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Gw53.0

Cardarine (GW501516) – Forschung

Überwiegend Mechanismus / Beobachtung

9 begutachtete Studien

Was die Evidenz sagt

Überwiegend Mechanismus / Beobachtung

Die meisten Studien zu Cardarine (GW501516) sind mechanistisch oder beobachtend statt RCTs, die einen klinischen Effekt messen — betrachte die Ergebnisse als vorläufig.

Die meiste Evidenz stammt aus mittelwertigen randomisierten Studien, veröffentlicht 2004–2019.

Basierend auf 9 Studien · 4 RCTs

Konfidenz

Mittlere Konfidenz

Nach Outcome

Cholesterol & lipids
Überwiegend Mechanismus / Beobachtung4 Studien
Endurance (preclinical)Der Ruf für Ausdauer beruht auf einer einzigen Laufband-Studie an Mäusen; keine Wirksamkeitsstudien am Menschen. Die Entwicklung wurde wegen Krebs an mehreren Organen bei Tieren eingestellt, und es ist von der WADA verboten. · Nicht etabliert (keine Wirksamkeitsdaten am Menschen)
Überwiegend Mechanismus / Beobachtung3 Studien
Safety profile
Zu wenige bewertete Studien2 Studien

Ältere Forschungsbasis

Neueste Studie von 2019

200420112019

1RCT2007

Sprecher DL, Massien C, Pearce G, Billin AN, Perlstein I, Willson TM · Arterioscler Thromb Vasc Biol (2007)

Quelle ansehen

2RCT2012

Olson EJ, Pearce GL, Jones NP, Sprecher DL · Arterioscler Thromb Vasc Biol (2012)

Quelle ansehen

3RCT2008

Risérus U, Sprecher D, Johnson T, Olson E, Hirschberg S, Liu A · Diabetes (2008)

Quelle ansehen

4RCT2011

Ooi EM, Watts GF, Sprecher DL, Chan DC, Barrett PH · J Clin Endocrinol Metab (2011)

Quelle ansehen

5Tierstudie2008

Einfach gesagt: PPARbeta/delta agonist and exercise training synergistically increase oxidative myofibers and running endurance in adult mice ... AMPK-PPARdelta pathway can be targeted by orally active drugs to enhance training adaptation or even to increase endurance without exercise.

Narkar VA, Downes M, Yu RT, Embler E, Wang YX, Banayo E, et al. · Cell (2008)

The foundational 'exercise mimetic' paper and the entire basis for cardarine's endurance reputation — but it is a MOUSE study
A PPARδ agonist combined with exercise training synergistically increased oxidative ('slow-twitch') myofibres and treadmill running endurance in mice
The AMPK agonist AICAR alone increased endurance ~44% even in sedentary mice, framing the AMPK–PPARδ axis as a druggable target

Quelle ansehen

6Übersicht2004

Einfach gesagt: PPARdelta is a key regulator of fatty acid catabolism and oxidative metabolism in skeletal muscle, positioning it as a target for the treatment of metabolic syndrome.

Luquet S, Lopez-Soriano J, Holst D, Gaudel C, Jehl-Pietri C, Fredenrich A, et al. · Biochimie (2004)

Mechanistic review of PPARδ as the master regulator of fatty-acid oxidation and oxidative-fibre metabolism in skeletal muscle
Explains the molecular rationale GW501516 exploits: PPARδ activation drives fatty-acid uptake and β-oxidation and an oxidative fibre-type shift
Frames PPARδ as a candidate target for metabolic syndrome — the original therapeutic hypothesis behind the compound

Quelle ansehen

7In vitro2010

Einfach gesagt: Since January 2009, the list of prohibited substances and methods of doping ... includes ... the PPAR-delta agonist GW1516, which is categorized as a gene doping substance.

Thevis M, Möller I, Thomas A, Beuck S, Rodchenkov G, Bornatsch W, et al. · Analytical and bioanalytical chemistry (2010)

Documents that GW501516 (GW1516) has been on the World Anti-Doping Agency prohibited list since January 2009 as a gene-doping agent
Characterised two major urinary metabolites (sulfoxide and sulfone) and implemented a validated LC-MS/MS urine assay for routine doping control (limit of detection 0.1 ng/ml)
Confirms cardarine is a banned doping substance with established detection in sport, not an approved therapeutic

Quelle ansehen

8Tierstudie2019

Einfach gesagt: GW501516 significantly enhanced colitis-associated colorectal cancer in AOM/DSS-induced mice.

Zhou D, Jin J, Liu Q, Shi J, Hou Y · European journal of pharmacology (2019)

Mandatory counter-evidence: the PPARδ agonist GW501516 itself significantly enhanced colitis-associated colorectal cancer in AOM/DSS-induced mice
GW501516 raised pro-inflammatory gene expression (COX-2, IL-6, IL-8, MCP-1) in inflamed colon and increased Glut1/SLC1A5 in colon cancer cells and tumours
Mechanistically links the compound's PPARδ activation to tumour promotion — coherent with the carcinogenicity that ended its development

Quelle ansehen

9In vitro2004

Einfach gesagt: These findings were confirmed with an additional high-affinity PPARdelta agonist, GW501516 ... activation of PPARdelta can result in increased growth in breast and prostate cancer cell lines.

Stephen RL, Gustafsson MC, Jarvis M, Tatoud R, Marshall BR, Knight D, et al. · Cancer research (2004)

Additional counter-evidence: the high-affinity PPARδ agonist GW501516 stimulated proliferation of human breast (T47D, MCF7) and prostate (LNCaP) cancer cell lines
GW501516 increased the proliferation marker Cdk2 and VEGFα/FLT-1, suggesting an autocrine proliferative and pro-angiogenic loop
Pro-proliferative effects extended to human endothelial cells, consistent with tumour angiogenesis

Quelle ansehen

In der Forschungsbibliothek ansehen

Cardarine (GW501516) – Forschung

Überwiegend Mechanismus / Beobachtung

Triglyceride:high-density lipoprotein cholesterol effects in healthy subjects administered a peroxisome proliferator activated receptor delta agonist.

Lipid effects of peroxisome proliferator-activated receptor-δ agonist GW501516 in subjects with low high-density lipoprotein cholesterol: characteristics of metabolic syndrome.

Activation of peroxisome proliferator-activated receptor (PPAR)delta promotes reversal of multiple metabolic abnormalities, reduces oxidative stress, and increases fatty acid oxidation in moderately obese men.

Mechanism of action of a peroxisome proliferator-activated receptor (PPAR)-delta agonist on lipoprotein metabolism in dyslipidemic subjects with central obesity.

AMPK and PPARdelta agonists are exercise mimetics.

Roles of peroxisome proliferator-activated receptor delta (PPARdelta) in the control of fatty acid catabolism. A new target for the treatment of metabolic syndrome.

Characterization of two major urinary metabolites of the PPARdelta-agonist GW1516 and implementation of the drug in routine doping controls.

PPARδ agonist enhances colitis-associated colorectal cancer.

Activation of peroxisome proliferator-activated receptor delta stimulates the proliferation of human breast and prostate cancer cell lines.