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Background And Regulatory History — Reference Sheet

By Editorial Desk · published 2025-09-16 · last reviewed 2025-09-30 · News

The short version of Investigational drug fits in a sentence. The long version — which is the one that helps — is below.

This page was last updated on 2025-09-30 and is reviewed periodically as new material appears.

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.

Identity and Pharmacological Classification

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.

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.

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

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.

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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.

Background from the literature

Fermium is a synthetic chemical element; it has symbol Fm and atomic number 100. It is an actinide and the heaviest element that can be formed by neutron bombardment of lighter elements, and hence the last element that can be prepared in macroscopic quantities, although pure fermium metal has not been prepared yet. A total of 20 isotopes are known, with 257Fm being the longest-lived with a half-life of 100.5 days. Fermium was discovered in 1952 in the debris of the first detonation test of a hydrogen bomb, and named after Enrico Fermi, one of the pioneers of nuclear physics. Its chemistry is typical for the late actinides, with a preponderance of the +3 oxidation state but also an accessible +2 oxidation state. Owing to the small amounts of produced fermium and all of its isotopes having relatively short half-lives, there are currently no uses for it outside basic scientific research.

Researchers report in a preprint the CRISPR alternative fanzor naturally present in eukaryotes with several potential advantages over CRISPR in genome editing, notably smaller size and higher selectiveness. A separate team further demonstrates in a preprint (14 June) the potential of this class of genome editors. 29 June – Astronomers report using a new technique to detect, for the first time, the release of neutrinos from the galactic plane of the Milky Way galaxy. Hazard research is published: study results suggest high-temperature cooking could cause DNA damage within food (especially meat) which in turn could cause human DNA damage (1 June), a study concludes the Italian Phlegraean Fields could be heading towards a first eruption since 1538 (9 June), a small team of researchers evaluates the credibility of net-zero climate targets as currently low (9 June), an AHA review shows that exposure to contaminant metals contributes to cardiovascular diseases (12 June), a study in the context of the opioid epidemic shows males are substantially (2–3 times greater) more vulnerable to or affected by drug overdose mortality than females (15 June), loss of Y chromosome can drive cancer growth (21 June), a study indicates nearly 40% of U.S.

=== Late onset === In milder (or partial) urea cycle enzyme deficiencies, ammonia accumulation may be triggered by illness or stress at almost any time of life, resulting in multiple mild elevations of plasma ammonia concentration [Bourrier et al. 1988]. Patients with partial enzyme deficiencies may have a delay of symptoms for months or years. Indicators that you maybe suffering from OTC deficiency or a urea cycle disorder include "episodes of delirium, erratic behavior, or reduced consciousness, headaches, vomiting, aversion to foods high in protein, and seizures."

Sources: en.wikipedia.org

Reference notes

== History == The first documented case of gutter oil in Taiwan was reported in 1985. In a subsequent investigation, 22 people were arrested for involvement in a recycling oil ring over 10 years based in Taipei. The worst offender was sentenced to 7 years in prison. The first documented case of gutter oil in mainland China was reported in 2000, when a street vendor was found to be selling oil obtained from restaurant garbage disposals. Some street vendors and restaurants in China are reported to have illegally used recycled oil unfit for human consumption to cook food. In 2010, it was estimated that gutter oil represented 10% of China's edible oil market (with 1 in every 10 restaurants using it) and that 3 million tonnes of gutter oil were consumed in China annually, with a network of distributors of gutter oil across central and eastern China. In 2011, the Chinese government began a major crackdown on the re-use of gutter oil for human consumption. In 2011, they arrested 32 people for producing the oil and seized 90 tonnes of it in 14 provinces. This amount is equivalent to around one-tenth of the oil typically used by restaurants. Feng Ping of the China Meat Research Center has said that "[t]he illegal oil shows no difference in appearance and indicators after refining and purification, because the law breakers are skillful at coping with the established standards." In September 2012, an ongoing investigation into the suspected use of gutter oil as a raw material in the Chinese pharmaceutical industry was revealed.

amino acid Any of a class of organic compounds whose basic structural formula includes a central carbon atom bonded to amine and carboxyl functional groups and to a variable side chain. Out of nearly 500 known amino acids, a set of 20 are coded for by the standard genetic code and incorporated into long polymeric chains as the building blocks of peptides and hence of polypeptides and proteins. The specific sequences of amino acids in the polypeptide chains that form a protein are ultimately responsible for determining the protein's structure and function.

The coffee tree produces fruit often referred to as a coffee cherry, but unlike the cherry, which contains a single pit, it most commonly contains two seeds with their flat sides together. The seeds are referred to as beans because of their appearance, though they are not true beans. A few coffee cherries, referred to as "peaberries" contain a single seed; they make up around 10% to 15% of all coffee beans. It is sometimes asserted that because the single bean does not need to share nutrients between two separated beans, it has a superior flavour profile with bright acidity, sweetness, and concentrated and complex flavours, but there is little evidence to support this; for example, peaberries may have been selected from high-quality beans. Coffee trees range from 5 to 10 m (16 to 33 ft) in height. As the tree gets older, it produces less fruit and slowly loses its resistance to pests and diseases. The coffee beans are in the seeds of fruits from trees and shrubs that originally grew naturally in African forests. Humans produce coffee by roasting, grinding and brewing the raw (green) coffee beans. Coffee plants are often grown in rows spaced apart depending on the desired density chosen by the farmer. Some farmers plant shade trees or cash-crop trees, such as orange trees, around them, or plant the coffee on the sides of hills to provide the conditions coffee needs to flourish.

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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