Formula I Compound and Azacitidine Synergy for Leukemia
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Solution Overview
Problem
Current treatments for myelodysplastic syndrome and acute myeloid leukemia are limited by low potency, high toxicity, and limited therapeutic response, with existing chemotherapeutic agents offering modest efficacy and significant side effects, necessitating the development of new therapies with improved potency and reduced toxicity.
Innovation Solution
A novel composition comprising a combination of antiproliferative agents, specifically a compound according to Formula I, such as (E)-2-(5-((2,4,6-trimethoxystyrylsulfonyl)methyl)-2-methoxyphenylamino)acetic acid, combined with a DNA methyltransferase inhibitor like azacitidine, to treat myelodysplastic syndrome and acute myeloid leukemia, aiming for synergistic cytotoxic effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing chemotherapeutic agents are used to treat myelodysplastic syndrome and acute myeloid leukemia, then treatment can be administered, but therapeutic potency is low and toxicity is high
Solution Approach 1:
The patent combines a compound of Formula I with a DNA methyltransferase inhibitor (such as azacitidine) into a single composition, creating a synergistic therapeutic effect that enhances potency while managing toxicity through complementary mechanisms of action
Solution Approach 2:
The invention creates a composite therapeutic composition integrating two distinct pharmacological agents with different mechanisms of action, where the compound of Formula I and DNA methyltransferase inhibitor work together to achieve superior therapeutic outcomes compared to either agent alone
2Reliability
If existing chemotherapeutic agents are used to treat myelodysplastic syndrome and acute myeloid leukemia, then treatment can be administered, but therapeutic response is limited
Solution Approach 1:
The patent combines a compound of Formula I with a DNA methyltransferase inhibitor (such as azacitidine) into a single composition, creating a synergistic therapeutic effect that enhances potency while managing toxicity through complementary mechanisms of action
3Device complexity
If single agent chemotherapy is used, then treatment simplicity is maintained, but synergistic cytotoxic effects are not achieved
Solution Approach 1:
The patent combines a compound of Formula I with a DNA methyltransferase inhibitor (such as azacitidine) into a single composition, creating a synergistic therapeutic effect that enhances potency while managing toxicity through complementary mechanisms of action
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 combination of the compound and azacitidine demonstrates a synergistic effect, enhancing therapeutic potency and reducing side effects, potentially leading to improved treatment outcomes for myelodysplastic syndrome and acute myeloid leukemia by inhibiting DNA methyltransferases and inducing apoptosis in leukemia cells.
Implementation Method 1
The combination of the compound and azacitidine demonstrates a synergistic effect, enhancing therapeutic potency and reducing side effects, potentially leading to improved treatment outcomes for myelodysplastic syndrome and acute myeloid leukemia by inhibiting DNA methyltransferases and inducing apoptosis in leukemia cells.
Data Source
AI summary
Methods and compositions are provided for treating myelodysplastic syndrome and acute myeloid leukemia, wherein the composition comprises at least one compound according to Formula I:wherein R1 is selected from the group consisting of —NH2, —NH—CH2—CO2H, —NH—CH(CH3)—CO2H, and —NH—C(CH3)2—CO2H, or a pharmaceutically acceptable salt of such a compound; and a DNA methyltransferase inhibitor, or a pharmaceutically acceptable salt thereof.