The first drugtamer‐PROTAC conjugate, which enhances tumor targeting and efficacy in vivo while reducing side effects, is developed by linking a nucleolin‐specific aptamer with nicotinamide phosphoribosyltransferase (NAMPT) PROTAC and fluorouridine nucleotides through a drug‐constituted DNA‐like oligomer (drugtamer) and a tumor microenvironment‐responsive linker. This evidence concerns the gene NAMPT and neoplasm.