Stabilized formulations containing anti-interleukin-4 receptor (IL-4R) antibodies
Inventors
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Assignees
Member
Glycos Biomedical LtdWe are UK/US entity with a team based in Maryland and North Carolina comprising an expert team that has linked triggers to disease states including TBI and acute injuries associated with radiation, acute lung injury and infection.
We are UK/US entity with a team based in Maryland and North Carolina comprising an expert team that has linked triggers to disease states including TBI and acute injuries associated with radiation, acute lung injury and infection.
Publication Number
US-12624115-B2
Publication Date
2026-05-12
Expiration Date
Abstract
The present invention provides pharmaceutical formulations comprising a human antibody that specifically binds to human interleukin-4 receptor (hIL-4R). The formulations may contain, in addition to an anti-hIL-4R antibody, at least one amino acid, at least one sugar, or at least one non-ionic surfactant. The pharmaceutical formulations of the present invention exhibit a substantial degree of antibody stability after storage for several months.
Core Innovation
A stabilized liquid pharmaceutical formulation is described for anti-human interleukin-4 receptor alpha antibodies. The formulation comprises a human anti-hIL-4Rb1 antibody as an immunoglobulin molecule having two heavy chains and two light chains interconnected by disulfide bonds, wherein the heavy chain variable region comprises the amino acid sequence of SEQ ID NO: 1 and the light chain variable region comprises the amino acid sequence of SEQ ID NO: 5.
The formulation further includes a thermal stabilizer, a non-ionic surfactant, and arginine, and it is defined by a pH from about 5.6 to about 6.2 and a viscosity of less than 35 cPoise. The anti-hIL-4Rb1 antibody is present at about 100 mg/ml to about 200 mg/ml, the thermal stabilizer is present at about 0.9% w/v to about 10% w/v, and arginine is present at about 20 to 100 mM.
The problem being solved is loss of formulation quality over time, including aggregation and changes in antibody forms during storage. The formulation is defined by a stability criterion in which less than about 5% of the anti-hIL-4Rb1 antibody recovered after 3 months of storage at 5b0 C. is aggregated, as determined by size exclusion chromatography.
Claims Coverage
The independent claim set out a pharmaceutical formulation with six inventive features: a human anti-hIL-4Rb1 antibody defined by SEQ ID sequences, a thermal stabilizer, a non-ionic surfactant, arginine, a pH and viscosity window, and a storage aggregation threshold. Dependent claims primarily refine component identities and quantitative ranges for particular excipients and formulation properties.
Human anti-hIL-4Rb1 antibody defined by SEQ ID sequences and immunoglobulin structure
The pharmaceutical formulation comprises a human anti-hIL-4Rb1 antibody as an immunoglobulin molecule with two heavy chains and two light chains interconnected by disulfide bonds, wherein each heavy chain variable region comprises the amino acid sequence of SEQ ID NO: 1 and each light chain variable region comprises the amino acid sequence of SEQ ID NO: 5, with an antibody concentration of about 100 mg/ml to about 200 mg/ml.
Thermal stabilizer presence with defined concentration range
The formulation includes a thermal stabilizer at a concentration from about 0.9% w/v to about 10% w/v.
Non-ionic surfactant incorporation
The formulation includes a non-ionic surfactant.
Arginine at specified concentration to control formulation properties
The formulation includes arginine at a concentration from about 20 to 100 mM.
pH window and viscosity constraint
The formulation has a pH from about 5.6 to about 6.2, and the viscosity of the formulation is less than 35 cPoise.
Low aggregation after storage as measured by size exclusion chromatography
Less than about 5% of the anti-hIL-4Rb1 antibody recovered from the pharmaceutical formulation after 3 months of storage at 5b0 C. is aggregated, as determined by size exclusion chromatography.
Across the inventive features, the claim coverage focuses on a human anti-hIL-4Rb1 antibody defined by SEQ ID NO: 1 and SEQ ID NO: 5, formulated with a thermal stabilizer, a non-ionic surfactant, and arginine, together with a defined pH window (5.6b76.2), a viscosity limit (<35 cPoise), and a defined aggregation threshold after 3 months at 5b0 C. (less than about 5% aggregated by size exclusion chromatography).
Stated Advantages
Provides a stabilized liquid formulation meeting a low aggregation criterion after storage (less than about 5% aggregated after 3 months at 5b0 C. by size exclusion chromatography).
Maintains low viscosity (less than 35 cPoise) while using the specified formulation components and pH window.
Reports stability/quality retention including high native conformation recovery and low aggregation, with limited acidic-form formation, after storage at selected temperatures.
Mitigates agitation-related effects through use of polysorbate 20/80 in the formulation.
Documented Applications
Contemplated parenteral delivery routes and container-device types, including subcutaneous administration and devices such as autoinjector/pen devices, as stated in the provided content.
Use of suitable containers including glass vials and syringes, including low-tungsten syringes with coated plungers, as described in the provided content.
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