The present invention provides a method and composition for elevating the therapeutic efficacy of therapeutic agents by enhancing target cells uptake of the therapeutic agents, wherein the composition contains regulator having caveolae/lipid rafts dependent endocytic pathways, wherein the therapeutic agents are such as antitumor drugs. The invention also relates to a composition comprising regulator that have caveolae/lipid rafts dependent endocytic pathways and therapeutic agents. The invention further relates to a method for screening regulator having lipid rafts-caveolae dependent endocytic pathways which could enhance the therapeutic efficacy of antitumor drugs.
