V2R Antagonist Combinations for Clear Cell Renal Carcinoma

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Solution Overview

Problem

Current therapeutic methods are inadequate for effectively treating clear cell renal cell carcinoma (RCC), particularly in suppressing tumor growth and proliferation, as V2R antagonists have shown mixed results in RCC cell lines and human tumors.

Innovation Solution

The use of V2R antagonists such as OPC31260 and OPC41061, administered effectively to subjects, which inhibit V2R signaling, reducing cell proliferation, angiogenesis, and tumor growth in clear cell RCC by inducing cell cycle arrest and apoptosis.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If V2R antagonists are used to treat clear cell renal cell carcinoma, then tumor growth suppression is improved, but treatment reliability is worsened due to mixed results in RCC cell lines and human tumors

Engineering Contradiction:
Improvetumor growth suppressionVSAvoidtreatment consistency
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent combines multiple V2R antagonists (OPC31260 and OPC41061) in specific dosage ratios to change the treatment parameters, achieving synergistic effects that improve both tumor growth suppression and treatment consistency compared to single-agent therapy

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention uses a composite approach by combining two different V2R antagonist compounds (OPC31260 and OPC41061) into a single treatment regimen, where the composite effect of both agents addresses the reliability issue while maintaining improved tumor growth suppression

Inventive Principle:
Principle #40Composite materials

2Productivity

If higher doses of V2R antagonists are administered to improve tumor growth suppression, then therapeutic efficacy is improved, but potential side effects worsen

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidside effects
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent uses sub-maximal doses of each individual V2R antagonist (OPC31260 and OPC41061) in combination, where the partial action of each agent at lower doses achieves the same therapeutic efficacy as higher single-agent doses while reducing side effects through synergistic interaction

Inventive Principle:
Principle #16Partial or excessive action

Data Source

PatentUS11110098B2Methods and medicaments for the treatment of renal cell carcinoma
Publication Date: 2021.09.07 UNIVERSITY OF KANSAS
  • US11110098B2 patent drawing
  • US11110098B2 patent drawing
  • US11110098B2 patent drawing

AI summary

The present disclosure is directed, among other things, to the surprising and unexpected efficacy provided by select V2R antagonists in significantly reducing the cell proliferation levels of clear cell renal cell carcinoma. Thus, the present disclosure provides methods, uses, and medicaments that include such select V2R antagonists for utility in treating clear cell renal cell carcinoma.