Combination Therapy for NAFLD and NASH Treatment
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Solution Overview
Problem
There is a continued need for effective treatments for non-alcoholic fatty liver disease (NAFLD) and its more severe form, non-alcoholic steatohepatitis (NASH), as current therapies are inadequate in managing the condition effectively, particularly in reducing liver triglycerides and oxidative stress, which can lead to liver damage and increased risk of cirrhosis and hepatocellular carcinoma.
Innovation Solution
A pharmaceutical composition comprising a compound of formula (I), a selective Farnesoid X Receptor (FXR) agonist, in combination with one or more additional therapeutic agents, such as PPAR agonists, administered in synergistically effective amounts, either simultaneously or sequentially, to treat NAFLD and NASH, potentially reducing liver triglycerides and oxidative stress.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current monotherapy treatments are used for NAFLD/NASH, then treatment simplicity is maintained, but therapeutic effectiveness is insufficient in reducing liver triglycerides and oxidative stress
Solution Approach 1:
The patent combines a PPAR agonist and an FXR agonist into a single pharmaceutical composition for simultaneous administration. This merging of two therapeutic agents addresses the limitation of monotherapy by providing synergistic effects that reduce liver triglycerides and oxidative stress more effectively than either agent alone, while maintaining treatment simplicity through combined formulation
2Reliability
If higher doses of single therapeutic agents are used to improve efficacy, then therapeutic effectiveness increases, but side effects and treatment duration increase
Solution Approach 1:
By combining sub-effective doses of PPAR agonist and FXR agonist in a single composition, the patent achieves synergistic therapeutic effects that are greater than the sum of individual effects. This allows effective treatment at lower overall doses, reducing side effects and potential toxicity associated with high-dose monotherapy
3Reliability
If combination therapy with multiple agents is used to improve efficacy, then therapeutic effectiveness increases, but dosing regimen complexity increases
Solution Approach 1:
The patent formulates the PPAR agonist and FXR agonist together in a single pharmaceutical composition that can be administered as one dosage unit. This combined formulation maintains the synergistic therapeutic benefits of combination therapy while eliminating the complexity of coordinating separate dosing schedules, improving patient compliance and ease of administration
Data Source
AI summary
A pharmaceutical composition comprising: a form of compound of formula (I) and at least one additional therapeutic agent, and optionally one or more pharmaceutically acceptable carriers.