Ole Tietz

Trans‐blood–brain barrier (BBB) delivery of therapeutic and diagnostic agents is a major challenge in the development of central nervous system (CNS) targeted radiopharmaceuticals. This review is an introduction to the use of peptides as delivery agents to transport cargos into the CNS. The most widely used BBB‐penetrating peptides are reviewed here, with a particular emphasis on the broad range of cargos delivered into the CNS using these. Cell‐penetrating peptides (CPPs) have been deployed as trans‐BBB delivery agents for some time; new developments in the CPP field offer exciting opportunities for the design of next generation trans‐BBB complexes. Many of the peptides highlighted here are ready to be combined with diagnostic and therapeutic radiopharmaceuticals to develop highly effective CNS‐targeted agents.