In this work, we designed cathepsin B‐activatable prodrugs of the VEGFR inhibitor sunitinib, since studies suggested a role of cathepsin B in inducing angiogenesis.6,18, 19, 20 This would offer the possibility of targeting tumor sites which comprise high levels of both: cathepsin B and VEGFR. The gene discussed is KDR; the disease is neoplasm.