CEACAM5 ADC Formulation for Long-Term Stability at Controlled pH

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Current formulations of huMAb2-3-SPDB-DM4, an antibody-drug conjugate, face challenges in achieving long-term stability and shelf life, making them difficult to formulate effectively for therapeutic applications.

Innovation Solution

A pharmaceutical formulation comprising an anti-human carcinoembryonic antigen-related cell adhesion molecule 5 (hCEACAM5) antibody-drug conjugate (ADC) with specific buffering agents, tonicity agents, surfactants, and optionally chelating agents, optimized at pH 5.0 to 6.5, which includes components like acetate, sorbitol, polysorbate 80, and EDTA, enhancing stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If huMAb2-3-SPDB-DM4 is formulated for therapeutic use, then it can treat CEACAM5-expressing cancers, but it suffers from poor long-term stability and short shelf life

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidshelf life

Core Design Contradiction:

ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent optimizes formulation parameters including pH (5.0-6.5), ionic strength, and component concentrations to enhance the stability and shelf life of huMAb2-3-SPDB-DM4 while maintaining its therapeutic effectiveness

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite formulation system combining huMAb2-3-SPDB-DM4 with buffering agents (acetate, histidine, citrate), tonicity agents (sorbitol, sucrose, mannitol), and surfactants (polysorbate 80, polysorbate 20, poloxamer 188) to achieve both stability and therapeutic efficacy

Inventive Principle:

Principle #40Composite materials

2Duration of action of stationary object

If huMAb2-3-SPDB-DM4 is formulated with additional stabilizing components, then shelf life and stability improve, but formulation complexity increases

Engineering Contradiction:

Improveshelf lifeVSAvoidformulation complexity

Core Design Contradiction:

Duration of action of stationary objectVSDevice complexity

Solution Approach 1:

The patent divides the formulation into distinct functional components (buffering agents for pH control, tonicity agents for osmotic balance, surfactants for surface tension control) that can be independently optimized and combined

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent selects formulation components that perform multiple functions: buffering agents maintain pH stability and protect against degradation, while also contributing to ionic strength control; tonicity agents protect against aggregation while maintaining osmotic balance

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS12564642B2CEACAM5 antibody-drug conjugate formulation

Publication Date: 2026.03.03 SANOFI SA(FR)

AI summary

Provided are stabilized formulations of the human carcinoembryonic antigen-related cell adhesion molecule 5 (hCEACAM5)-targeted antibody-drug conjugate huMAb2-3-SPDB-DM4, as well as methods for making and using same.