This invention discloses a type of click-type covalent
drug, its regionally selective
delivery system, and its applications. The invention comprises two parts: a click-type covalent
drug and a tumor regionally selective
delivery system. The click-type covalent
drug consists of three parts: an azacyclic
alkyne (DBCO), a
small molecule drug, and a
linker, having the structure of Formula 1. Optionally, the
small molecule drug is a
membrane protein inhibitor, an immunomodulator, or a chemotherapeutic drug. The click-type covalent drug reacts with
azide-labeled target cells via a click reaction, forming a
covalent bond that binds to the
cell membrane, increasing the local
drug concentration and prolonging the drug
retention time, thereby enhancing
selective inhibition of the target cells. The regionally selective
delivery system is co-assembled from an amphiphilic block
polymer and the click-type covalent drug for regionally selective delivery. This invention achieves
covalent binding to
azide-labeled
tumor cells through the click-type covalent drug, while having no effect on unlabeled normal cells, reducing toxic side effects on normal tissues.