Epimers and isomers of tetrazole-containing rapamycin analogs are immunomodulatory agents and are useful in the treatment of restenosis and immune and autoimmune diseases. Also disclosed are cancer-, fungal growth-, restenosis-, post-transplant tissue rejection- and immune- and autoimmune disease-inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosis, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. It is preferred to use a combination of native rapamycin and its tetrazole containing isomers and epimers. One particular preferred application of such a combination of rapamycin and its tetrazole containing isomers and epimers is in medicated devices and local vascular delivery wherein the stability and lipid solubility and subsequently diffusion through tissue and cell membranes of the tetrazole isomers and epimers are essential to the success of the combined rapamycin formulation.