SORT1-targeted docetaxel TH1902

A peptide-drug conjugate composed of the second-generation taxane docetaxel and the sortilin (SORT1)-targeting peptide TH19P01, with potential antineoplastic activity. Upon administration of SORT1-targeted docetaxel TH1902, the TH19P01 moiety targets and binds to SORT1 expressed on tumor cells. Upon internalization, docetaxel binds to and stabilizes the beta-tubulin subunit, thereby inhibiting microtubule disassembly which results in cell-cycle arrest at the G2/M phase and cell death. SORT1 is overexpressed in a variety of cancers and plays an important role in protein internalization, sorting and trafficking.