In addition to integrins, interleukin‐13 receptor α2 (IL‐13Rα2), and neuropilin1 (NRP1), overexpressed in glioma cells (U87MG), have provided attractive targeting sites for improving drug accumulation.[109] However, delivery of the prodrug into glioblastoma always has to consider the drug resistance attributed to the activation of drug efflux transporters such as P‐glycoprotein (P‐gp).[108]The rational design of prodrug systems that covalently conjugate fluorophores and these targeting ligands enables their accumulation and drug release to glioma tumor cells (Table 5). Here, NRP1 is linked to glioblastoma.