Anti-RSV Antibody Formulation for High-Concentration Injectability

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Solution Overview

Problem

Current formulations of anti-RSV antibodies lack stability and bioactivity during storage and transportation, leading to issues such as high viscosity, aggregation, and suboptimal concentration for effective subcutaneous and intravenous administration.

Innovation Solution

Formulations comprising anti-RSV antibodies or antigen-binding fragments with specific buffers, stabilizers (e.g., non-reducing sugars and amino acids), non-ionic surfactants, and antioxidants, optimized for high concentrations and low viscosity, maintaining stability and bioactivity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If high concentration of anti-RSV antibody is used for subcutaneous administration, then therapeutic benefit is maximized, but viscosity increases making injection difficult

Engineering Contradiction:

Improveantibody concentrationVSAvoidinjectability

Core Design Contradiction:

Quantity of substanceVSEase of operation

Solution Approach 1:

The patent modifies formulation parameters including pH (adjusted to specific ranges using buffers like histidine or acetate), ionic strength, and composition (adding excipients such as amino acids, sugars, and surfactants) to reduce antibody viscosity at high concentrations, enabling both high therapeutic dosage and ease of subcutaneous injection

Inventive Principle:

Principle #35Parameter changes

2Quantity of substance

If high concentration of anti-RSV antibody is used, then therapeutic benefit is maximized, but aggregation increases reducing stability

Engineering Contradiction:

Improveantibody concentrationVSAvoidantibody stability

Core Design Contradiction:

Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent introduces intermediary substances (excipients) including amino acids (arginine, lysine, proline), sugars (sucrose, trehalose), and surfactants (polysorbate 80, poloxamer 188) that act as mediators to prevent antibody aggregation and maintain stability at high concentrations during storage and administration

Inventive Principle:

Principle #24Intermediary (Mediator)

3Quantity of substance

If high concentration of anti-RSV antibody is used, then therapeutic benefit is maximized, but osmolality increases beyond physiological conditions

Engineering Contradiction:

Improveantibody concentrationVSAvoidosmolality

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent adjusts the osmolality parameter by optimizing buffer concentration, ionic strength, and excipient levels to maintain formulation osmolality within or near physiological ranges, preventing osmotic stress while delivering high antibody concentrations therapeutically

Inventive Principle:

Principle #35Parameter changes

4Ease of manufacture

If conventional formulations are used, then storage and transport are simplified, but bioactivity is lost over time

Engineering Contradiction:

Improveformulation simplicityVSAvoidbioactivity

Core Design Contradiction:

Ease of manufactureVSReliability

Solution Approach 1:

The patent incorporates stabilizing excipients and optimizes formulation conditions in advance to prevent bioactivity loss during storage and transport, ensuring the antibody remains therapeutically effective without requiring complex cold chain logistics

Inventive Principle:

Principle #10Preliminary action

Data Source

PatentUS12565526B2Formulations of anti-RSV antibodies and methods of use thereof

Publication Date: 2026.03.03 MERCK SHARP & DOHME LLC

AI summary

The present invention relates to stable formulations comprising antibodies or antigen-binding fragments thereof that bind to respiratory syncytial virus (RSV). Also provided are methods of preventing and/or treating RSV-related diseases with the formulations of the invention.