Cardarine GW501516 — a PPAR-δ agonist that is not a SARM
Cardarine (GW501516, endurobol) activates peroxisome proliferator–activated receptor delta. It is not a selective androgen receptor modulator. Clinical development for dyslipidemia reached Phase 2 (including NCT00158899 for low HDL) and was abandoned amid rodent carcinogenicity concerns in the development history. Endurance “exercise mimetic” phenotypes in mice (Narkar et al., 2008) and USADA athlete advisories explain why it shares retail shelves with SARMs. This monograph exists to correct that identity error with primary and high-quality secondary records from the 5 August 2026 harvest. It recommends no human use.
01 Names and target
GW501516 is a selective PPAR‑δ (PPARD) agonist developed by
GlaxoSmithKline / Ligand for dyslipidemia (contemporary development note PMID
16625823). Community names include Cardarine and endurobol. It does not bind the
androgen receptor as its primary mechanism and must never be filed as a SARM in
identity tables. PubMed open counts for GW501516 OR cardarine are
large because PPAR biology is a broad field; compound-specific clinical packages
are much smaller.
02 Exercise-mimetic preclinical signal
Narkar et al. (2008) showed that a PPAR‑β/δ agonist and exercise training synergistically increased oxidative myofibers and running endurance in adult mice, and explored AMPK agonism (AICAR) in related designs (PMID 18674809). That paper is the scientific root of the “exercise mimetic” slogan. It is a mouse endurance phenotype, not a human sports medicine approval, and not an AR-SARM result.
03 NCT00158899 and dyslipidemia programmes
ClinicalTrials.gov NCT00158899 evaluated GW501516 versus fenofibrate and placebo in subjects with low HDL cholesterol in a multi-centre, randomised, double-blind proof-of-concept and dose-response Phase 2 design. The registry API harvest lists status COMPLETED. The brief purpose was to compare safety, tolerability, and effect on raising HDL-c versus placebo. That registry fact is not a modern efficacy endorsement; development did not proceed to an approved medicine.
04 Carcinogenicity and programme stop
Public secondary and review sources in the harvest — including USADA athlete advisory language and PPAR‑δ development commentaries — state that clinical development was halted after rodent carcinogenicity findings in long-term toxicology. This monograph treats that stop as the governing programme fact. It does not invent tumour incidence tables that were not in the admitted primary package at harvest; readers needing raw tox tables must go to regulatory/toxicology primary sources when available.
05 Anti-doping adjacency
USADA’s public advisory “What Should Tested Athletes Know About GW1516?” (Camoufox harvest) exists because athletes encounter the compound in the same illicit marketplace as SARMs. WADA prohibition and athlete education are regulatory facts. Hair and urine detection papers (e.g. PMID 32298044) confirm analytical interest.
06 Absences
No approved human indication exists. Modern randomised endurance trials in athletes with pharmaceutical material are not the backbone of this document. Forum dosing lore is refused. Calling Cardarine a SARM is an identity error this series exists to stop.
07 Reading order
The SARMs class monograph includes Cardarine only to name the shelf error. This compound monograph is the PPAR‑δ record. Sibling AR-SARM monographs do not inherit Cardarine’s carcinogenicity narrative as if it were an AR finding.
08 Harvest literature map
Deep-harvest strata for Cardarine: (1) PPAR‑δ / exercise-mimetic
preclinical core (PMID 18674809); (2) historical dyslipidemia Phase 2
registry residue including NCT00158899; (3) programme-stop / rodent
carcinogenicity narrative in secondary and athlete-advisory sources; (4) doping
detection (hair/urine). PubMed open count for GW501516 OR cardarine
is large because PPAR biology is broad; compound-specific clinical packages are
not. Polymorph chemistry papers (PMID 38794285) are materials science, not
efficacy. Steatohepatitis PPAR agonist papers are target-class biology, not
Cardarine approvals.
How this document was assembled
Commissioned 5 August 2026 in the Adjacent Compounds / SARMs group
and rewritten the same day after a deep research-API harvest (Tavily, Exa,
PubMed E-utilities, ClinicalTrials.gov API v2, Camoufox for selected primary
pages). Artefacts live under
projects/adjacent_compounds_research_2026/deep_harvest/.
HOUSE_STYLE governs presentation. PubMed-indexed references are NCBI-resolved.
Evidence handling
Study type is named in the reporting sentence. Animal and in-vitro results are not phrased as human outcomes. Sponsor press is secondary until peer-reviewed full text is admitted. Consumer case reports are grey-market exposure literature unless product analytics accompany the report. Cardarine is never called a SARM.
References
- Kintz P, Ameline A, Gheddar L, Raul JS. Testing for GW501516 (cardarine) in human hair using LC/MS-MS and confirmation by LC/HRMS. Drug Test Anal. 2020;12(7):980-986.
PMID 32298044 · doi:10.1002/dta.2802 - Lefere S, Puengel T, Hundertmark J, Penners C, Frank AK, Guillot A, et al.. Differential effects of selective- and pan-PPAR agonists on experimental steatohepatitis and hepatic macrophages(☆). J Hepatol. 2020;73(4):757-770.
PMID 32360434 · doi:10.1016/j.jhep.2020.04.025 - Narkar VA, Downes M, Yu RT, Embler E, Wang YX, Banayo E, et al.. AMPK and PPARdelta agonists are exercise mimetics. Cell. 2008;134(3):405-15.
PMID 18674809 · doi:10.1016/j.cell.2008.06.051 · PMC2706130 - Pelton P. GW-501516 GlaxoSmithKline/Ligand. Curr Opin Investig Drugs. 2006;7(4):360-70.
PMID 16625823 - Solomon ZJ, Mirabal JR, Mazur DJ, Kohn TP, Lipshultz LI, Pastuszak AW. Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications. Sex Med Rev. 2019;7(1):84-94.
PMID 30503797 · doi:10.1016/j.sxmr.2018.09.006 · PMC6326857 - Turza A, Pascuta P, Muresan-Pop M, Mare L, Borodi G, Popescu V. Five Novel Polymorphs of Cardarine/GW501516 and Their Characterization by X-ray Diffraction, Computational Methods, Thermal Analysis and a Pharmaceutical Perspective. Pharmaceutics. 2024;16(5).
PMID 38794285 · doi:10.3390/pharmaceutics16050623 · PMC11125426 - U.S. Anti-Doping Agency. What Should Tested Athletes Know About GW1516?
https://www.usada.org/spirit-of-sport/what-should-athletes-know-gw1516 - ClinicalTrials.gov. NCT00158899 — GW501516 in low HDL-c. Protocol inventory.
https://clinicaltrials.gov/study/NCT00158899 - U.S. Food and Drug Administration. Consumer updates and warning letters on body-building products containing SARMs. Regulatory context.
https://www.fda.gov/ - World Anti-Doping Agency. Prohibited List — S1 Anabolic Agents (selective androgen receptor modulators).
https://www.wada-ama.org/ - NIDDK LiverTox. Selective Androgen Receptor Modulators (SARMs). NCBI Bookshelf NBK619971.
https://www.ncbi.nlm.nih.gov/books/NBK619971/ - ClinicalTrials.gov. Protocol inventory via API v2; not peer-reviewed results.
https://clinicaltrials.gov/ - PubChem compound summary pages used for identity cross-checks.
https://pubchem.ncbi.nlm.nih.gov/
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