If you have been reading about Metabolic modulator 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.
Last reviewed on 2026-07-01. Where a claim depends on a specific study, the study is described rather than over-claimed.
Early clinical research explored GW501516 for lipid disorders, obesity, and diabetes. Some short-term human studies reported changes in HDL cholesterol, LDL cholesterol, and triglycerides. The development program was discontinued after rodent studies showed dose-dependent tumor formation in multiple tissues, including liver, bladder, stomach, and skin. These findings raised concerns about long-term cancer risk in humans. Because human exposure data are limited, the clinical significance of the rodent tumors remains uncertain.
Literature on cardarine often separates receptor pharmacology from toxicology. Mechanistic papers describe PPARδ activation and gene expression changes, while safety assessments focus on carcinogenicity and species differences. Questions remain about whether rodent tumors arise through PPARδ-dependent or off-target mechanisms. Another open area is how human metabolism and exposure compare with those in animal studies. Analytical methods such as liquid chromatography–mass spectrometry are used to confirm identity in biological and product samples.
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.
| Property | Value | Notes |
|---|---|---|
| Primary target | PPARδ | Nuclear receptor; not androgen receptor |
| Studied indications | Dyslipidemia; obesity; diabetes | Early clinical research; development discontinued |
| Rodent toxicity | Tumor formation in multiple tissues | Dose-dependent findings in some studies |
| Human approval | None | No approved therapeutic use |
| Typical analytical method | LC-MS/MS | Used for identity and quantification |
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.
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.
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.
GW501516 acts as a ligand for PPAR delta, a nuclear receptor that regulates transcription of genes involved in fatty acid oxidation and energy use. Activation of this receptor in skeletal muscle shifts metabolism toward fat burning in animal models. The compound does not burn fat directly; it changes gene expression over hours to days. Researchers study it to understand metabolic flexibility and exercise adaptation. Effects observed in rodents are not automatically expected in humans.
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.
== External links == Creatine+Kinase,+Mitochondrial+Form at the U.S. National Library of Medicine Medical Subject Headings (MeSH) This article incorporates text from the United States National Library of Medicine, which is in the public domain.
== Main publications == Photoaffinity labeling of corticotropin receptors (co-author, PNAS (USA) 77: 3967-3970, 1980) Comparison of the tyrosine kinase activity with the proliferation rate in human solid tumors and tumor cell lines (co-author, TUMOR BIOLOGY 9: 315-322, 1988) Flk1 as a Target for Tumor Growth Inhibition (co-author, CANCER RESEARCH 56: 3540-3345, 1996) Tumor-selective somatostatin analog (TT-232) with strong in vitro and in vivo antitumor activity (co-author, PNAS 93: 12513-12518, 1996 The antitumor somatostatin analogue TT-232 induces cell cycle arrest through PKCdelta and c-Src (co-author, BIOCHEM. BIOPHYS. RES. COM.
== Clinical significance == If certain bones of the skull grow too fast then premature fusion of the sutures, craniosynostosis, may occur. This can result in skull deformities. These deformities include:
Sources: en.wikipedia.org
A new class of gene targeting MR contrast agents has been introduced to show gene action of unique mRNA and gene transcription factor proteins. These new contrast agents can trace cells with unique mRNA, microRNA and virus; tissue response to inflammation in living brains. The MR reports change in gene expression with positive correlation to TaqMan analysis, optical and electron microscopy.
== Function == Peptide deformylase removes the formyl group from the N terminus of nascent polypeptides as they are synthesized by the ribosome. The function of peptide deformylase can be described by the following equation, where formyl-L-methionyl peptide and water react under the formation of formate and methionyl peptide:
African histoplasmosis Alternariosis Antibiotic candidiasis (iatrogenic candidiasis) Black piedra Candidal intertrigo Candidal onychomycosis Candidal paronychia Candidal vulvovaginitis Candidid Chromoblastomycosis (chromomycosis, cladosporiosis, Fonseca's disease, Pedroso's disease, phaeosporotrichosis, verrucous dermatitis) Chronic mucocutaneous candidiasis Coccidioidomycosis (California disease, desert rheumatism, San Joaquin Valley fever, valley fever) Congenital cutaneous candidiasis Cryptococcosis Dermatophytid Diaper candidiasis Disseminated coccidioidomycosis (coccidioidal granuloma) Distal subungual onychomycosis Entomophthoromycosis Erosio interdigitalis blastomycetica Favus Fungal folliculitis (majocchi granuloma) Fusariosis Geotrichosis Granuloma gluteale infantum Histoplasmosis (cave disease, Darling's disease, Ohio Valley disease, reticuloendotheliosis) Hyalohyphomycosis Kerion Lobomycosis (keloidal blastomycosis, lacaziosis, Lobo's disease) Mucormycosis Mycetoma (Madura foot, maduromycosis) North American blastomycosis (blastomycetic dermatitis, blastomycosis, Gilchrist's disease) Onychomycosis (dermatophytic onychomycosis, ringworm of the nail, tinea unguium) Oral candidiasis (thrush) Otomycosis Perianal candidiasis Perlèche (angular cheilitis) Phaeohyphomycosis Piedra (trichosporosis) Pityrosporum folliculitis Primary cutaneous aspergillosis Primary cutaneous coccidioidomycosis Primary cutaneous histoplasmosis Primary pulmonary coccidioidomycosis Primary pulmonary histoplasmosis Progressive disseminated histoplasmosis Proximal subungual onychomycosis Rhinosporidiosis South American blastomycosis (Brazilian blastomycosis, paracoccidioidal granuloma, paracoccidioidomycosis) Sporotrichosis (rose-gardener's disease) Systemic candidiasis Tinea barbae (barber's itch, ringworm of the beard, tinea sycosis) Tinea capitis (herpes tonsurans, ringworm of the hair, ringworm of the scalp, scalp ringworm, tinea tonsurans) Tinea corporis (ringworm, tinea circinata, tinea glabrosa) Tinea corporis gladiatorum Tinea cruris (crotch itch, eczema marginatum, gym itch, jock itch, ringworm of the groin) Tinea faciei Tinea imbricata (tokelau) Tinea incognito Tinea manuum Tinea nigra (superficial phaeohyphomycosis, tinea nigra palmaris et plantaris) Tinea pedis (athlete's foot, ringworm of the foot) Tinea versicolor (dermatomycosis furfuracea, pityriasis versicolor, tinea flava) Trichophyton mentagrophytes VII (TMVII) (an emerging sexually transmitted tinea of the genitals, buttocks, face, trunk, and extremities) White piedra White superficial onychomycosis Zygomycosis (phycomycosis)
Before it was widely banned, it saw limited use in psychotherapy. In 2017 the United States Food and Drug Administration (FDA) granted breakthrough therapy designation for MDMA-assisted psychotherapy for post-traumatic stress disorder (PTSD). MDMA has limited approved medical uses in a small number of countries, but is illegal in most jurisdictions. Canada has allowed limited distribution of MDMA upon application to and approval by Health Canada. In Australia, it may be prescribed in the treatment of PTSD by specifically authorised psychiatrists. Fourteen systematic reviews of up to 353 participants suggest MDMA-assisted psychotherapy may substantially improve PTSD symptoms, response, and remission rates compared to psychotherapy alone, but the evidence is low to very low certainty and safety data are limited, with some increased transient adverse events. Some researchers have proposed that psychedelics in general may act as active "super placebos" used for therapeutic purposes.
Sources: en.wikipedia.org
It targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not act primarily on androgen receptors. This distinction separates it from SARMs.
Rodent studies found dose-dependent tumors in several organs. The sponsor discontinued the program over cancer concerns. Human risk from long-term use remains unknown.
Controlled human endurance trials are lacking. Animal studies show increased exercise capacity under some conditions. Anecdotal reports are not equivalent to clinical evidence.
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.