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US 2013/0280282 A1Published application
Dr5 ligand drug conjugates
AssigneesDaiichi Sankyo Company, Limited, Seattle Genetics, Inc.
InventorsToshiaki Ohtsuka, Kimihisa Ichikawa, Ayumi Yada
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Abstract
Ligand Drug Conjugates are provided having a DR5 binding moiety attached via linking groups and/or spacers to a therapeutic agent that are effective in treatment of various cancers.
Claims22
A ligand drug conjugate having the formula:
- L-(LU-D)p (I)
- or a pharmaceutically acceptable salt thereof, having specificity for target cells expressing DR5, wherein:
- L is a Ligand unit which is an anti-DR5 antibody comprising (a) a heavy chain immunoglobulin having the CDR1 consisting of amino residues 1-5 of SEQ ID NO:11, the CDR2 consisting of amino acid residues 1-17 of SEQ ID NO:12, and the CDR3 consisting of amino acid residues 1-13 of SEQ ID NO:13;
- and (b) a light chain immunoglobulin having the CDR1 consisting of amino residues 1-16 of SEQ ID NO:14, the CDR2 consisting of amino acid residues 1-7 of SEQ ID NO:15, and the CDR3 consisting of amino acid residues 1-9 of SEQ ID NO:16;
- and
- (LU-D) is a Linker unit-Drug unit moiety, wherein
- LU is a Linker unit, and
- D is a Drug unit, wherein the Drug unit is an auristatin;
- and
- the subscript p is an integer of from 1 to 20.
7 more elements
Dependencies are inferred from the claim text.