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US 11,077,195 B2Granted
IL-2 conjugates and methods of use thereof
AssigneeSynthorx, Inc.
InventorsJerod Ptacin, Carolina E. Caffaro, Marcos Milla
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Abstract
Disclosed herein are compositions, kits, and methods comprising interleukin (IL) conjugates (e.g., IL-2 conjugates) useful for the treatment of one or more indications. Also described herein are pharmaceutical compositions and kits comprising one or more of the interleukin conjugates (e.g., IL-2 conjugates).
Claims33
An IL-2 conjugate comprising:
- an IL-2 polypeptide comprising a substituted lysine comprising an axidoethoxy moiety covalently attached to a conjugating moiety comprising a polyethylene glycol (PEG), wherein:
- the IL-2 polypeptide comprises an amino acid sequence having at least 80% sequence identity to SEQ ID NO:
- 1;
- and
- the substituted lysine substitutes for an amino acid at position K35, F42, F44, K43, E62, P65, R38, T41, E68, Y45, V69, or L72 in reference to the amino acid positions within SEQ ID NO:
- 1.
3 more elements
An IL-2 conjugate comprising the amino acid sequence of SEQ ID NO:
- 50, wherein [AzK_L1_PEG30 kD] is an L-amino acid having the structure of Formula (XVI) or Formula (XVII):
- wherein:
- m is 2;
- n is an integer such that —(OCH2CH2)n—OCH3 has a molecular weight of about 30 kDa;
- and
- the wavy lines indicate covalent bonds to amino acid residues within SEQ ID NO:
- 50 that are not replaced.
4 more elements
An IL-2 conjugate comprising the amino acid sequence of SEQ ID NO:
- 3, wherein at least one amino acid at position K34, F41, F43, K42, E61, P64, R37, T40, E67, Y44, V68, or L71 is replaced by the structure of Formula (I):
- wherein:
- Z is CH2 and Y is
- Y is CH2 and Z is
- Z is CH2 and Y is
- or
- Y is CH2 and Z is
- W is a PEG group having a molecular weight of about 5 kDa, 10 kDa, 15 kDa, 20 kDa, 25 kDa, 30 kDa, 35 kDa, 40 kDa, 45 kDa, 50 kDa, or 60 kDa;
- X is an L-amino acid having the structure:
- X−1 indicates the point of attachment to the preceding amino acid residue;
- and
- X+1 indicates the point of attachment to the following amino acid residue.
9 more elements
An IL-2 conjugate comprising the amino acid sequence of SEQ ID NO:
- 3, wherein the amino acid at position P64 is replaced by the structure of Formula (I):
- wherein:
- Z is CH2 and Y is
- or
- Y is CH2 and Z is
- W is a PEG group having a molecular weight of about 30 kDa;
- X is an L-amino acid having the structure:
- X−1 indicates the point of attachment to the preceding amino acid residue;
- and
- X+1 indicates the point of attachment to the following amino acid residue.
7 more elements
Dependencies are inferred from the claim text.