Macitentan Combination Therapy for Pulmonary Hypertension
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Solution Overview
Problem
Current treatments for diseases involving endothelin, such as pulmonary hypertension, often face challenges with side effects like flushing and systemic hypotension, and there is a need for more effective synergistic therapies combining endothelin receptor antagonists with prostacyclin receptor agonists.
Innovation Solution
A product containing macitentan, an endothelin receptor antagonist, in combination with a compound having prostacyclin receptor agonist properties, such as NS-304, is administered simultaneously or over a period to treat diseases like pulmonary hypertension, reducing side effects and enhancing therapeutic efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If endothelin receptor antagonists are used to treat diseases like pulmonary hypertension, then therapeutic efficacy is improved, but side effects like flushing and systemic hypotension occur
Solution Approach 1:
The patent combines macitentan (an endothelin receptor antagonist) with a prostacyclin receptor agonist in a single pharmaceutical composition. This merging of two different therapeutic agents with complementary mechanisms of action allows the treatment to achieve better efficacy while the prostacyclin agonist component helps mitigate the side effects of the endothelin antagonist, thereby resolving the contradiction between therapeutic efficacy and side effect profile
2Object-generated harmful factors
If prostacyclin receptor agonists are used alone, then side effects like flushing and systemic hypotension occur, but combining them with endothelin receptor antagonists reduces these side effects
Solution Approach 1:
The patent merges the endothelin receptor antagonist and prostacyclin receptor agonist into a single combined pharmaceutical composition. This approach reduces treatment complexity by simplifying the administration regimen (single pill vs. multiple medications) while maintaining the beneficial effect of reducing side effects through the synergistic combination of both agents
3Reliability
If combination therapy with endothelin receptor antagonists and prostacyclin receptor agonists is used, then synergistic therapeutic effect is achieved, but treatment complexity increases
Solution Approach 1:
The patent combines two therapeutic agents with different mechanisms of action into a single pharmaceutical composition, thereby achieving synergistic therapeutic effects while simplifying the treatment regimen. The fixed-dose combination eliminates the need for separate administration of multiple medications, reducing pill burden and improving patient compliance without compromising the synergistic effect
Data Source
AI summary
The invention relates to a product containing the compound of formula (I) below or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having prostacyclin receptor (IP) agonist properties, or a pharmaceutically acceptable salt thereof.