Anti-191P4D12 ADC Composition With Excipient-Tuned Stability
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Solution Overview
Problem
Existing pharmaceutical compositions for anti-191P4D12 antibody drug conjugates lack optimal physical and pharmaceutical properties, requiring tailored excipients to enhance bioavailability, ease of manufacture, and stability.
Innovation Solution
A pharmaceutical composition comprising anti-191P4D12 antibody drug conjugates with specific CDR sequences, linked to monomethyl auristatin E via a linker, and formulated with L-histidine, polysorbate-20, trehalose dihydrate, and sucrose excipients, optimized for concentration and pH to enhance stability and efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional excipients are used in antibody drug conjugate formulations, then the formulation can be maintained with standard components, but the physical and pharmaceutical properties (bioavailability, stability, ease of manufacture) are not optimized
Solution Approach 1:
The patent changes the chemical and physical parameters of the excipient formulation by specifying precise concentrations of L-histidine (10-50 mM), polysorbate-20 (0.01-0.1%), trehalose dihydrate (1-20%), and sucrose (1-20%). These parameter optimizations enhance the stability and manufacturability of the antibody drug conjugate formulation compared to conventional excipient combinations.
2Quantity of substance
If standard pharmaceutical excipients are used, then the formulation process is simplified, but bioavailability and stability are not enhanced
Solution Approach 1:
The patent employs a composite excipient system combining four specific components: L-histidine, polysorbate-20, trehalose dihydrate, and sucrose. This composite formulation enhances bioavailability and stability while maintaining reasonable formulation complexity through the synergistic interaction of these specific excipients at optimized concentrations.
3Stability of the object's composition
If the antibody drug conjugate is formulated with optimized excipients, then stability and bioavailability are improved, but the formulation complexity increases
Solution Approach 1:
The patent optimizes formulation parameters by defining specific concentration ranges for each excipient component, which enhances stability while managing formulation complexity through precise parameter control rather than requiring complex formulation processes.
Data Source
AI summary
A pharmaceutical composition comprising an antibody drug conjugate comprising an antibody or antigen binding fragment thereof that binds to 191P4D12 conjugated to one or more units of monomethyl auri statin E (MMAE) and a pharmaceutically acceptable excipient comprising L-histidine, polysorbate-20 (TWEEN-20), and at least one of trehalose dihydrate and sucrose.