Conjugated C1 Esterase Inhibitor and Uses Thereof
AssigneeShire Human Genetic Therapies, Inc.
InventorsKevin Holmes, Angela Norton, Clark Pan
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Abstract
The present invention provides, among other things, a conjugated C1-INH for improved treatment of complement-mediated disorders, including hereditary angioedema (HAE). In some embodiments, a conjugated C1-INH provided by the present invention is a PEGylated C1-INH. In some embodiments, a conjugated C1-INH provided by the present invention is a polysialic acid (PSA) conjugated C1-INH.
Claims33
A composition comprising a conjugated C1 esterase inhibitor (C1-INH) comprising:
- a C1-INH protein comprising at least one glycan residue;
- and
- at least one polyethylene glycol (PEG) moiety,
- wherein the at least one polyethylene glycol (PEG) moiety is covalently linked to the at least one glycan residue.
A composition comprising a conjugated C1 esterase inhibitor (C1-INH) comprising:
- a C1-INH protein comprising at least one polyethylene glycol (PEG) moiety;
- and
- wherein the at least one PEG moiety is covalently linked to the C1-INH protein via an oxime linkage.
3-6. (canceled)
9-22. (canceled)
24-27. (canceled)
A method of producing a conjugated C1 esterase inhibitor (C1-INH), said method comprising steps of:
- providing a C1-INH protein comprising at least one glycan residue and/or at least one amine group;
- and
- providing a PEG moiety under conditions that permit the PEG moiety reacts with the at least one glycan residue and/or the at least one amine group to form a linkage, thereby producing the conjugated C1-INH.
31-48. (canceled)
(canceled)
A composition comprising a conjugated C1 esterase inhibitor (C1-INH) comprising:
- a C1-INH protein comprising at least one glycan residue;
- at least one polysialic acid (PSA) moiety,
- wherein the at least one polysialic acid (PSA) moiety is covalently linked to the at least one glycan residue.
A composition comprising a conjugated C1 esterase inhibitor (C1-INH) comprising
- a C1-INH protein comprising at least one glycan residue;
- and
- at least one polysialic acid (PSA) moiety,
- wherein the at least one polysialic acid (PSA) moiety is covalently linked to the C1-INH protein via an oxime linkage or a hydrazone linkage.
53-57. (canceled)
59-73. (canceled)
76-78. (canceled)
A method of producing a conjugated C1 esterase inhibitor (C1-INH), said method comprising steps of:
- providing a C1-INH protein comprising at least one glycan residue and/or at least one amine group;
- and
- providing a polysialic acid (PSA) moiety under conditions that permit the PSA moiety to react with the at least one glycan residue and/or the at least one amine group to form a linkage, thereby producing the conjugated C1-INH.
81-85. (canceled)
87-89. (canceled)
91-92. (canceled)
94-95. (canceled)
97-99. (canceled)
Dependencies are inferred from the claim text.