Cardarine (GW501516) is a small molecule that switches on PPAR-delta, a receptor that controls how muscles burn fat. GlaxoSmithKline tested it in people for its effects on blood fats, then stopped development. It is not a peptide and is not approved for human use anywhere we could find.
Also known as: GW501516, GW1516, GW-501516.
There is no approved product. GSK's trials gave 2.5 or 10 mg once a day for 2 weeks to healthy volunteers (Sprecher 2007), 10 mg a day for 2 weeks to moderately overweight men (Risérus 2008), and 2.5, 5 or 10 mg a day for 12 weeks to 268 people with low HDL cholesterol (Olson 2012). Development was stopped after these trials. These are trial protocols, not personalized advice; confirm any dosing with your prescriber.
Cardarine is not approved. In 2013 WADA took the rare step of warning athletes about it, saying GW501516 was withdrawn from research and terminated by its developer when serious toxicities were found in preclinical studies, and that clinical approval has not and will not be given. The studies WADA pointed to are two 2009 GSK abstracts: in 2-year studies, rats and mice given GW501516 every day developed tumors in several organs, including the liver, stomach, bladder, thyroid, uterus and skin, at every dose tested (Geiger 2009; Newsholme 2009).
WADA bans PPAR-delta agonists, naming GW1516 (GW501516), banned in and out of competition under "metabolic modulators" (S4.4.1). When researchers tested 44 products sold online as SARMs (Van Wagoner 2017), some contained GW501516 instead of, or as well as, what the label said.
In the human trials, cardarine raised HDL cholesterol and lowered triglycerides and LDL: in the 12-week trial, HDL rose by up to 16.9% and triglycerides fell by 16.9% (Olson 2012). These trials lasted at most 12 weeks, too short to show whether the cancers seen in rodents happen in people.
The GSK trial summaries we read give no half-life or time to peak, so we do not list one.
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