Compound 1 Pharmaceutical Formulation for Cancer Treatment
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
There is a need for compounds that inhibit TAM receptor tyrosine kinases such as Axl and Mer to treat various cancers, as their overexpression leads to tumor growth and poor prognosis in patients.
Innovation Solution
The development of pharmaceutical compositions comprising Compound 1, N-(4-fluorophenyl)-N-(4-((7-methoxy-6-(methylcarbamoyl)quinolin-4-yl)oxy)phenyl)cyclopropane-1,1-dicarboxamide, in its free base or pharmaceutically acceptable salt forms, which are suitable for oral administration and include diluents, binders, disintegrants, glidants, lubricants, and optional film coatings, to inhibit protein kinases and treat cancers.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If Compound 1 is formulated as a pharmaceutical composition with multiple excipients (diluents, binders, disintegrants, glidants, lubricants, and film coating), then manufacturability and therapeutic efficacy are improved, but device complexity and formulation complexity increase
Solution Approach 1:
The pharmaceutical composition is divided into multiple functional components: Compound 1 (active ingredient), diluents (for volume), binders (for cohesion), disintegrants (for breakdown), glidants (for flow), lubricants (for friction reduction), and film coating (for protection). Each component serves a specific manufacturing or therapeutic function, resolving the contradiction by making the formulation process easier through specialized segmentation of functions.
2Reliability
If Compound 1 is used to inhibit TAM receptor tyrosine kinases, then therapeutic efficacy is improved, but the need for precise dosing and formulation control increases manufacturing difficulty
Solution Approach 1:
The patent specifies precise parameters for Compound 1 including its chemical structure (N-(4-fluorophenyl)-N-(4-((7-methoxy-6-(methylcarbamoyl)quinolin-4-yl)oxy)phenyl)cyclopropane-1,1-dicarboxamide), crystalline form, salt forms, and dosage ranges. These parameter specifications ensure reliable inhibition of TAM receptor tyrosine kinases while providing clear manufacturing guidelines to control the active ingredient's properties and dosing.
3Productivity
If multiple excipients are included in the pharmaceutical composition, then therapeutic efficacy and manufacturability are improved, but the quantity of substance and cost increase
Solution Approach 1:
The patent extracts and specifies only the necessary excipients for optimal therapeutic efficacy and manufacturability: diluents, binders, disintegrants, glidants, lubricants, and optional film coating. By selectively including only these essential components rather than unnecessary additives, the formulation achieves high productivity while minimizing the total quantity of substance and associated costs.
Data Source
AI summary
The present invention relates to pharmaceutical compositions of the c-Met inhibitor, Compound 1. The invention also relates to methods of treating a disease, disorder, or syndrome mediated at least in part by modulating in vivo activity of a protein kinase using the pharmaceutical composition and to processes for making the pharmaceutical compositions.