Copanlisib and Anti-PD-1 Antibody Combination for Cancer Resistance
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Solution Overview
Problem
Current cancer therapies, particularly those targeting the PI3K pathway and immune checkpoint inhibitors, face challenges in overcoming tumor resistance and enhancing anti-tumor immunity, with limited efficacy in cancers with altered PI3K activation and impaired immune responses.
Innovation Solution
Combining 2,3-dihydroimidazo[1,2-c]quinazoline compounds with anti-PD-1 antibodies, administered in various pharmaceutical formulations, to inhibit PI3K and PD-1 pathways synergistically, thereby enhancing anti-tumor activity and overcoming resistance.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If PI3K pathway inhibitors are used to treat cancer, then tumor cell survival signaling is blocked, but tumor resistance and impaired anti-tumor immunity develop
Solution Approach 1:
The patent combines PI3K pathway inhibitors with anti-PD-1 antibodies into a dual-target therapy regimen. This merging of two distinct therapeutic mechanisms addresses both tumor cell survival signaling and immune checkpoint inhibition simultaneously, overcoming the resistance that develops with single-agent therapy and enhancing overall anti-tumor efficacy through synergistic action
2Reliability
If anti-PD-1 antibodies are used to enhance anti-tumor immunity, then immune response is activated, but efficacy is limited in cancers with altered PI3K activation
Solution Approach 1:
The patent merges anti-PD-1 antibody therapy with PI3K pathway inhibition to create a combination regimen that simultaneously blocks tumor survival signaling and activates immune response. This dual approach overcomes the limited efficacy of anti-PD-1 monotherapy in cancers with altered PI3K activation by addressing both the tumor's survival mechanisms and the immune system's functional status
3Reliability
If combination therapy is used to overcome resistance, then anti-tumor efficacy is enhanced, but treatment complexity increases
Solution Approach 1:
The patent merges two targeted therapies into a coordinated combination regimen with defined dosing schedules and administration protocols. While this enhances anti-tumor efficacy by addressing multiple resistance mechanisms, the treatment complexity is managed through structured combination protocols that specify timing, dosing, and monitoring parameters for both agents
Data Source
AI summary
* combinations of:component A: one or more 2,3-dihydroimidazo[1,2-c]quinazoline compounds of general formula (A1) or (A2) as defined herein, or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof;component B: anti-Programmed Cell Death Protein 1 (also referred to as “PD-1” or “CD279” (cluster of differentiation 279)) antibody (anti-PD-1 mAb) as defined herein; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially;independently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route;* use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and* a kit comprising such a combination.