abstract |
The present invention relates to antibody-drug conjugates (ADCs) in which a plurality of active agents are conjugated to antibodies via one or more branched linkers. The branched linker may comprise a branching unit, the two active agents are coupled to a branching unit via a second linker, and the branching unit is coupled to the antibody by a primary linker. The activators may be the same or different. In this particular embodiment, the two or more branched linkers are conjugated to an antibody, such as a 2-4 branched linker, each capable of binding to a different C-terminal cysteine of the heavy or light chain of the antibody. The branched linker may comprise a first branch comprising a polyethylene glycol unit coupled to a branching unit and an activator coupled to the branching unit through a second branch. In this particular embodiment, the two or more branched linkers are conjugated to an antibody, such as a 2-4 branched linker, each capable of binding to a different C-terminal cysteine of the heavy or light chain of the antibody. |