Figure 1. ‘Click and Clear' strategy.

Biological inactivation and fast clearance of a circulating drug, Warfarin-N₃ 2, by in vivo Strain Promoted Alkyne Azide Cycloaddition (SPAAC) reaction. A mouse submitted to anticoagulant therapy (WN₃, 2) is treated with a clearing agent (BCN-peg₆-OH, 9) prone to react with the anticoagulant drug. In vivo bio-orthogonal reaction between circulating WN₃ 2 and BCN-peg₆-OH 9 leads to the formation of an inactivated compound 10 which is readily cleared from the bloodstream, restoring normal coagulation activity. The pictures of mice and syringe have been downloaded from Servier Medical Art Database which provides these illustrations through the Creative Commons license (https://creativecommons.org/licenses/by/3.0/).