The invention provides a protected anti-neoplastic agent of the formula Hyp-N, wherein N is an anti-neoplastic agent and a protectable hydroxyl group of the anti-neoplastic is substituted with Hyp; Hyp is a moiety having the formula:whereinR2 is hydrogen;R3 is hydrogen or C1-C6 alkyl;R1 is C1-C6 alkyl or C1-C6 alkoxy, optionally substituted with one or more heteroatom-containing groups; andR4 is hydrogen, C1-C6 alkyl, or C1-C6 alkoxy, optionally substituted with one or more heteroatom-containing groups.