.org

Related pages on this site

Reference notes

=== Physical examination === Inspection of the patient's skin, particularly on the lower extremities, in conjunction with a thorough medical history, can provide valuable information regarding the possible presence of sudomotor dysfunction. Evidence of altered skin hydration, such as hyperkeratosis, excessive skin dander, rhagades, and ulcers, can be suggestive of sudomotor dysfunction. Presence of intense foot odor may be another presentation.

== Laboratory methods == Hemoglobin A2 has a crucial role in screening and diagnosis of the beta-thalassemia trait. Various laboratory methods exist, each providing different outcomes of accuracy. The different quantification methods of HbA2 relies on how effective it can be separated from other hemoglobin variants. Various laboratory methods are employed, such as cation exchange high-performance liquid chromatography (HPLC), microcolumn chromatography, and cellulose acetate electrophoresis with elution. At first, cellulose acetate electrophoresis was utilized to measure HbA2, but this process proved to be too time-consuming and labor-intensive, making it impractical for large examinations or samples. Similar efficiency issues were encountered with other methods like IEF and scanning densitometry. These two methods separate proteins based on their isoelectric point. Chromatography, another commonly used method, demonstrated reliability in diagnosing individuals with the beta carrier gene. However, this method was also time-consuming and inefficient when dealing with large sample numbers. Out of the various methods, the one that accurately measures HbA2 is HPLC. It is a reliable technique because it's able to accurately determine HbA2, HbF, and Hb variants. The various different Hb variants include: HbS, HbE, Hb Lepore, HbC, HbD and HbO-Arab. There are several different factors that can contribute to the quantification of HbA2 to be inaccurately measured.

Chronic consumption is also associated with an effect on CREB phosphorylation and function via postsynaptic NMDA receptor signaling cascades through a MAPK/ERK pathway and CAMK-mediated pathway. These modifications to CREB function in the mesolimbic pathway induce expression (i.e., increase gene expression) of ΔFosB in the NAcc, where ΔFosB is the "master control protein" that, when overexpressed in the NAcc, is necessary and sufficient for the development and maintenance of an addictive state (i.e., its overexpression in the nucleus accumbens produces and then directly modulates compulsive alcohol consumption).

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.

What is cardarine?

Cardarine is a common name for the investigational compound GW501516. It acts as a PPARδ agonist and is not approved for human use. It is prohibited in sport.

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