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Background And Regulatory History — Reference Sheet

By Editorial Desk · published 2026-07-28 · last reviewed 2026-08-01 · Faq

This is a working overview of PPARδ agonist, written for readers who want more than a one-paragraph summary but less than a textbook.

This page was last updated on 2026-08-01 and is reviewed periodically as new material appears.

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.

Detection and Regulatory Landscape

A common misconception is that cardarine has been proven safe for human use. In reality, human clinical data are limited, and long-term animal studies have raised concerns about cancer. Another misconception is that it is a supplement or vitamin-like compound. It is a synthetic research chemical with no approved medical indication. Scientific discussion often focuses on its mechanism and detection rather than therapeutic use. Regulatory and anti-doping literature treats it primarily as a prohibited substance.

Cardarine is explicitly prohibited by the World Anti-Doping Agency under the class of PPARδ agonists. Its presence in urine or blood samples can be detected using mass spectrometry-based methods, often liquid chromatography-tandem mass spectrometry. Athletes who test positive may face sanctions, including bans from competition. The compound is also regulated as a prescription-only or unapproved drug in many countries. Enforcement varies by jurisdiction, and some regions treat it as a controlled substance. Online sales may occur despite these restrictions, creating quality and legal risks.

Laboratory detection of cardarine typically involves sample preparation followed by chromatographic separation and mass spectrometric identification. Urine is the most common matrix for anti-doping tests, though blood and hair have also been explored. Methods can target the parent compound or its metabolites, depending on the expected window of detection. Reference standards are required for accurate quantification. Matrix effects and dilution can influence results, so laboratories use internal standards and validation protocols. The exact detection window varies with dose, route, and individual metabolism.

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.

Mechanism and Detection

Preclinical research reported that GW501516 increased running endurance in mice and improved lipid profiles in some animal species. Early human trials explored effects on high-density lipoprotein cholesterol, triglycerides, and glucose handling, but the program was discontinued. Published human data are sparse and do not establish efficacy for any condition. Studies also examined PPAR delta in cancer biology, with conflicting findings across models. The relationship between receptor activation, tissue context, and disease risk remains an active area of investigation.

Anti-doping laboratories identify GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the usual matrix, and detection can occur after the parent compound has cleared from blood. The exact detection window depends on dose, formulation, individual metabolism, and assay sensitivity. Because the compound is prohibited at all times, athletes are subject to testing in and out of competition. Analytical methods continue to improve as new metabolites and designer analogs are characterized.

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Preclinical Findings and Safety Signals

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.

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.

Supporting material

=== MHC class II + peptide interactions === HLA-DM is an integral protein in the mechanism regulating which antigens are presented extracellularly on APCs. It binds partially to the peptide-binding groove of MHC class II molecules. This can affect how well your immune system responds to foreign invaders. HLA-DM is required to release CLIP from MHC class II molecules, to chaperone empty MHC molecules against denaturation, and to control proper loading and release of peptides at the peptide-binding groove. It also interacts heavily with chaperone protein HLA-DO. All of this ensures proper antigen presentation by an APC, to activate other immune cells. This is critical to rid the body of harmful infections. For example, proper antigen presentation benefits T cell activation, and memory T cell survival and generation. Without it, T cells leaving their site of production and entering the circulatory vessels of the body will not be activated against a danger. The immune system will not be able to kill dangerous or infected cells, and will not react quickly against a second infection.

Portugal's main import markets in 2026 were Spain at 32.9% and Germany at 11.9%. Portugal's main imports are machinery and mechanical appliances, chemical products, agricultural products, and mineral fuels. Since the 1990s, Portugal's economic model has been based on public consumption and economic development focused on exports, private investment and the development of its high-tech sector. Consequently, business services have overtaken more traditional industries such as wine and cork in export earnings. Operated by the Euronext Lisbon, Portugal's stock market, the PSI, includes 16 major companies based on the country, including Sonae, Mota-Engil, Corticeira Amorim, The Navigator Company, and EDP. In 2025, Portugal ranked 16th among European Union member states in innovation by the European Innovation Scoreboard, while placing 31st worldwide in the Global Innovation Index. In 2024, neuroscience accounted for 12.5% of Portugal's scientific output, the second-highest national share, and the country ranked 23rd worldwide in total neuroscience output. Among the research institutions based in the country are the Gulbenkian Institute of Molecular Medicine, the International Iberian Nanotechnology Laboratory, and the Champalimaud Foundation which was the world's 11th top non-profit institution in neuroscience research between 2019 and 2023.

Viral inactivation is the process of rendering a virus incapable of causing infection. It plays a critical role across multiple fields, including clinical medicine, diagnostics, research, and the food industry. In clinical practice, inactivation is essential for preventing viral transmission through blood products—such as transfusions and other biological materials—as well as in biopharmaceutical manufacturing. In diagnostic and research contexts, inactivation enables the safe study and manipulation of viruses without risking transmission to laboratory staff or healthcare personnel. Moreover, in vaccine development, inactivated viruses are employed to stimulate the host immune system, promoting the production of neutralizing antibodies. A wide range of viral inactivation techniques exist, ranging from physical removal by filtration to mechanical and chemical methods. The choice of technique depends on the specific context and intended purpose. In many situations, a combination of methods is employed—particularly when handling highly pathogenic viruses—where absolute sterility is crucial. Some of the more common viruses removed by these methods are the HIV-1 and HIV-2 viruses; hepatitis A, B, and C; and parvoviruses.

== Medical uses == Ixazomib is used in combination with lenalidomide and dexamethasone for the treatment of multiple myeloma in adults after at least one prior therapy. There are no experiences with children and youths under 18 years of age. The study relevant for approval included 722 people. In this study, ixazomib increased the median time of progression-free survival from 14.7 months (in the placebo+lenalidomide+dexamethasone study arm including 362 people) to 20.6 months (under ixazomib+lenalidomide+dexamethasone, 360 people), which was a statistically significant effect (p = 0.012). 11.7% of patients in the ixazomib group had a complete response to the treatment, versus 6.6% in the placebo group. Overall response rate (complete plus partial) was 78.3% versus 71.5%. A phase 3 study demonstrated a significant improvement in progression-free survival (PFS) with ixazomib-lenalidomide-dexamethasone (IRd) compared with placebo. High-risk cytogenetic abnormalities were defined as del(17p), t(4;14), and/or t(14;16); additionally, patients were assessed for 1q21 amplification. Of 722 randomized patients, 552 had cytogenetic results; 137 (25%) had high-risk cytogenetic abnormalities and 172 (32%) had 1q21 amplification alone. PFS was improved with IRd versus placebo in both high-risk and standard-risk cytogenetics subgroups: in high-risk patients, with median PFS of 21.4 versus 9.7 months; in standard-risk patients, with median PFS of 20.6 versus 15.6 months.

Ash is the solid remnants of fires. Specifically, ash refers to all non-aqueous, non-gaseous residues that remain after something burns. In analytical chemistry, to analyse the mineral and metal content of chemical samples, ash is the non-gaseous, non-liquid residue after complete combustion. Ashes as the end product of incomplete combustion are mostly mineral, but usually still contain an amount of combustible organic or other oxidizable residues. The best-known type of ash is wood ash, as a product of wood combustion in campfires, fireplaces, etc. The darker the wood ashes, the higher the content of remaining charcoal from incomplete combustion. The ashes are of different types. Some ashes contain natural compounds that make soil fertile. Others have chemical compounds that can be toxic but may break down in soil from chemical changes and microorganism activity. Like soap, ash is also a disinfecting agent (alkaline). The World Health Organization recommends ash or sand as alternative for handwashing when soap is not available. Before industrialization, ash soaked in water was the primary means of obtaining potash.

Sources: en.wikipedia.org

Notes from published material

The mass number of this isotope was not clearly established (possibly 258 or 259) at the time. In 1965, 256Lr was synthesized by Flyorov et al. from 243Am and 18O. Thus IUPAC recognized the nuclear physics teams at Dubna and Berkeley as the co-discoverers of lawrencium.

At a White House press briefing on September 22, 2025, President Trump, joined by Kennedy and other senior officials, said the FDA would revise drug labels to discourage the use of acetaminophen (sold under the brand name Tylenol) during pregnancy, citing a possible link to autism. Medical and public health experts disputed the claim. Steven J. Fleischman, president of the American College of Obstetricians and Gynecologists, wrote, "It is highly unsettling that our federal health agencies are willing to make an announcement that will affect the health and well-being of millions of people without the backing of reliable data." A month later, on October 29, Kennedy retracted his statements from the press conference, stating that acetaminophen use in pregnancy is not linked to autism. On November 10, 2025, in response to President Trump's false claim, a 2025 British Medical Journal umbrella review was fast-tracked and confirmed no convincing evidence that paracetamol (acetaminophen) use during pregnancy increases the risk of autism spectrum disorder (ASD) or attention deficit hyperactivity disorder (ADHD) in children. The review, led by researchers at the University of Liverpool, analysed nine systematic reviews covering 40 observational studies and concluded that any apparent associations were likely due to family genetics, maternal health, or other shared factors rather than the drug itself.

His funeral in Medellín drew crowds of mourners and prompted national reflection on the violence surrounding the game. Humberto Muñoz Castro, a bodyguard employed by the alleged drug trafficker Santiago Gallón, confessed to the shooting and was sentenced to 43 years' imprisonment, of which he served eleven; investigators discounted early suggestions that gambling syndicates had ordered the killing, though the theory persisted.

121. Paul T, Paul T, Katwal S, Aroori P, Dawer P, Bhatia H, Njideaka-Kevin T, Guntipalli P, Yadav T. Benzene and human health: a comprehensive review of carcinogenic risks, mechanisms, and preventive strategies. Ann Med Surg (Lond). 2025 Sep 3;87(11):7206-7212. doi: 10.1097/MS9.0000000000003806. PMID 41180735; PMCID: PMC12578042.

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 banned in sports?

Yes, WADA prohibits cardarine as a PPARδ agonist. It appears on the prohibited list and can be detected in urine or blood. Athletes using it risk sanctions.

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