The present invention relates to amphiphilic drug-oligomer conjugates capable
of traversing the blood-brain barrier ("BBB") and to methods of making and using
such conjugates. An amphiphilic drug-oligomer conjugates comprise a therapeutic
compound conjugated to an oligomer, wherein the oligomer comprises a lipophilic
moiety coupled to a hydrophilic moiety. The conjugates of the invention further
comprise therapeutic agents such as proteins, peptides, nucleosides, nucleotides,
antiviral agents, antineoplastic agents, antibiotics, etc., and prodrugs, precursors,
derivatives and intermediates thereof, chemically coupled to amphiphilic oligomers.