Conjugates of an il-7 moiety and a polymer
Inventors
Charych, Deborah H. • Zhang, Ping • Kirk, Peter Benedict
Assignees
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Publication Number
US-12629407-B2
Publication Date
2026-05-19
Expiration Date
Abstract
Conjugates of an IL-7 moiety and one or more nonpeptidic, water-soluble polymers are provided. Typically, the non-peptidic, water-soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided, among other things, are compositions comprising conjugates, methods of making conjugates, and methods of administering compositions to an individual.
Core Innovation
The invention relates to a conjugate comprising an interleukin-7 (IL-7) moiety covalently attached to a poly(ethylene glycol) polymer at an amino group of the IL-7 moiety via an amine linkage. The conjugate possesses a measurable degree of IL-7 bioactivity. The poly(ethylene glycol) component includes an integer variable (n) defining values from 2 to 4000.
The disclosed conjugates include branched or functionalized mPEG derivatives and representative linkage elements connecting to an IL-7 moiety. The linkage chemistries depicted include carbamate linkage, amide linkage, secondary-amine linkages, thioether and disulfide linkages, and cleavable or releasable linkages, together with optional linker and spacer contexts associated with the polymer and IL-7 attachment.
Claims Coverage
The claim coverage centers on one independent claim defining an IL-7/PEG conjugate with covalent attachment at an amino group via an amine linkage and measurable IL-7 bioactivity. Dependent claims refine the PEG component, the attachment site, the number of attached PEG polymers, and the IL-7 amino acid sequence using SEQ ID NOs 1 through 8.
IL-7 covalently attached to PEG at an amino group via an amine linkage
A conjugate comprising an interleukin-7 (IL-7) moiety covalently attached to a poly(ethylene glycol) polymer at an amino group of the IL-7 moiety via an amine linkage.
PEG chain length parameter (n) range
Each (n) is independently an integer having a value of from 2 to 4000.
Measurable degree of IL-7 bioactivity
The conjugate possesses a measurable degree of IL-7 bioactivity.
PEG weight-average molecular-weight constraint
The poly(ethylene glycol) polymer has a weight-average molecular weight between about 500 Da and about 100,000 Da.
Specific PEG molecular-weight embodiments
The poly(ethylene glycol) polymer has a weight-average molecular weight of about 20,000 or about 40,000 Daltons.
N-terminus amino-group attachment of PEG to IL-7
The poly(ethylene glycol) polymer is covalently attached to an amino group at the N-terminus of the IL-7 moiety.
Controlled number of PEG polymers attached to IL-7
The IL-7 moiety includes one, two, three, or four poly(ethylene glycol) polymers attached.
IL-7 amino acid sequence restricted to enumerated SEQ ID NOs
The IL-7 component contains an amino acid sequence chosen from SEQ ID NOs 1 through 8.
The claims cover PEGylated IL-7 conjugates in which IL-7 is attached to a PEG polymer at an amino group via an amine linkage and the conjugate possesses measurable IL-7 bioactivity. Dependent claim coverage further limits PEG molecular weight, the IL-7 attachment location, the number of PEG polymers attached, and IL-7 identity selected from defined SEQ ID NOs.
Stated Advantages
Controls immunogenicity, elimination, localization, and sustained JAK/STAT pathway signaling by using releasable versus non-releasable linkages.
Maintains measurable IL-7 bioactivity.
Selected formulations/compositions can be substantially free of albumin/non-IL-7 proteins.
Documented Applications
Measurable IL-7 bioactivity is evaluated by STATS phosphorylation in 2E8 cells.
IL-7 labeling using thiol-selective PEG conjugation reagents, including IL-7 conjugates formed with thiol attachment sites on IL-7.
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