Cardarine was created in 1992 by Ligand Pharmaceuticals and GlaxoSmithKline (GSK) as a metabolic agent for cancer, obesity, and cardiovascular disease. Phase 1 trials began in 2000 for hyperlipidemia, followed by phase I/II in 2002. The development of cardarine was stopped in 2007 due to safety concerns when preclinical toxicology showed it caused various cancers.