Inhalable Imatinib Formulations for Pulmonary Arterial Hypertension
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Solution Overview
Problem
Current treatments for pulmonary arterial hypertension (PAH) using imatinib are limited by severe adverse events and inefficiencies in drug delivery, particularly due to high doses required for systemic administration, which can lead to adverse effects like subdural hematoma.
Innovation Solution
Development of inhalable formulations with high ratios of imatinib or its salts (50% or more) that are micronized to achieve deep lung penetration, reducing the volume of non-active components and minimizing systemic exposure, thereby enhancing patient comfort and safety while maintaining therapeutic efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high doses of imatinib are administered systemically to treat PAH, then therapeutic efficacy is improved, but severe adverse events increase
Solution Approach 1:
The patent applies local quality by formulating imatinib as inhalable particles with specific size ranges (0.5-5 μm) that enable selective deposition in pulmonary tissue. This localizes the drug action to the lungs where PDGFR is upregulated, achieving therapeutic efficacy while minimizing systemic circulation and associated adverse events like subdural hematoma
2Quantity of substance
If conventional oral or IV administration is used, then systemic delivery is achieved, but lung exposure is insufficient
Solution Approach 1:
The patent segments the drug delivery system into inhalable particles with specific aerodynamic properties. By formulating imatinib as discrete particles in the 0.5-5 μm range, the system enables direct pulmonary deposition, achieving high local lung exposure while reducing the total dose required compared to systemic administration
3Reliability
If large volumes of formulation are inhaled to deliver therapeutic API concentration, then drug delivery is improved, but patient comfort and safety deteriorate
Solution Approach 1:
The patent changes the concentration parameter of API in the inhalable formulation to 50% or higher. This high-API ratio formulation delivers therapeutically effective concentrations in smaller total volumes, improving patient comfort and safety by reducing the overall amount of compound inhaled while maintaining effective drug delivery
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The high-API ratio inhalable formulations provide greater lung exposure with lower doses, reducing adverse events and improving treatment outcomes for PAH and other pulmonary cardiovascular conditions, such as lung transplant rejection and pulmonary veno-occlusive disease, by directly targeting the lung tissue.
Implementation Method 1
Inhalable formulations with high ratios of imatinib or its salts (50% or more) that are micronized to achieve deep lung penetration
Data Source
AI summary
The invention relates to inhalable imatinib formulations, manufacture, and uses thereof.