One approach to improving the activity of anticancer drugs is to bind them to the human α-fetoprotein (HAFP) that recognizes the tumor-associated cell-surface HAFP receptor. A drug can be bound to the HAFP by covalent conjugation or within a non-covalent complex. Specially designed linkers couple cytotoxins to the HAFP and ensure the stability of the HAFP-drug conjugate in the circulation and the activation of the drug in the cancer cell. On the other hand, AFP-drug non-covalent complexes can exploit the natural role of the AFP as a nutrition delivery "shuttle". In this article we review the design of HAFP-drug conjugates and AFP-drug complexes and their potential uses.