Anti-HER2 immunoconjugates, and uses thereof
The invention provides immunoconjugates of Formula I comprising an anti-HER2 antibody linked by conjugation to one or more 8-Het-2-aminobenzazepine derivatives. The invention also provides 8-Het-2-aminobenzazepine derivative intermediate compositions comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the immunoconjugates through a linker or linking moiety. The invention further provides methods of treating cancer with the immunoconjugates.
1 . An 8-Het-2-aminobenzazepine-linker compound of formula:
2 . An immunoconjugate comprising an antibody covalently attached to one or more 8-Het-2-aminobenzazepine moieties by a linker, and having formula:
or a pharmaceutically acceptable salt thereof, wherein Ab is an antibody and p is an integer from 1 to 8.
3 . A pharmaceutical composition comprising a therapeutically effective amount of an immunoconjugate according to claim 2 or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable diluents, vehicles, carriers, excipients, or a combination thereof.
4 . A method for treating cancer in a subject comprising administering to the subject a therapeutically effective amount of an immunoconjugate according to claim 2 or a pharmaceutically acceptable salt thereof.