Stabilizing alkylglycoside compositions and methods thereof

Inventors

Maggio, Edward T.

Assignees

Aegis Therapeutics LLC

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 interferons, such as interferon-alpha, interferon-beta, interferon-gamma, and variants thereof.

Core Innovation

The document describes liquid or lyophilized pharmaceutical compositions comprising interferon and a stabilizing agent, where the stabilizing agent is dodecyl-beta-D-maltoside. The compositions are formulated to increase stability and to reduce aggregation and/or reduce immunogenicity of interferon during systemic delivery or after lyophilized storage and reconstitution.

The document further describes stabilizing alkylglycoside surfactants and related saccharide alkyl ester surfactants as a means to mitigate self-associating peptide/protein therapeutics aggregation and fibril formation. The described peptide/protein therapeutics include interferons, insulin, amylin, and an HIV entry inhibitor peptide, including Peptide T/DAPTA.

The document states that the stabilizing behavior depends on the alkylglycoside anomer composition, describing that a beta-anomer-rich dodecyl maltoside stabilizes longer than an alpha-anomer or an alpha-contaminated beta-anomer. It also describes quantitative surfactant properties, including critical micelle concentration thresholds, as part of the stabilization rationale for the alkylglycoside surfactant system.

Claims Coverage

The relevant set includes three independent claims. Each independent claim centers on interferon combined with dodecyl-beta-D-maltoside as the stabilizing agent, with differences in formulation form and one claim specifying the alkylsaccharide as consisting of dodecyl beta-D-maltoside.

Across the independent claims, the main inventive concept is the use of dodecyl-beta-D-maltoside as the stabilizing agent in interferon compositions to increase stability while reducing aggregation and/or immunogenicity, with claim coverage split by liquid vs lyophilized form and by specifying the stabilizing agent as an alkylsaccharide consisting of dodecyl-beta-D-maltoside.

Stated Advantages

Documented Applications