| abstract |
The present invention provides tetrazole-containing rapamycin analogs and 42-epirapamycin analogs that possess different polarities across the compounds that can exhibit different stability and solubility characteristics in the formulation. Epimers and isomers of tetrazole-containing rapamycin analogs are immunomodulators and are useful in the treatment of restenosis, immune and autoimmune diseases. Also disclosed are compositions that inhibit cancer, fungal growth, restenosis, tissue rejection after transplantation, and immune and autoimmune diseases in mammals, and methods for inhibiting these diseases. It is preferred to use a blend of natural rapamycin and its tetrazole-containing isomers and epimers. Particularly preferred applications of such formulations are medical devices and local vascular delivery, where the stability and lipid solubility of the tetrazole isomers and epimers, and subsequent diffusion across tissues and cell membranes, are formulated rapamycin formulations Essential to the success of. [Selection] Figure 2 |