Chiauranib and Immune Checkpoint Inhibitor Combination for Synergistic Antitumor Therapy
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Solution Overview
Problem
Current combinations of targeted therapy drugs and immune checkpoint inhibitors in cancer treatment face challenges in predicting efficacy, achieving optimal dosing, reducing adverse events, and enhancing clinical outcomes, particularly due to the complex mechanisms involved in tumor targeted therapy and immunotherapy.
Innovation Solution
The combination of chiauranib, a small molecule antitumor targeted drug with multiple protein kinase inhibition activity, and an immune checkpoint inhibitor, such as a PD-1 or PD-L1 inhibitor, to create a synergistic antitumor effect through inhibition of tumor angiogenesis, cell mitosis, and inflammatory microenvironment regulation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If targeted therapy drugs and immune checkpoint inhibitors are used in combination, then antitumor efficacy is improved, but the complexity of predicting efficacy and achieving optimal dosing increases
Solution Approach 1:
The patent combines chiauranib (a targeted therapy drug with VEGFR/PDGFR/c-Kit inhibition activity) and immune checkpoint inhibitors (anti-PD-1 or anti-PD-L1 antibodies) into a fixed-ratio combination product. This merging of two distinct therapeutic mechanisms into a single formulated product simplifies the dosing complexity while maintaining synergistic antitumor efficacy, as the fixed ratio pre-determines the optimal dosing relationship between the two agents
2Productivity
If higher doses of targeted therapy drugs and immune checkpoint inhibitors are used, then tumor inhibition rate increases, but adverse events increase
Solution Approach 1:
The patent establishes specific dosage parameters for the combination therapy: chiauranib at 50-200 mg/day (preferably 100 mg/day) combined with anti-PD-1 antibody at 100-500 mg (preferably 200 mg) or anti-PD-L1 antibody at 250-1000 mg (preferably 500 mg). These optimized parameter ranges achieve synergistic tumor inhibition while minimizing adverse events, as evidenced by the improved tumor inhibition rates with reduced toxicity observed in animal models
Data Source
AI summary
The present invention relates to the field of medicines, and in particular relates to use of chiauranib in combination with an immune checkpoint inhibitor in antitumor therapy. Use of a combination of chiauranib or a derivative thereof and the immune checkpoint inhibitor in the preparation of a medicine for treating a tumor, a pharmaceutical composition and a kit comprising the combination, and a method for treating a tumor by administering a therapeutically effective amount of the pharmaceutical composition or the kit to a tumor patient in need thereof. The combination has a synergistic effect and is suitable for treating a cancer.