IL-15/IL-15Rα Heterodimer Dose Escalation Regimens

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Solution Overview

Problem

Current therapies for enhancing IL-15-mediated immune function, particularly in treating cancer, infectious diseases, and HIV, face challenges in achieving effective dosing without systemic toxicity and maintaining lymphocyte activation while avoiding side effects such as blood pressure changes and increased body temperature.

Innovation Solution

A dose escalation regimen of IL-15/IL-15Rα complexes, where IL-15 is covalently or noncovalently bound to IL-15Rα, is administered in escalating doses to maintain an effective ratio of IL-15 to lymphocyte cells, ensuring lymphocyte proliferation and survival without systemic viral load increase, and can be combined with other therapies like monoclonal antibodies.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If high doses of IL-15 are administered to enhance immune function, then lymphocyte activation and proliferation are improved, but systemic toxicity and side effects such as blood pressure changes and increased body temperature occur

Engineering Contradiction:
Improveimmune function enhancementVSAvoidsystemic toxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses IL-15Rα as an intermediary component to deliver IL-15 in a controlled manner. The heterodimer complex of IL-15 and IL-15Rα serves as a mediator that targets IL-15 delivery to specific cells expressing the IL-15 receptor, reducing systemic exposure and toxicity while maintaining immune enhancement effects

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent implements a dose escalation regimen that systematically increases the dose of IL-15/IL-15Rα complex from low to high levels over time. This parameter change approach allows the immune system to adapt gradually, achieving effective lymphocyte activation while minimizing acute systemic toxicity and side effects

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If dose escalation regimen is used to reduce toxicity, then treatment safety is improved, but treatment duration and complexity increase

Engineering Contradiction:
Improvesystemic toxicityVSAvoidtreatment duration
Core Design Contradiction:
Object-affected harmful factorsVSLoss of time

Solution Approach 1:

The patent employs a structured dose escalation protocol where patients receive progressively increasing doses according to a predetermined schedule. This preliminary planning of dose increments allows for systematic toxicity management while establishing an effective therapeutic dose efficiently, balancing safety with treatment time

Inventive Principle:
Principle #10Preliminary 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

This approach effectively enhances immune function, activates lymphocytes, and reduces HIV in HIV-infected cells without significant side effects, achieving a balance of IL-15 levels to support lymphocyte health and immune response.

Implementation Method 1

IL-15 signaling has been shown to occur through the heterodimeric complex of IL-15Rβ and IL-15R γ. This heterodimeric complex can bind to the IL-2/IL-15 βγ receptor and activate the cells via the Jak/Stat pathway.

Methodology Applied
Scientific EffectCytokine signaling:

Implementation Method 2

IL-15 heterodimers released from the cell surface after cleavage of the membrane bound heterodimers binds to the IL-15 βγ Receptor on lymphocytes.

Methodology Applied
Scientific EffectProteolytic cleavage:

Data Source

PatentEP3174974B1Il-15 and il-15ralpha heterodimer dose escalation regimens for treating conditions
Publication Date: 2020.05.20 NOVARTIS AG
  • EP3174974B1 patent drawingFigure 1A~1B
  • EP3174974B1 patent drawingFigure 2A~2B
  • EP3174974B1 patent drawingFigure 3A~3B

AI summary

Described herein are dose escalation regimens for the administration of complexes comprising interleukin-15 ("IL-15") covalently or noncovalently bound to IL-15 receptor alpha ("IL-15Rα") to patients in order to enhance IL-15 -mediated immune function. In a specific aspect, the dose escalation regimens are useful in the prevention, treatment, and/or management of disorders in which enhancing IL-15 -mediated function is beneficial, such as cancer, infectious diseases, immunodeficienices and lymphopenia. In another specific aspect, the dose escalation regimens are useful for eradicating or reducing HIV in HIV- infected patients.