Combination Therapy Using Factor XII and C1 Inhibitors

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Solution Overview

Problem

Current treatments for disorders of the contact activation system, such as thrombosis, lack efficacy and often require high doses of costly therapeutic agents, necessitating the development of more effective and dose-reducing combinations for conditions like arterial thrombosis, interstitial lung disorders, and neurological inflammatory disorders.

Innovation Solution

Combination therapies involving a Factor XII inhibitor, such as rHA-Infestin-4 or anti-FXII antibodies, and a C1 esterase inhibitor, like BERINERT®, are administered to synergistically treat disorders of the contact activation system, including thrombotic disorders, interstitial lung disorders, and neurological inflammatory disorders, potentially allowing for reduced dosages and enhanced efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If monotherapy with C1 esterase inhibitor is used, then treatment is simpler and cost is lower, but therapeutic efficacy is insufficient for severe thrombotic disorders

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidtreatment complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines C1 esterase inhibitor with Factor XII inhibitor into a single therapeutic composition, merging two mechanisms of action to achieve synergistic effects. This combination addresses the insufficiency of monotherapy by simultaneously inhibiting multiple components of the contact activation system, thereby improving therapeutic efficacy for severe thrombotic disorders while maintaining a unified treatment protocol.

Inventive Principle:
Principle #5Merging (Combining)

2Reliability

If high doses of therapeutic agents are used, then therapeutic efficacy is improved, but treatment cost increases

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoiddrug dosage
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

By combining C1 esterase inhibitor with Factor XII inhibitor, the patent achieves synergistic inhibition of the contact activation system. This combination allows for reduced individual dosages of each agent while maintaining or improving therapeutic efficacy, thereby reducing overall treatment cost compared to high-dose monotherapy.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent modifies the therapeutic approach by changing the dosing parameters through combination therapy. The synergistic interaction between the two inhibitors enables the use of lower, more cost-effective dosages while achieving the desired therapeutic effect, thus optimizing the balance between efficacy and cost.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If combination therapy with Factor XII inhibitor and C1 esterase inhibitor is used, then synergistic efficacy is achieved, but treatment protocol becomes more complex

Engineering Contradiction:
Improvesynergistic efficacyVSAvoidtreatment protocol complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent merges two therapeutic agents with different mechanisms of action into a unified composition. By combining C1 esterase inhibitor and Factor XII inhibitor, the patent achieves synergistic efficacy through simultaneous inhibition of multiple pathways in the contact activation system, while the combination is formulated as a single treatable unit to manage protocol complexity.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentUS20240398914A1Combination therapy using a factor xii inhibitor and a c-1 inhibitor
Publication Date: 2024.12.05 CSL BEHRING GMBH
  • US20240398914A1 patent drawing
  • US20240398914A1 patent drawing

AI summary

Methods and compositions are disclosed for treating disorders of the contact activation system, comprising the administration of at least one C1-Inhibitor (C1-INH) and at least one Factor XII (FXII) inhibitor.