TUBULYSIN COMPOUNDS AND CONJUGATES THEREOF

摘要

A tubulysin compound conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by Lp. Each occurrence of D is independently a tubulysin compound having a molecular weight < 5 kDa. LD and Lp are distinct linkers connecting the tubulysin compound and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-tubulysin compound-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.