A Pretargeting Strategy Enabled by Bioorthogonal Reactions Towards Advanced Nuclear Medicines: Application and Perspective

Pretargeting is an innovative and promising approach in nuclear medicine for targeted-imaging/therapy through the following bioorthogonal reactions.It requires two reactive participants,one of which is a targeting vector and the other is a small radiolabeled probe capable of specifically coupling through bioorthogonal reactions with the targeting vector accumulated in the disease site.Compared to the conventional direct targeting approach,such a two-step scheme conceptually can achieve a higher imaging contrast and an improved therapeutic effect owing to the suppressed non-specific targeting.In this review,we will first give a brief introduction on pretargeting systems and the history of bioorthogonal reactions,and then focus on some important works about radionuclide delivering through the bioorthogonal reaction based pretargeting strategy.Finally,we will discuss the steps forward in respect to the future clinical translation and truly hope that this methodology would continue to make contributions to nuclear medicines.