CPC C07K 16/2863 (2013.01) [A61K 47/68031 (2023.08); A61K 47/68035 (2023.08); A61K 47/6849 (2017.08); A61P 35/00 (2018.01); C07K 16/32 (2013.01); A61K 38/00 (2013.01); A61K 2039/505 (2013.01); C07K 2317/52 (2013.01); C07K 2317/73 (2013.01); C07K 2317/77 (2013.01); C07K 2317/94 (2013.01)] | 10 Claims |
1. An antibody-drug conjugate, wherein the antibody-drug conjugate comprises:
(a) a heavy chain variable domain and a light chain variable domain selected from the group of:
(i) SEQ ID NO: 5 and SEQ ID NO: 6, respectively;
(ii) SEQ ID NO: 11 and SEQ ID NO: 12, respectively;
(iii) SEQ ID NO: 13 and SEQ ID NO: 14, respectively;
(iv) SEQ ID NO: 15 and SEQ ID NO: 16, respectively;
(v) SEQ ID NO: 17 and SEQ ID NO: 18, respectively; and
(vi) SEQ ID NO: 21 and SEQ ID NO: 22, respectively;
(b) a light chain constant region sequence of SEQ ID NO: 157 comprising a valine to cysteine substitution at amino acid position 98, wherein the drug is monomethyl auristatin E (MMAE) and the MMAE is conjugated to the cysteine at amino acid position 98 via a valine-citrulline (vc) linker; and
(c) a heavy chain CH1-CH2-CH3 sequence of SEQ ID NO: 155 or SEQ ID NO: 189 optionally comprising one or more of (A) through (C):
(A) a lysine to cysteine substitution at amino acid position 105 and deletion of a threonine at amino acid positions 106 and 108;
(B) a methionine to tyrosine substitution at amino acid position 135, a serine to threonine substitution at amino acid position 137, and a threonine to glutamic acid substitution at amino acid position 139; and
(C) a methionine to leucine substitution at amino acid position 311 and an asparagine to serine substitution at amino acid position 317.
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