CPC C07K 16/28 (2013.01) [A61K 47/55 (2017.08); A61K 47/65 (2017.08); A61K 47/6801 (2017.08); C07K 16/18 (2013.01)] | 21 Claims |
1. A method of preparing a dual-drug conjugate, the method comprising conjugating a first moiety comprising D1 to a lysine side chain of A and conjugating a second moiety comprising D2 to cysteine side chains of A, thereby producing a dual-drug conjugate which is a compound of Formula I
![]() or a pharmaceutically acceptable salt thereof,
wherein:
A is an antibody or antigen-binding antibody fragment;
D1 is an active agent;
each L1 is independently a linker comprising at least one N (nitrogen) atom;
the nitrogen between the antibody or antigen-binding antibody fragment and the carbonyl of C(O)-L1-D1 is the nitrogen of a Lys side chain of the antibody or antigen-binding antibody fragment;
D2 an active agent, wherein D1 and D2 are different active agents;
each L2 is independently a linker;
the E-component is selected from the group consisting of
![]() L3 is —(CH2)—;
L4 is —(CH2)—;
m is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10; and
n is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.
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