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US 2019/0338045 A1Published application
Monomethylvaline compounds capable of conjugation to ligands
AssigneeSeattle Genetics, Inc.
InventorsSvetlana O. DORONINA, Peter D. SENTER, Brian E. TOKI, Toni Beth KLINE
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Abstract
Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.
Claims29
An antibody-drug conjugate having the formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- Ab is an antibody,
- S is sulfur,
- each W is independently an Amino Acid unit,
- w is an integer ranging from 0 to 12,
- Y is a Spacer unit,
- y is 0, 1 or 2,
- D is a drug moiety, and
- p ranges from 1 to about 20, and
- wherein the antibody is attached to the drug linker compound through a cysteine residue of the antibody as denoted in the above formula.
7 more elements
Dependencies are inferred from the claim text.