Antibody fragment-peg conjugates
First Claim
Patent Images
1. A conjugate comprising a humanized antibody Fab′
- fragment further comprising an antigen binding site,wherein said antigen binding site (a) binds to human interleukin-8 (IL-8), and (b) comprises the complementarity determining regions of (i) 6G4V11N35A light chain (FIG. 36, SEQ ID NO;
56) or (ii) the 6G4V11N35E light chain (FIG. 45, SEQ ID NO;
62), wherein said humanized antibody Fab′
fragment is covalently attached to a polyethylene glycol (PEG) molecule having an average molecular weight of at least 20 kD, and wherein the apparent size of the conjugate is at least about 500 kD, and at least about 8 fold greater than the apparent size of the antibody fragment.
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Abstract
Humanized anti-IL-8 monoclonal antibodies and variants thereof are described for use in diagnostic applications and in the treatment of inflammatory disorders. Also described is a conjugate formed by an antibody fragment covalently attached to a non-proteinaceous polymer, wherein the apparent size of the conjugate is at least about 500 kD. The conjugate exhibits substantially improved half-life, mean residence time, and/or clearance rate in circulation as compared to the underivatized parental antibody fragment.
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Citations
15 Claims
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1. A conjugate comprising a humanized antibody Fab′
- fragment further comprising an antigen binding site,
wherein said antigen binding site (a) binds to human interleukin-8 (IL-8), and (b) comprises the complementarity determining regions of (i) 6G4V11N35A light chain ( FIG. 36 , SEQ ID NO;
56) or (ii) the 6G4V11N35E light chain (FIG. 45 , SEQ ID NO;
62),wherein said humanized antibody Fab′
fragment is covalently attached to a polyethylene glycol (PEG) molecule having an average molecular weight of at least 20 kD, andwherein the apparent size of the conjugate is at least about 500 kD, and at least about 8 fold greater than the apparent size of the antibody fragment. - View Dependent Claims (2, 3, 4, 5, 6, 9, 10, 11, 12, 13, 14, 15)
- fragment further comprising an antigen binding site,
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7. A conjugate comprising a humanized antibody Fab′
- fragment,
wherein said antibody fragment;
(a) binds to human interleukin 8 (IL-8);
(b) comprises the complementarity determining regions of (i) 6G4V11N35A light chain (FIG. 36 , SEQ ID NO;
56) or (ii) 6G4V11N35E light chain (FIG. 45 , SEQ ID NO;
62), and (c) is covalently attached to a single polyethylene glycol (PEG) molecule of at least 20 kD, andwherein said conjugate has an apparent size of at least about 500 kD and at least about 8 fold greater than the apparent size of the antibody fragment.
- fragment,
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8. A conjugate comprising a humanized antibody Fab′
- fragment,
wherein said antibody fragment;
(a) binds to human interleukin 8 (IL-8);
(b) comprises the complementarity determining regions of (i) 6G4V11N35A light chain (FIG. 36 , SEQ ID NO;
56) or (ii) 6G4V11N35E light chain (FIG. 45 , SEQ ID NO;
62), and (c) is covalently attached to a polyethylene glycol (PEG) molecule having an average molecular weight of at least about 40 kD,wherein the apparent size of the conjugate is at least about 500 kD, and at least about 8 fold greater than the apparent size of the antibody fragment.
- fragment,
Specification