The invention describes vitamin receptor binding drug delivery conjugates and preparation method thereof.This drug delivery conjugates is made up of vitamin receptor bound fraction, bivalence joint (L) and medicine.The vitamin receptor bound fraction be vitamin or its vitamin receptor in conjunction with analog or derivant, medicine comprises its analog or derivant.The vitamin receptor bound fraction is covalently bound to the bivalence joint, and medicine or its analog or derivant are covalently bound to the bivalence joint, wherein bivalence joint (L) but comprise one or more spacer nipple releasing-joints and hetero atom joint.The method and the pharmaceutical composition that utilize this drug delivery conjugates to eliminate pathogenic cell colony have also been described.
