Reactive oxygen species-mediated prodrug cleavage (ROS-mediated prodrug cleavage)

Reactive oxygen species-mediated prodrug cleavage is a drug delivery and activation mechanism in which a chemical linker is engineered into a prodrug so that it is stable under normal conditions but selectively cleaved in the presence of elevated ROS. This strategy exploits the higher ROS levels found in diseased tissues (such as tumors and sites of ischemic injury) to release the active drug specifically at the target site, thereby improving therapy selectivity and reducing systemic toxicity. ROS-cleavable linkers commonly include thioketal, boronate ester, or amino acid residues susceptible to oxidation. This mechanism does not represent a molecular target itself but a stimulus-responsive system for therapeutic drug release[1][2][5].

Other names

ROS-triggered prodrug activationROS-responsive linker cleavageoxidative prodrug activation

Prodrug remains inactive until exposed to pathological levels of ROS, which cleave the linker, releasing the active drug at the site of elevated ROS[1][2][5]