| 摘要 |
The present invention generally relates to antigen-specific immunoconjugates for selectively delivering effector moieties that influence cellular activity. More specifically, the invention provides novel immunoconjugates comprising a first antigen binding moiety, an Fc domain and a single effector moiety. In addition, the present invention relates to polynucleotides encoding such immunoconjugates, and vectors and host cells comprising such polynucleotides. The invention further relates to methods for producing the immunoconjugates of the invention, and to methods of using these immunoconjugates in the treatment of disease. |
| 主权项 |
1. An immunoconjugate comprising (i) an immunoglobulin molecule comprising a first and a second antigen binding Fab molecule, an Fc domain consisting of two subunits, and (ii) an effector moiety, wherein not more than one effector moiety is present; and wherein
said first and said second Fab molecule are directed to CEA and comprise a heavy chain variable region sequence that is at least about 95%, 96%, 97%, 98%, 99% or 100% identical to the sequence of SEQ ID NO: 191, and a light chain variable region sequence that is at least about 95%, 96%, 97%, 98%, 99% or 100% identical to the sequence of SEQ ID NO: 189; and said effector moiety is a mutant human interleukin-2 (IL-2) polypeptide comprising the amino acid substitutions F42A, Y45A, L72G, wherein numbering of the amino acid positions is relative to the human IL-2 sequence in SEQ ID NO: 2. |
