Anti-INSR Antibody Formulation for Long-Term Storage Stability

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Solution Overview

Problem

Existing formulations of anti-insulin receptor antibodies, such as RZ358, face stability issues during storage, leading to degradation and loss of potency, which affects their efficacy in treating conditions related to hyperinsulinemia and hypoglycemia.

Innovation Solution

A composition comprising an anti-INSR antibody, histidine or histidine HCL, methionine, a surfactant like polysorbate, and a sugar alcohol such as sorbitol or mannitol, formulated at specific concentrations and pH, which enhances stability and maintains antibody potency over extended storage periods.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing formulations of anti-insulin receptor antibodies are used, then the antibody can be administered for treatment, but the antibody degrades during storage and loses potency

Engineering Contradiction:

Improveantibody stability during storageVSAvoidstorage duration

Core Design Contradiction:

ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent optimizes formulation parameters including pH (adjusted to specific ranges using buffers like histidine or citrate), ionic strength, and concentrations of excipients (surfactants at 0.01-0.5%, amino acids at 1-50 mM, sugar alcohols at 10-300 mM) to minimize antibody degradation during storage, thereby resolving the contradiction between maintaining stability and extending storage duration

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent introduces intermediary substances (excipients) such as surfactants (polysorbate 20, polysorbate 80), amino acids (histidine, methionine, arginine), and sugar alcohols (sorbitol, mannitol) that act as protective mediators between the antibody and degrading environmental factors, thereby enhancing stability over extended storage periods

Inventive Principle:

Principle #24Intermediary (Mediator)

2Stability of the object's composition

If existing formulations are used, then the antibody can be stored, but degradation occurs leading to loss of therapeutic efficacy

Engineering Contradiction:

Improveantibody composition stabilityVSAvoidantibody potency

Core Design Contradiction:

Stability of the object's compositionVSLoss of substance

Solution Approach 1:

The patent incorporates protective excipients in advance into the formulation to cushion the antibody against degradation mechanisms (aggregation, oxidation, deamidation) that occur during storage, preventing potency loss before it happens rather than attempting to restore it later

Inventive Principle:

Principle #11Beforehand cushioning (Prior cushioning)

Solution Approach 2:

The patent creates a composite pharmaceutical formulation combining the anti-insulin receptor antibody with multiple excipients (surfactants, amino acids, sugar alcohols, buffers) that work synergistically to maintain composition stability and prevent potency loss during storage

Inventive Principle:

Principle #40Composite materials

Data Source

PatentUS20260070996A1Formulations for Anti-insulin receptor antibody and uses thereof

Publication Date: 2026.03.12 XOMA US LLC

AI summary

The present disclosure relates, in general, to formulations comprising anti-insulin receptor antibody RZ 358 and use thereof to treat hyperinsulinemia disorders.