Vitamin receptor binding drug delivery conjugates

Abstract

The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.

1 . A vitamin receptor binding drug delivery conjugate comprising:
 (a) a vitamin receptor binding moiety;   (b) a bivalent linker; and   (c) a drug, or an analog or derivative thereof;   wherein the vitamin receptor binding moiety is covalently linked to the bivalent linker;   the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker; and   the bivalent linker comprises one or more components selected from the group consisting of spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof;   providing that the bivalent linker includes at least one releasable linker that is not a disulfide.   
     
     
         2 - 63 . (canceled)