Rapamycin (also named sirolimus, Wyeth) and other rapalogues including temsirolimus (CCI-779, Wyeth), everolimus (RAD001, Novartis Pharmaceutical), and deforolimus (AP23573, Ariad Pharmaceutical) are macrocyclic lactones acting as anticancer agents that target mTOR in several human cancers in vitro and in vivo. The main differences between rapalogues lie in changes in chemical properties in terms of drug solubility and metabolism. This evidence concerns the gene MTOR and cancer.