CARDARINE
PPAR-δ agonist that shifts fuel use from glucose to lipids, enhancing endurance and fat oxidation; development halted over cancer concerns.
GW501516 reached Phase II clinical trials for dyslipidemia and metabolic disorders but development was discontinued after long-term rodent studies demonstrated rapid development of multiple cancers across multiple organ systems. Animal models showed improved lipid profiles, insulin sensitivity, and exercise endurance. A published case report documented severe rhabdomyolysis and hepatotoxicity (ALT 922, AST 2558, CPK 86435) in a user combining cardarine with ostarine. WADA has prohibited GW501516 at all times since 2009 under metabolic modulators. No human efficacy or long-term safety data exist at performance-enhancing doses; all risk-benefit assumptions are extrapolated from preclinical studies.