Stabilizing alkylglycoside compositions and methods thereof
Inventors
Assignees
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Publication Number
US-8846044-B2
Publication Date
2014-09-30
Expiration Date
Abstract
The present invention relates to alkylglycoside-containing compositions and methods for increasing the stability, reducing the aggregation and immunogenicity, increasing the biological activity, and reducing or preventing fibrillar formation of a peptide, polypeptide, or variant thereof, for example parathyroid hormone (PTH) or PTH analogs, amylin, a monoclonal antibody, insulin, Peptide T or analog thereof, gastrin, gastrin releasing peptides, gastrin releasing peptide-like (GRP) proteins, epidermal growth factor or analog thereof.
Core Innovation
The invention relates to pharmaceutical compositions and methods for increasing the stability of a monoclonal antibody by using a stabilizing agent comprising at least one alkylglycoside. The stabilizing agent is described as a surfactant used to increase stability, reduce aggregation, reduce immunogenicity, and extend shelf life while preserving activity.
The document addresses aggregation-driven potency loss and immunogenicity as issues for protein therapeutics, including monoclonal antibodies, and frames the invention as reducing loss of biological activity associated with aggregation and fibril formation. The core approach is to use alkylglycoside surfactants to control these stability liabilities of monoclonal antibodies and related protein therapeutics.
The alkylglycoside approach is supported by discussion of surfactants in relation to critical micelle concentration thresholds and preference for low CMC agents, as well as alkylglycoside anomer purity, including beta anomer versus alpha contamination, as factors associated with stability outcomes. The disclosed uses are tied to monoclonal antibodies, including an IgG class example, and additional peptide/protein therapeutics described alongside the alkylglycoside stabilization concept.
Claims Coverage
The partial claim set includes two independent claims. The coverage is concentrated on a monoclonal antibody stabilized by specified alkylglycoside surfactants, and on a method that forms a composition with the monoclonal antibody, the alkylglycoside stabilizing agent, and a buffering agent to increase stability.
Monoclonal antibody stabilized by an alkylglycoside surfactant
A pharmaceutical composition for increasing stability, reducing aggregation or reducing immunogenicity of a monoclonal antibody comprising a monoclonal antibody and a stabilizing agent comprising at least one alkylglycoside, wherein the alkylglycoside is selected from specified D-maltoside, D-glucoside, maltoside, glucoside, sucroside, alkyl thiomaltoside, alkyl thioglucoside, alkyl maltotrioside, and related long chain aliphatic derivatives.
Method of admixing monoclonal antibody with alkylglycoside and buffering agent
A method for increasing the stability of a monoclonal antibody comprising admixing the monoclonal antibody, a stabilizing agent and a buffering agent to form a composition, wherein the stabilizing agent is at least one alkylglycoside surfactant, thereby increasing the stability of the monoclonal antibody.
Across the independent claim coverage, the key inventive element is the use of specified alkylglycoside surfactants as stabilizing agents with a monoclonal antibody. The method independent claim further requires a buffering agent in addition to the alkylglycoside surfactant to form a composition for increasing stability.
Stated Advantages
Increasing stability of a monoclonal antibody.
Reducing aggregation of a monoclonal antibody.
Reducing immunogenicity of a monoclonal antibody.
Extending shelf life while preserving activity.
Documented Applications
Pharmaceutical compositions and methods for increasing stability of a monoclonal antibody, including compositions intended to reduce aggregation and/or reduce immunogenicity.
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